| (11) | EP 2 006 271 A9 |
(12) | CORRECTED EUROPEAN PATENT APPLICATION |
published in accordance with Art. 153(4) EPC |
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(54) | SUBSTITUTED BICYCLIC CYCLIC DERIVATIVE AND USE THEREOF |
(57) [Object] To provide a compound having prostaglandin production-suppressing action and leukotriene production-suppressing action. [Means for solution] A compound represented by the formula (I): [In the formula, ---- represents a single bond, or a double bond, Link represents a single bond, or a saturated or unsaturated straight hydrocarbon having 1 or 2 carbon atoms, W represents a single bond, oxygen atom, sulfur atom, N(Rw) etc., Rw represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms etc, Rs represents -D-Rx etc., D represents a single bond, oxygen atom, sulfur atom etc., Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms etc., one of V1 and V2 represents Zx, and the other represents AR, Zx represents hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms etc., AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms etc.], or a salt thereof. |
Field of the Invention
Background Art
Patent document 1: WO99/19291
Patent document 2: U.S. Patent No. 5,391,817
Patent document 3: WO00/35886
Patent document 4: WO03/011842
Patent document 5: WO04/011446
Patent document 6: WO03/07686
Patent document 7: WO05/016862
Disclosure of the Invention
Object to be Achieved by the Invention
Means for Achieving the Object
<1> A compound represented by the formula (I):
[In the formula, ---- represents a single bond or a double bond (provided that both the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E), and the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety do not simultaneously represent a double bond, and when Link represents a single bond, the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond);
Link represents a single bond, or a saturated or unsaturated straight hydrocarbon having 1 or 2 carbon atoms ;
W represents a single bond, methylene group, oxygen atom, sulfur atom, or N(Rw);
Rw represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or - A6-Qp;
A6 represents a single bond or methylene group;
Qp represents phenyl group, and the phenyl group may be substituted with one of T1 or two or more of the same or different T1;
T1 represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, hydroxyl group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group, nitro group, an alkoxyl group having 1 to 4 carbon atoms, or a mono- or dialkylamino group having 1 to 4 carbon atoms;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, oxygen atom, sulfur atom, -S(O)-, -S(O)2-, or - C(O)-;
Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or represents Ra represented by the following formula:
R1-Aa- (Ra)
Rb represented by the following formula:
or Rc represented by the following formula:
Aa in Ra represents a single bond, an alkylene (aa) having 1 to 3 carbon atoms, or an alkenylene (aa') having 2 or 3 carbon atoms, and the alkylene (aa) and the alkenylene (aa') may be independently substituted with a lower alkyl group having 1 to 4 carbon atoms;
R1 represents a saturated cyclic alkyl group having 3 to 7 carbon atoms or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, and R1 may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms;
Q in Rb represents a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or a heterocyclic ring (q), and binds to A2 at an arbitrary position, and the heterocyclic ring (q) contains 1 to 4 of the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom;
A1 represents a single bond, an alkylene (al) having 1 to 3 carbon atoms, or an alkenylene (a1') having 2 or 3 carbon atoms, and the alkylene (a1) and the alkenylene (a1') may be independently substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group;
A2 represents a single bond, oxygen atom, sulfur atom, -S(O)-, -S(O)2-, or - N(R4)-(provided that when A2 represents oxygen atom, sulfur atom, -S(O)-, -S(O)2., or -N(R4)-, A1 represents ethylene or trimethylene);
R2 and R3 independently represents hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group, -OR5, -N(R6)(R6'), - NHCOR7, -NHSO2R8, or -A6-Qa, or they bind to each other to represent methylenedioxy group;
Qa represents a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or heterocyclic ring (qa), binds to A6 at an arbitrary position on the ring, and may be substituted with one of T1 or two or more of the same or different T1, and the heterocyclic ring (qa) contains 1 to 4 of the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom;
R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms;
R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or -A6-Qa;
R8 represents a lower alkyl group having 1 to 4 carbon atoms;
R6 has the same meaning as that of R6, or binds to R6 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group, or morpholino group;
symbol p in Rc represents an integer of 2 to 4;
A4 represents a single bond, methylene, or ethylene;
A5 represents -C(O)-, -C(S)-, or -S(O)2-;
Rd represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa;
Re represents an alkyl group having 1 to 8 carbon atoms, -A6-Qa, -(CH2)iR14, - OR28, -SR28, or -N(R29)(R30);
symbol i represents an integer of 1 to 3;
R14 represents hydroxyl group, an alkoxyl group having 1 to 4 carbon atoms, carboxyl group, or an N,N-dialkylcarbamoyl group having 1 to 4 carbon atoms;
R28 represents an alkyl group having 1 to 8 carbon atoms or -A6-Qa;
R29 represents an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, or -A6-Qa;
R30 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group, or morpholino group;
Rz has the same meaning as that of Rx, or represents methyl group, ethyl group, or -A5-Re;
Ry represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or -A6-Qp represents, or binds to Rz to form, together with the nitrogen atom to which they bind, a saturated or unsaturated cyclic substituent (qy) having 3 to 7 atoms, the cyclic substituent (qy) may contain one of nitrogen atom, oxygen atom, or sulfur atom besides the nitrogen atom, and the cyclic substituent (qy) may further be substituted with one of Rf or two of the same or different Rf;
Rf represents an alkyl group having 1 to 8 carbon atoms or -A6-Qp;
one of V1 and V2 represents Zx, and the other represents AR;
Zx represents hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, fluorine atom, chlorine atom, bromine atom, nitro group, - OR9, or -N(Rn1)(Rn2);
R9 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or -A6-Qp;
Rn1 represents hydrogen atom or a linear or branched saturated alkyl group having 1 to 4 carbon atoms;
Rn2 has the same meaning as that of Rn1, or represents -COR23 or -SO2R24, or binds to Rn1 to form a 3- to 6-membered ring together with the nitrogen atom to
which they bind to form a saturated nitrogen-containing cycloalkyl group, or morpholino group;
R23 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxyl group having 1 to 4 carbon atoms, -O-A6-Qp, or -N(R25)(R26);
R25 represents hydrogen atom or a linear or branched saturated alkyl group having 1 to 4 carbon atoms;
R26 has the same meaning as that of R25, or binds to R25 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group, or morpholino group;
R24 represents a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono- or dialkylamino group having 1 to 4 carbon atoms;
AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or heterocyclic ring (ar), and may be substituted with one of Xa or two or more of the same or different Xa;
the heterocyclic ring (ar) contains 1 to 4 of the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom;
Xa represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, a saturated cyclic alkyl group having 3 to 7 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, -(CH2)iR14, -OR10, - N(R11)(R12), -SO2R13, or -COR27;
R10 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms or -(CH2)iR14;
R11 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms;
R12 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, -COR15, or -SO2R16, or binds to R11 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group, or morpholino group;
R15 represents a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, amino group, a mono- or dialkylamino group having 1 to 4 carbon atoms, or -A6-Qa;
R13 and R16 independently represent a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono- or dialkylamino group having 1 to 4 carbon atoms;
R27 represents hydrogen atom, hydroxyl group, an alkoxyl group having 1 to 4 carbon atoms, a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono- or dialkylamino group having 1 to 4 carbon atoms;
Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, -(CH2)mN(R18)(R19), or -C(R20)2OC(O)A3R21;
symbol m represents an integer of 2 or 3;
R18 has the same meaning as that of R19, or binds to R19 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group, or morpholino group;
R19 represents methyl group, ethyl group, or propyl group;
R20 represents hydrogen atom, methyl group, ethyl group, or propyl group;
R21 represents a lower alkyl group having 1 to 4 carbon atoms, a saturated cyclic alkyl group having 3 to 6 carbon atoms, or phenyl group; and
A3 represents a single bond or oxygen atom] (this compound may sometimes be hereinafter referred to simply as "Compound (I)" of the present invention"), or a salt thereof.
<2> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), V1 is Zx, and V2 is AR.
<3> The compound or salt thereof according to <1> or <2> mentioned above, wherein, in the formula (I), W is methylene group.
<4> The compound or salt thereof according to <1> or <2> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH; and W is methylene group.
<5> The compound or salt thereof according to <1> or <2> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH; and
W is methylene group.
<6> The compound or salt thereof according to <1> or <2> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2 and
W is methylene group.
<7> The compound or salt thereof according to <1> or <2> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond; the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2; and
W is oxygen atom.
<8> The compound or salt thereof according to <1> or <2> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2; and
W is NH or N(methyl).
<9> The compound or salt thereof according to any one of <1> to <8> mentioned above, wherein, in the formula (I), AR as V1 or V2 is a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-d]thiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene ring (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa).
<10> The compound or salt thereof according to any one of <1> to <8> mentioned above, wherein, in the formula (I), AR as V1 or V2 is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa).
<11> The compound or salt thereof according to any one of <1> to <8> mentioned above, wherein, in the formula (I), AR as V1 or V2 is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group.
<12> The compound or salt thereof according to any one of <1> to <8> mentioned above, wherein, in the formula (I), AR as V1 or V2 is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group.
<13> The compound or salt thereof according to any one of <1> to <12>, wherein, in the formula (I), when Rb is contained in Rs, Q in Rb is phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4H-chromenyl group, dihydrobenzodioxyl group, benzisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1,3-dihydrobenzimidazole group, dihydro-3H-benzoxazole group, or dihydro-3H-benzothiazole group (the aforementioned groups bind to A2 at an arbitrary position on the ring); and
when Qa exists in a moiety of the structure, Qa is phenyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, or indazolyl group (the aforementioned groups may be substituted with one of T1 or two or more of the same or different T1, and bind to A6 at an arbitrary position on the ring).
<14> The compound or salt thereof according to any one of <1> to <13>, wherein, in the formula (I), when Rs represents -D-Rx, D is a single bond, oxygen atom, or sulfur atom.
<15> The compound or salt thereof according to any one of <1> to <13>, wherein, in the formula (I), when Rs represents -D-Rx, D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
when Rx represents Rb, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
when Rs is -N(Ry)(Rz), Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the
same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group).
<16> The compound or salt thereof according to any one of <1> to <13>, wherein, in the formula (I), when Rs represents -D-Rx, D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, or cycloheptylmethyl group, or Rb mentioned above;
when Rx represents Rb, Q in Rb is phenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, or indan-2-yl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, or methylene group, methylmethylene group, or ethylene group when A2 is a single bond, or ethylene group when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, or dimethylamino group;
when Rs is -N(Ry)(Rz), Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from the group consisting of pyrrolidino group, piperidino group, morpholino group, and piperazino group, and the cyclic substituent (qy) may be substituted with one of substituent or two of the same or different substituents selected from methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, and phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group).
<17> The compound or salt thereof according to any one of <1> to <13>, wherein, in the formula (I), when Rs represents -D-Rx, D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group; and
when Rs represents -N(Ry)(Rz), -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-diffuorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(triffuoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group.
<18> The compound or salt thereof according to any one of <1> to <17> mentioned above, wherein, in the formula (I), when Rs represents -D-Rx, D is a single bond.
<19> The compound or salt thereof according to any one of <1> to <17> mentioned above, wherein, in the formula (I), Rs is -O-Rx.
<20> The compound or salt thereof according to any one of <1> to <15> mentioned above, wherein, in the formula (I), Rs is -S-Rx.
<21> The compound or salt thereof according to any one of <1> to <17> mentioned above, wherein, in the formula (I), Rs is -N(Ry)(Rz).
<22> The compound or salt thereof according to any one of <1> to <13>, wherein, in the formula (I), Rs is phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2,3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3-difluorophenyl group, 2,4-difluorophenyl group, 2,5-difluorophenyl group, 3,4-difluorophenyl group, 2,3-dichlorophenyl group, 2,4-dichlorophenyl group, 2,5-dichlorophenyl group, 2,6-dichlorophenyl group, 3,4-dichlorophenyl group, 3,5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4-(N,N-dimethylamino)phenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, or thiophen-3-yl group.
<23> The compound or salt thereof according to any one of <1> to <22> mentioned above, wherein, in the formula (I), Zx as V1 or V2 is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group.
<24> The compound or salt thereof according to any one of <1> to <22> mentioned above, wherein, in the formula (I), Zx as V1 or V2 is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group.
<25> The compound or salt thereof according to any one of <1> to <24> mentioned above, wherein, Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<26> The compound or salt thereof according to any one of <1> to <24> mentioned above, wherein, Y is hydrogen atom, methyl group, or ethyl group.
<27> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-d]thiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<28> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2;
W is oxygen atom;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline; benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-d]thiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<29> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2;
W is NH, or N(methyl);
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-dlthiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<30> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<31> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2;
W is oxygen atom;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group,
isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group,
methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<32> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2;
W is NH, or N(methyl);
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond, oxygen atom, or sulfur atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group,
isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<33> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is Rx;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<34> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -O-Rx;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<35> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -S-Rx;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<36> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -N(Ry)(Rz);
Rz is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y is hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
<37> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D represents a single bond, or oxygen atom;
Rx is a substituent of propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, or Rb mentioned above;
Q in Rb is phenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, or indan-2-yl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, or methylene group, methylmethylene group, or ethylene group when A2 is a single bond, or ethylene group when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, or dimethylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group(provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from the group consisting of pyrrolidino group, piperidino group, morpholino group, and piperazino group, and the cyclic substituent (qy) may be substituted with one of substituent or two of the same or different substituents selected from methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, and phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, indol-5-yl group, indol-4-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, quinolin-6-yl group, quinolin-3-yl group, dihydro-1H-quinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, dihydro-2H-isoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, N-methylamino group, N,N-dimethylamino group, 2-hydroxyethylamino group, or carboxyl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<38> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<39> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2; and
W is oxygen atom;
Rs is -D-Rx;
D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<40> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is oxygen atom;
Rs is -N(Ry)(Rz);
the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<41> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<42> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -O-Rx;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<43> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -N(Ry)(Rz);
the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<44> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2,3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3-difluorophenyl group, 2,4-difluorophenyl group, 2,5-difluorophenyl group, 3,4-difluorophenyl group, 2,3-dichlorophenyl group, 2,4-dichlorophenyl group, 2,5-dichlorophenyl group, 2,6-dichlorophenyl group, 3,4-dichlorophenyl group, 3,5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4-(N,N-dimethylamino)phenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, or thiophen-3-yl group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<45> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, or cycloheptylmethyl group, or Rb mentioned above;
Q in Rb is phenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, or indan-2-yl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, or methylene group, methylmethylene group, or ethylene group when A2 is a single bond, or ethylene group when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, or dimethylamino group;
Rz has the same meaning as that of Rx, or is methyl group, or ethyl group;
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from the group consisting of pyrrolidino group, piperidino group, morpholino group, and piperazino group, and the cyclic substituent (qy) may be substituted with one of substituent or two of the same or different substituents selected from methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, and phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, benzofuran-5-yl group, benzo[b]thiophen-5-yl group, indol-5-yl group, benzothiazol-6-yl group, quinolin-6-yl group, quinolin-3-yl group, 1H-indazol-5-yl group, isoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa is oxo group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, N-methylamino group, N,N-dimethylamino group, 2-hydroxyethylamino group, or carboxyl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<46> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<47> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
Rs is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<48> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
Rs is -O-Rx;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<49> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
Rs is -N(Ry)(Rz);
the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<50> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), W is methylene group, or oxygen atom;
when Rs represents -D-Rx, D is a single bond or oxygen atom;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group; and
AR is a residue of indole or 1H-indazole.
<51> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2 or CH2CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
when Rs represents -D-Rx, D is a single bond or oxygen atom;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group; and
AR is a residue of indole or 1H-indazole.
<52> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
when Rs represents -D-Rx, D is a single bond or oxygen atom;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group; and
AR is a residue of indole or 1H-indazole.
<53> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
when Rs represents -D-Rx, D is a single bond or oxygen atom;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group; and
AR is a residue of indole or 1H-indazole.
<54> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2, or CH2CH2; and
W is oxygen atom;
when Rs represents -D-Rx, D is a single bond or oxygen atom;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group; and
AR is a residue of indole or 1H-indazole.
<55> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond;
Link is CH2;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond or oxygen atom;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group; and
AR is a residue of indole or 1H-indazole.
<56> The compound or salt thereof according to any one of <50> to <55> mentioned above, wherein Rx is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group); and
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group. <57> The compound or salt thereof according to any one of <50> to <55> mentioned above, wherein Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group.
<58> The compound.or salt thereof according to any one of <50> to <57> mentioned above, wherein Rz is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb is a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb is a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 is oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 is ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group; and
Ry is hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz is methyl group, or ethyl group, Ry is a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group).
<59> The compound or salt thereof according to any one of <50> to <57> mentioned above, wherein the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group.
<60> The compound or salt thereof according to any one of <50> to <59> mentioned above, wherein AR is indol-5-yl group, indol-4-yl group, indol-6-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, or 1H-indazol-6-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa). <61> The compound or salt thereof according to any one of <50> to <59> mentioned above, wherein AR is 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, or 3-hydroxy-1-methyl-1H-indazol-5-yl group. <62> The compound or salt thereof according to any one of <50> to <59> mentioned above, whereinAR is 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, or 1-ethyl-1H-indazol-5-yl group.
<63> The compound or salt thereof according to <1> mentioned above, wherein, in the formula (I), the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) is a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a single bond, Link is CH2, or when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety is a double bond, Link is CH;
W is methylene group;
Rs is -D-Rx or -N(Ry)(Rz);
D is a single bond or oxygen atom;
Rx is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent -N(Ry)(Rz) is N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-diffuorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) is Zx, and V2 on the ring (E) is AR;
Zx is hydrogen atom or amino group;
AR is 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, or 1-ethyl-3-hydroxy-1H-indazol-5-yl group; and
Y is hydrogen atom, methyl group, or ethyl group.
<64> A medicament comprising a compound represented by the aforementioned formula (I) having an arbitrary combination of choices selected from all of those described in this specification or a pharmacologically acceptable salt thereof as an active ingredient.
The medicament of the present invention can be applied to various diseases as:
<65> An agent for suppressing production of a prostaglandin and/or a leukotriene, which comprises a compound represented by the aforementioned formula (I) having an arbitrary combination of choices selected from all of those described in this specification or a pharmacologically acceptable salt thereof as an active ingredient.
Specifically, there is provided:
<66> The medicament according to <64> mentioned above, which is for prophylactic and/or therapeutic treatment of a disease induced by production of a prostaglandin and/or a leukotriene;
and as the aforementioned medicament for prophylactic and/or therapeutic treatment of a disease, the present invention provides, for example:
<67> The medicament according to <64> mentioned above, which is for prophylactic and/or therapeutic treatment of an inflammatory disease of mammal;
<68> The medicament according to <64> mentioned above, which is for prophylactic and/or therapeutic treatment of an autoimmune disease of mammal;
<69> The medicament according to <64> mentioned above, which is for prophylactic and/or therapeutic treatment of an allergic disease of mammal;
<70> The medicament according to <64> mentioned above, which is for antipyresis and/or analgesis of mammal;
<71> The medicament according to <64> mentioned above, which is for prophylactic and/or therapeutic treatment of a fibrosis of mammal;
and the like.
<72> The medicament according to <64> mentioned above, which is for prophylactic and/or therapeutic treatment of a biological condition of mammal in which an acute or chronic inflammatory reaction is observed.
According to preferred embodiments of these medicaments, there is provided:
<73> The medicament according to any one of <64> to <72> mentioned above, which is in the form of a pharmaceutical composition comprising a prophylactically and/or therapeutically effective amount of a compound represented by the aforementioned formula (I) having an arbitrary combination of choices selected from all of those described in this specification or a pharmacologically acceptable salt thereof and a pharmacologically acceptable carrier.
<74> A method for prophylactic and/or therapeutic treatment of a disease induced by production of a prostaglandin and/or a leukotriene, which comprises administering a prophylactically and/or therapeutically effective amount of a compound represented by the aforementioned formula (I) having an arbitrary combination of choices selected from all of those described in this specification or a pharmacologically acceptable salt thereof to a mammal.
As the aforementioned method for prophylactic and/or therapeutic treatment, the present invention provides:
<75> The method according to <74> mentioned above, which is a method for prophylactic and/or therapeutic treatment of an inflammatory disease of mammal; <76> The method according to <74> mentioned above, which is a method for prophylactic and/or therapeutic treatment of an autoimmune disease of mammal; <77> The method according to <74> mentioned above, which is a method for prophylactic and/or therapeutic treatment of an allergic disease of mammal;
<78> The method according to <74> mentioned above, which is a method for antipyresis and/or analgesis of mammal;
<79> The method according to <74> mentioned above, which is a method for prophylactic and/or therapeutic treatment of a fibrosis of mammal;
and the like.
Effect of the Invention
Best Mode for Carrying out the Invention
the ring-constituting carbon atom at the 1-position of the ring (E)(double bond)CH-COOY;
the ring-constituting carbon atom at the 1-position of the ring (E)(double bond)CHCH2-COOY;
the ring-constituting carbon atom at the 1-position of the ring (E)-CH(double bond)CH-COOY;
the ring-constituting carbon atom at the 1-position of the ring (E)(double bond)C-(double bond)CH-COOY;
the ring-constituting carbon atom at the 1-position of the ring (E)-C(triple bond)C-COOY;
and the like. Among them,
the ring-constituting carbon atom at the 1-position of the ring (E)(double bond)CH-COOY;
is a particularly preferred example.
As Link, CH, CH2, and CH2CH2 are preferred examples, CH, and CH2 are particularly preferred examples, and CH2 is an extremely preferred example.[Rz represents a substituent which is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group represents, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;[Rz represents a substituent which is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, or cycloheptylmethyl group, or Rb mentioned above;
Q in Rb represents phenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, or indan-2-yl group;the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2 or CH2CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, oxygen atom, or sulfur atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or represents methyl group, or ethyl group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-d]thiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group,
(N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents either CH2 or CH2CH2;
W represents oxygen atom;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, oxygen atom, or sulfur atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or represents methyl group, or ethyl group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-d]thiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a double bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents either CH2 or CH2CH2;
W represents NH, or N(methyl);
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, oxygen atom, or sulfur atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or represents methyl group, or ethyl group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents a residue of naphthalene, benzofuran, benzo[b]thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo[d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H-indazole, imidazo[1,2-a]pyridine, 1H-pyrrolo[2,3-b]pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo[3,2-b]pyridine, benzo[1,2,5]thiadiazole, 1H-benzotriazole, 1,3-dihydropyrrolo[2,3-b]pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1,8]naphthylidine, [1,5]naphthylidine, 1H-pyrrolo[3,2-c]pyridine, 1H-pyrrolo[2,3-c]pyridine, 1H-pyrazolo[4,3-b]pyridine, 1H-pyrazolo[4,3-c]pyridine, 1H-pyrazolo[3,4-c]pyridine, 1H-pyrazolo[3,4-b]pyridine, [1,2,4]triazolo[4,3-a]pyridine, thieno[3,2-c]pyridine, thieno[3,2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindole, 1H-pyrazolo[3,4-d]thiazole, 2H-isoindole, [1,2,4]triazolo[1,5-a]pyrimidine, 1H-pyrazolo[3,4-b]pyrazine, 1H-imidazo[4,5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2 or CH2CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, oxygen atom, or sulfur atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Rz has the same meaning as that of Rx, or represents methyl group, or ethyl group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents a group which is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2 or CH2CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents Rx;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2 or CH2CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -O-Rx,;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2 or CH2CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -S-Rx;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, or Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R3 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2 or CH2CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -N(Ry)(Rz);
Rz represents a substituent which is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, or 2-cycloheptylethyl group, Rb mentioned above;
Q in Rb represents a group which is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, methylene group, methylmethylene group, ethylmethylene group, phenylmethylene group, ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group (provided that when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-, A1 represents ethylene group, methylethylene group, dimethylethylene group, ethylethylene group, phenylethylene group, ethenylene group, trimethylene group, or methyltrimethylene group);
R2 and R8 independently represents hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, N,N-dimethylamino group, piperidino group, morpholino group, acetylamino group, or methylsulfonylamino group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, homopiperidino group, morpholino group, piperazino group, homopiperazino group, pyrrol-1-yl group, imidazol-1-yl group, pyrazol-1-yl group, and thiomorpholino group, and the cyclic substituent (qy) may be substituted with one of alkyl group having 1 to 8 carbon atoms or two of the same or different alkyl groups having 1 to 8 carbon atoms, phenyl group, or phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, or N,N-dimethylamino group;
AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, benzo[b]thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo[d]isothiazol-5-yl group, benzo[d]isothiazol-4-yl group, benzo[d]isothiazol-6-yl group, benzo[d]isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo[c]isothiazol-5-yl group, benzo[c]isothiazol-4-yl group, benzo[c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo[1,2-a]pyridin-7-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1H-pyrrolo[2,3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo[3,2-b]pyridin-5-yl group, 1H-pyrrolo[3,2-b]pyridin-6-yl group, benzo[1,2,5]thiadiazol-5-yl group, benzo[1,2,5]thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-5-yl group, 1,3-dihydropyrrolo[2,3-b]pyridin-4-yl group, 1,3-dihydrobenzimidazol-5-yl group, 1,3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1,8]naphthylidin-3-yl group, [1,8]naphthylidin-4-yl group, [1,5]naphthylidin-3-yl group, [1,5]naphthylidin-4-yl group, 1H-pyrrolo[3,2-c]pyridin-6-yl group, 1H-pyrrolo[3,2-c]pyridin-4-yl group, 1H-pyrrolo[2,3-c]pyridin-5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, 1H-pyrazolo[4,3-b]pyridin-5-yl group, 1H-pyrazolo[4,3-b]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-6-yl group, 1H-pyrazolo[4,3-c]pyridin-4-yl group, 1H-pyrazolo[3,4-c]pyridin-5-yl group, 1H-pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo[3,4-b]pyridin-5-yl group, 1H-pyrazolo[3,4-b]pyridin-4-yl group, [1,2,4]triazolo[4,3-a]pyridin-6-yl group, [1,2,4]triazolo[4,3-a]pyridin-7-yl group, thieno[3,2-c]pyridin-2-yl group, thieno[3,2-c]pyridin-3-yl group, thieno[3,2-c]pyridin-6-yl group, thieno[3,2-b]pyridin-2-yl group, thieno[3,2-b]pyridin-3-yl group, thieno[3,2-b]pyridin-5-yl group, thieno[3,2-b]pyridin-6-yl group, 1H-thieno[3,2-c]pyrazol-5-yl group, 1H-thieno[3,2-c]pyrazol-4-yl group, benzo[d]isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo[d]isoxazol-6-yl group, benzo[d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo[c]isoxazol-6-yl group, benzo[c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizin-8-yl group, 1,3-dihydroindol-5-yl group, 1,3-dihydroindol-4-yl group, 1,3-dihydroindol-6-yl group, 1H-pyrazolo[3,4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1,2,4]triazolo[1,5-a]pyrimidin-6-yl group, 1H-pyrazolo[3,4-b]pyrazin-5-yl group, 1H-imidazo[4,5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N,N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N,N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N,N-dimethylsulfamoyl)amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N,N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N,N-dimethylcarbamoyl group; and
Y represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, or oxygen atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, or cycloheptylmethyl group, or Rb mentioned above;
Q in Rb represents phenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, or indan-2-yl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, or methylene group, methylmethylene group, or ethylene group when A2 represents a single bond, or ethylene group when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, or dimethylamino group;
Rz has the same meaning as that of Rx, or represents methyl group, or ethyl group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, morpholino group, and piperazino group, and the cyclic substituent (qy) may be substituted with one substituent or two of the same or different substituents selected from methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, and phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a substituent which is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzo[b]thiophen-5-yl group, benzo[b]thiophen-4-yl group, indol-5-yl group, indol-4-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, quinolin-6-yl group, quinolin-3-yl group, dihydro-1H-quinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, dihydro-2H-isoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, N-methylamino group, N,N-dimethylamino group, 2-hydroxyethylamino group, or carboxyl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, or oxygen atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent -N(Ry)(Rz) represents N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a group which is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a group which is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -O-Rx;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a group which is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents -N(Ry)(Rz);
the substituent -N(Ry)(Rz) represents N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a group which is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, or a double bond;
when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond, Link represents CH2, and when the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a double bond, Link represents CH;
W represents methylene group;
Rs represents phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2,3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3-difluorophenyl group, 2,4-difluorophenyl group, 2,5-difluorophenyl group, 3,4-difluorophenyl group, 2,3-dichlorophenyl group, 2,4-dichlorophenyl group, 2,5-dichlorophenyl group, 2,6-dichlorophenyl group, 3,4-dichlorophenyl group, 3,5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4-(N,N-dimethylamino)phenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, or thiophen-3-yl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a group which is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino)naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2,3-dimethylbenzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 2-methylbenzo[b]thiophen-5-yl group, 3-methylbenzo[b]thiophen-5-yl group, 2,3-dimethylbenzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1,2-dimethyl-1H-indol-5-yl group, 1,3-dimethyl-1H-indol-5-yl group, 1,2,3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2,3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2,3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 2,3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, benzo[d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, or oxygen atom;
Rx represents a substituent which is propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, or cycloheptylmethyl group, or Rb mentioned above;
Q in Rb represents phenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, or indan-2-yl group;
A2 in Rb represents a single bond, oxygen atom, sulfur atom, -N(methyl)-, or - N(ethyl)-;
A1 in Rb represents a single bond, or methylene group, methylmethylene group, or ethylene group when A2 represents a single bond, or ethylene group when A2 represents oxygen atom, sulfur atom, -N(methyl)-, or -N(ethyl)-;
R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, or dimethylamino group;
Rz has the same meaning as that of Rx, or represents methyl group, or ethyl group;
Ry represents hydrogen atom, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, or isopentyl group (provided that when Rz represents methyl group, or ethyl group, Ry represents a substituent other than hydrogen atom), or may bind to Rz to form, together with the nitrogen atom, a cyclic substituent (qy) selected from pyrrolidino group, piperidino group, morpholino group, and piperazino group, and the cyclic substituent (qy) may be substituted with one substituent or two of the same or different substituents selected from methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, and phenylmethyl group (provided that the benzene ring of the phenyl group, or the phenylmethyl group may be substituted with one of substituent or two of the same or different substituents selected from the group consisting of methyl group, fluorine atom, chlorine atom, trifluoromethyl group, hydroxyl group, methoxy group, and dimethylamino group);
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents a substituent which is naphthalen-2-yl group, benzofuran-5-yl group, benzo[b]thiophen-5-yl group, indol-5-yl group, benzothiazol-6-yl group, quinolin-6-yl group, quinolin-3-yl group, 1H-indazol-5-yl group, isoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa);
Xa represents oxo group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, N-methylamino group, N,N-dimethylamino group, 2-hydroxyethylamino group, or carboxyl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, or oxygen atom;
Rx represents a group which is propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent -N(Ry)(Rz) represents N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-l,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -O-Rx;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, and 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, and N-methylamino group;
AR represents naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -N(Ry)(Rz);
the substituent -N(Ry)(Rz) represents N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, amino group, or N-methylamino group;
AR represents naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, benzo[b]furan-5-yl group, benzo[b]thiophen-5-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1,2-dihydroquinolin-6-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, isoquinolin-6-yl group, 1-oxo-1,2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -D-Rx or -N(Ry)(Rz);
D represents a single bond, or oxygen atom;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent -N(Ry)(Rz) represents N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom or amino group;
AR represents 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, or 1-ethyl-1H-indazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom or amino group;
AR represents 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, or 1-ethyl-1H-indazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -O-Rx;
Rx represents propyl group, isopropyl group, butyl group, isobutyl group, isopentyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, phenyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2-thienyl group, 3-thienyl group, 2-furyl group, 3-furyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-hydroxyindan-2-yl group, 5-hydroxyindan-2-yl group, 4,7-dihydroxyindan-2-yl group, 5,6-dihydroxyindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl)ethyl group, 1-(3-fluorophenyl)ethyl group, 1-(4-fluorophenyl)ethyl group, 1-(2-chlorophenyl)ethyl group, 1-(3-chlorophenyl)ethyl group, 1-(4-chlorophenyl)ethyl group, 1-(2-methoxyphenyl)ethyl group, 1-(3-methoxyphenyl)ethyl group, 1-(4-methoxyphenyl)ethyl group, benzyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3-(trifluoromethyl)phenylmethyl group, 4-(trifluoromethyl)phenylmethyl group, 2-hydroxyphenylmethyl group, 3-hydroxyphenylmethyl group, 4-hydroxyphenylmethyl group, 2-methoxyphenylmethyl group, 3-methoxyphenylmethyl group, 4-methoxyphenylmethyl group, 2-(2-methylphenyl)ethyl group, 2-(3-methylphenyl)ethyl group, 2-(4-methylphenyl)ethyl group, 2-(2-methoxyphenyl)ethyl group, 2-(3-methoxyphenyl)ethyl group, 2-(4-methoxyphenyl)ethyl group, 2-(2-fluorophenyl)ethyl group, 2-(3-fluorophenyl)ethyl group, 2-(4-fluorophenyl)ethyl group, 2-(2-chlorophenyl)ethyl group, 2-(3-chlorophenyl)ethyl group, 2-(4-chlorophenyl)ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2-[3-(trifluoromethyl)phenyl]ethyl group, 2-[4-(trifluoromethyl)phenyl]ethyl group, 2-[4-(N,N-dimethylamino)phenyl]ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy)ethyl group, 2-(3-chlorophenyloxy)ethyl group, 2-(4-chlorophenyloxy)ethyl group, 2-(phenylthio)ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2-(N-ethyl-N-phenylamino)ethyl group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom or amino group;
AR represents 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, or 1-ethyl-1H-indazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the ring-constituting carbon atom at the 2-position of the ring (E) represents a single bond;
the bond between the ring-constituting carbon atom at the 1-position of the ring (E) and the Link moiety represents a single bond;
Link represents CH2;
W represents methylene group;
Rs represents -N(Ry)(Rz);
the substituent -N(Ry)(Rz) represents N,N-dimethylamino group, N-ethyl-N-methylamino group, N,N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N-isopentylamino group, N-isopentyl-N-methylamino group, N-ethyl-N-isopentylamino group, N-(2-ethylbutyl)amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N-(cyclopentylmethyl)amino group, N-(cyclopentylmethyl)-N-methylamino group, N-(cyclohexylmethyl)amino group, N-(cyclohexylmethyl)-N-methylamino group, N-phenylamino group, N-(2-methylphenyl)amino group, N-(4-methylphenyl)amino group, N-(2-fluorophenyl)amino group, N-(3-fluorophenyl)amino group, N-(4-fluorophenyl)amino group, N-(2-chlorophenyl)amino group, N-(3-chlorophenyl)amino group, N-(4-chlorophenyl)amino group, N-(indan-2-yl)amino group, N-(1-phenylethyl)amino group, N-[1-(2-fluorophenyl)ethyl]amino group, N-[1-(3-fluorophenyl)ethyl]amino group, N-[1-(4-fluorophenyl)ethyl]amino group, N-[1-(2-chlorophenyl)ethyl]amino group, N-[1-(3-chlorophenyl)ethyl]amino group, N-[1-(4-chlorophenyl)ethyl]amino group, N-benzylamino group, N-benzyl-N-methylamino group, N-benzyl-N-ethylamino group, N-(2-methylphenylmethyl)amino group, N-methyl-N-(2-methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N-methyl-N-(3-methylphenylmethyl)amino group, N-(4-methylphenylmethyl)amino group, N-methyl-N-(4-methylphenylmethyl)amino group, N-(2-fluorophenylmethyl)amino group, N-(2-fluorophenylmethyl)-N-methylamino group, N-(3-fluorophenylmethyl)amino group, N-(3-fluorophenylmethyl)-N-methylamino group, N-(4-fluorophenylmethyl)amino group, N-(4-fluorophenylmethyl)-N-methylamino group, N-(2-chlorophenylmethyl)amino group, N-(2-chlorophenylmethyl)-N-methylamino group, N-(3-chlorophenylmethyl)amino group, N-(3-chlorophenylmethyl)-N-methylamino group, N-(4-chlorophenylmethyl)amino group, N-(4-chlorophenylmethyl)-N-methylamino group, N-(2,3-difluorophenylmethyl)amino group, N-(2,3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmethyl)amino group, N-(2,4-difluorophenylmethyl)-N-methylamino group, N-(2,5-difluorophenylmethyl)amino group, N-(2,5-difluorophenylmethyl)-N-methylamino group, N-(3,4-difluorophenylmethyl)amino group, N-(3,4-difluorophenylmethyl)-N-methylamino group, N-(3,5-difluorophenylmethyl)amino group, N-(3,5-difluorophenylmethyl)-N-methylamino group, N-(2,3-dichlorophenylmethyl)amino group, N-(2,3-dichlorophenylmethyl)-N-methylamino group, N-(2,4-dichlorophenylmethyl)amino group, N-(2,4-dichlorophenylmethyl)-N-methylamino group, N-(2,5-dichlorophenylmethyl)amino group, N-(2,5-dichlorophenylmethyl)-N-methylamino group, N-(2,6-dichlorophenylmethyl)amino group, N-(2,6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N-(3,4-dichlorophenylmethyl)-N-methylamino group, N-(3,5-dichlorophenylmethyl)amino group, N-(3,5-dichlorophenylmethyl)-N-methylamino group, N-[2-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[2-(trifluoromethyl)phenylmethyl]amino group, N-[3-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[3-(trifluoromethyl)phenylmethyl]amino group, N-[4-(trifluoromethyl)phenylmethyl]amino group, N-methyl-N-[4-(trifluoromethyl)phenylmethyl]amino group, pyrrolidino group, 2-methylpyrrolidino group, 3-methylpyrrolidino group, 2,5-dimethylpyrrolidino group, 3,4-dimethylpyrrolidino group, piperidino group, 2-methylpiperidino group, 3-methylpiperidino group, 4-methylpiperidino group, 4-ethylpiperidino group, 4-propylpiperidino group, 4-isopropylpiperidino group, 4-butylpiperidino group, 4-isobutylpiperidino group, 4-cyclopentylpiperidino group, 4-cyclohexylpiperidino group, 4-(cyclopentylmethyl)piperidino group, 4-(cyclohexylmethyl)piperidino group, 4-phenylpiperidino group, 4-(2-methylphenyl)piperidino group, 4-(4-methylphenyl)piperidino group, 4-(2-fluorophenyl)piperidino group, 4-(3-fluorophenyl)piperidino group, 4-(4-fluorophenyl)piperidino group, 4-(2-chlorophenyl)piperidino group, 4-(3-chlorophenyl)piperidino group, 4-(4-chlorophenyl)piperidino group, 4-benzylpiperidino group, 4-(2-methylphenylmethyl)piperidino group, 4-(3-methylphenylmethyl)piperidino group, 4-methylphenylmethyl)piperidino group, 4-(2,3-dimethylphenylmethyl)piperidino group, 4-(3,5-dimethylphenylmethyl)piperidino group, 4-(2-fluorophenylmethyl)piperidino group, 4-(3-fluorophenylmethyl)piperidino group, 4-(4-fluorophenylmethyl)piperidino group, 4-(2-chlorophenylmethyl)piperidino group, 4-(3-chlorophenylmethyl)piperidino group, 4-(4-chlorophenylmethyl)piperidino group, 4-(2,3-difluorophenylmethyl)piperidino group, 4-(2,4-difluorophenylmethyl)piperidino group, 4-(2,5-difluorophenylmethyl)piperidino group, 4-(3,4-difluorophenylmethyl)piperidino group, 4-(2,3-dichlorophenylmethyl)piperidino group, 4-(2,4-dichlorophenylmethyl)piperidino group, 4-(2,5-dichlorophenylmethyl)piperidino group, 4-(2,6-dichlorophenylmethyl)piperidino group, 4-(3,4-dichlorophenylmethyl)piperidino group, 4-(3,5-dichlorophenylmethyl)piperidino group, 4-(3,6-dichlorophenylmethyl)piperidino group, 4-(2-methoxyphenylmethyl)piperidino group, 4-(3-methoxyphenylmethyl)piperidino group, 4-(4-methoxyphenylmethyl)piperidino group, 2,6-dimethylpiperidino group, 3,5-dimethylpiperidino group, 4,4-dimethylpiperidino group, homopiperidino group, morpholino group, 3,5-dimethylmorpholino group, 4-phenylpiperazino group, 4-(2-methylphenyl)piperazino group, 4-(4-methylphenyl)piperazino group, 4-(2-fluorophenyl)piperazino group, 4-(3-fluorophenyl)piperazino group, 4-(4-fluorophenyl)piperazino group, 4-(2-chlorophenyl)piperazino group, 4-(3-chlorophenyl)piperazino group, 4-(4-chlorophenyl)piperazino group, 4-benzylpiperazino group, 4-(2-methylphenylmethyl)piperazino group, 4-(3-methylphenylmethyl)piperazino group, 4-methylphenylmethyl)piperazino group, 4-(2,3-dimethylphenylmethyl)piperazino group, 4-(3,5-dimethylphenylmethyl)piperazino group, 4-(2-fluorophenylmethyl)piperazino group, 4-(3-fluorophenylmethyl)piperazino group, 4-(4-fluorophenylmethyl)piperazino group, 4-(2-chlorophenylmethyl)piperazino group, 4-(3-chlorophenylmethyl)piperazino group, 4-(4-chlorophenylmethyl)piperazino group, 4-(2,3-difluorophenylmethyl)piperazino group, 4-(2,4-difluorophenylmethyl)piperazino group, 4-(2,5-difluorophenylmethyl)piperazino group, 4-(3,4-difluorophenylmethyl)piperazino group, 4-(2,3-dichlorophenylmethyl)piperazino group, 4-(2,4-dichlorophenylmethyl)piperazino group, 4-(2,5-dichlorophenylmethyl)piperazino group, 4-(2,6-dichlorophenylmethyl)piperazino group, 4-(3,4-dichlorophenylmethyl)piperazino group, 4-(3,5-dichlorophenylmethyl)piperazino group, 4-(3,6-dichlorophenylmethyl)piperazino group, 4-(2-methoxyphenylmethyl)piperazino group, 4-(3-methoxyphenylmethyl)piperazino group, or 4-(4-methoxyphenylmethyl)piperazino group;
the substituent V1 on the ring (E) represents Zx, and V2 on the ring (E) represents AR;
Zx represents hydrogen atom or amino group;
AR represents 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, or 1-ethyl-1H-indazol-5-yl group; and
Y represents hydrogen atom, methyl group, or ethyl group.
<Preparation methods of the compounds of the present invention>
(2) The deprotection reaction under an acidic condition is performed, for example, in an organic solvent (dichloromethane, chloroform, dioxane, ethyl acetate, anisole and the like) in the presence of an organic acid (acetic acid, trifluoroacetic acid, methanesulfonic acid, p-toluenesulfonic acid and the like), a Lewis acid (boron tribromide, boron trifluoride, aluminum bromide, aluminum chloride and the like), or an inorganic acid (hydrochloric acid, sulfuric acid and the like), or a mixture thereof (hydrogen bromide/acetic acid and the like) at a temperature of -10 to 100°C. There is also a method of adding ethanethiol, 1,2-ethanedithiol, or the like as an additive.
(3) The deprotection reaction by hydrogenolysis is performed, for example, in a solvent [ether type solvents (tetrahydrofuran, dioxane, dimethoxyethane, diethyl ether and the like), alcohol type solvents (methanol, ethanol and the like), benzene type solvents (benzene, toluene and the like), ketone type solvents (acetone, methyl ethyl ketone and the like), nitrile type solvents (acetonitrile and the like), amide type solvents (dimethylformamide and the like), ester type solvents (ethyl acetate and the like), water, acetic acid, mixtures of two or more types of those solvents, and the like] in the presence of a catalyst (palladium/carbon powder, platinum oxide (PtO2), activated nickel and the like) and a hydrogen source such as hydrogen gas of ordinary pressure or under pressurization, ammonium formate, or hydrazine hydrate at a temperature of -10 to 60°C.
(4) The deprotection reaction of silyl group is performed, for example, by using tetra-n-butylammonium fluoride or the like in a water-miscible organic solvent (tetrahydrofuran, acetonitrile and the like) at a temperature of -10 to 60°C.
(5) The deprotection reaction using a metal is performed, for example, in an acidic solvent (acetic acid, buffer of pH 4.2 to 7.2, a mixture of such a solution and an organic solvent such as tetrahydrofuran) in the presence of zinc powder with or without ultrasonication at a temperature of -10 to 60°C.
(6) The deprotection reaction using a metal complex is performed, for example, in an organic solvent (dichloromethane, dimethylformamide, tetrahydrofuran, ethyl acetate, acetonitrile, dioxane, ethanol and the like), water, or a mixture thereof in the presence of a trap reagent (tributyltin hydride, triethylsilane, dimedone, morpholine, diethylamine, pyrrolidine and the like), an organic acid (acetic acid, formic acid, 2-ethylhexanoic acid and the like) and/or an organic acid salt (sodium 2-ethylhexanoate, potassium 2-ethylhexanoate and the like) in the presence or absence of a phosphine type regent (triphenylphosphine and the like) by using a metal complex [tetrakistriphenylphosphine palladium(0), bis(triphenylphosphine) palladium(II) dichloride, palladium(II) acetate, tris(triphenylphosphine) rhodium(I) chloride and the like] at a temperature of -10 to 60°C.
Further, besides the aforementioned methods, the deprotection reaction can be performed by referring to and examining ordinary chemical literatures, for example, Protective Groups In Organic Synthesis, mentioned above, references cited in the literatures, and the like.[Preparation Method 1] (Step a)
[Preparation Method 2] (Step b)
[Preparation Method 3] (Step c)
[Preparation Method 4]
[Preparation Method 4] (Step d)
[Preparation Method 4] (Step e)
[Preparation Method 4] (Step f)
[Preparation Method 4] (Step f-1)
[Preparation Method 4] (Step f-2)
[Preparation Method 4] (Step f-3)
[Preparation Method 4] (Step f-4)
[Preparation Method 4] (Step h)
[Preparation Method 5]
[Preparation Method 5] (Step d)
[Preparation Method 5] (Step e)
[Preparation Method 5] (Step g)
[Preparation Method 6] (Step e)
[Preparation Method 7] (Step i)
[Preparation Method 8] (Step d)
[Preparation Method 8] (Step h)
[Preparation Method 8] (Step g)
[Preparation Method 9]
[Preparation Method 9] (Step j)
[Preparation Method 9] (Step k)
[Preparation Method 9] (Step k-1)
[Preparation Method 9] (Step k-2)
[Preparation Method 9] (Step k-3)
[Preparation Method 9] (Step 1)
[Preparation Method 9] (Step m)
[Preparation Method 9] (Step m-1)
[Preparation Method 9] (Step m-2)
[Preparation Method 9] (Step b)
[Preparation Method 9] (Step a)
[Preparation Method 10]
[Preparation Method 10] (Step j)
[Preparation Method 10] (Step k)
[Preparation Method 10] (Step 1)
[Preparation Method 10] (Step m)
[Preparation Method 10] (Step b)
[Preparation Method 10] (Step a)
[Preparation Method 11] (Step e)
Preparation Method 4, Step e.
[Preparation Method 12] (Step i)
[Preparation Method 13]
[Preparation Method 13] (Step h)
[Preparation Method 14]
[Preparation Method 14] (Step n-1)
[Preparation Method 14] (Step n-2)
[Preparation Method 14] (Step f)
[Preparation Method 14] (Step d)
[Preparation Method 14] (Step g)
[Preparation Method 15]
[Preparation Method 15] (Step f-2)
[Preparation Method 15] (Step o)
Examples
Structure | abbreviation | Structure | abbreviation | Structure | abbreviation |
|
cPenMeO |
|
cHexMeO |
|
iBuO |
|
2EtBuO |
|
2,3DMeBuO |
|
cPenO |
|
cHexO |
|
cHepO |
|
BnO |
|
(R)1PhEtO |
|
2ClBnO |
|
4FBnO |
|
2-IndanO |
|
2(4FPh)EtO |
|
2(4DMAPh)EtO |
|
2(3-Py)EtO |
|
2(PhO)EtO |
|
3F,4(OMe)BnO |
|
2FRMeO |
|
2TPMeO | ||
|
2-Nap |
|
1-Nap |
|
5-Ind |
|
1Me-5-Ind |
|
5-1Idz |
|
1Me-5-1Idz |
|
2Me-5-1Idz |
|
5-Bzt |
|
5-2ABzt |
|
2Me-5-Bzt |
|
5-BT |
|
5-BF |
|
3-Qu |
|
6-IQ |
Reference Example 1
Synthesis of 5-cyclopentyloxy-2,3-dihydroindan-1-one (Intermediate A-1) (Preparation Method 14, Step f-2)
Synthesis of ethyl 2-(5-cyclopentyloxy-2,3-dihydroinden-1-ylidene)acetate (Intermediate A-2) (Preparation Method 9, Step k-1)
Synthesis of ethyl 2-(5-cyclopentyloxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-3) (Preparation Method 9, Step j)
Synthesis of ethyl 2-(6-bromo-5-cyclopentyloxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-4) (Preparation Method 8, Step h)
Reference Example 2
Synthesis of 5-benzyloxy-2,3-dihydroindan-1-one (Intermediate A-5) (Preparation Method 14, Step f-1)
Synthesis of ethyl 2-(5-benzyloxy-2,3-dihydroinden-1-ylidene)acetate (Intermediate A-6) (Preparation Method 9, Step k-1)
Synthesis of ethyl 2-(5-hydroxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-7) (Preparation Method 9, Step j)
Synthesis of ethyl 2-(5-benzyloxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-8) (Preparation Method 4, Step f-1)
Synthesis of ethyl 2-(5-benzyloxy-6-bromo-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-9) (Preparation Method 8, Step h)
Reference Example 3
Synthesis of ethyl 2-(5-t-butyldiphenylsilyloxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-12)
Synthesis of ethyl 2-(6-bromo-5-t-butyldiphenylsilyloxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-13) (Preparation Method 8, Step h)
Synthesis of ethyl 2-(6-bromo-5-hydroxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-14)
Synthesis of ethyl 2-(6-bromo-5-cyclohexylmethyloxy-2,3-dihydro-1H-inden-1-yl)acetate (Intermediate A-15) (Preparation Method 4, Step f-1)
Table-Al | |||||
Reagent | The name of reagent | manifacture | Reagent | The name of reagent | manifacture |
Al1 | Cyclopentanol | TCI | Al19 | 5-Methoxy-2-indanol | |
Al2 | Cyclopentanemethanol | Ald | Al20 | 5,6-Dimethoxy-2-indanol | |
Al3 | Cyclohexanol | WAKO | Al21 | 5-Fluoro-2-indanol | |
Al4 | Cycloheptanol | TCI | Al22 | 1,2,3,4-Tetrahydro-2-naphthol | Acros |
Al5 | 2-Ethyl-1-butanol | TCI | Al23 | 1,2,3,4-Tetrahydro-1-naphthol | WAKO |
Al6 | 2-[4-(Dimethylamino)phenyl]ethan | Ald | Al24 | 2-(2-Methylphenyl)ethyl alcohol | TCI |
Al7 | 2-Phenoxyethanol | TCI | Al25 | 3-Fluorophenylethyl alcohol | Ald |
Al8 | Phenethyl Alcohol | TCI | Al26 | 2-(o-Chlorophenyl)ethanol | WAKO |
Al9 | 2-Fluorophenylethyl alcohol | TCI | Al27 | 2-Naphthaleneethanol | TCI |
Al10 | 4-Chlorophenylethyl alcohol | Ald | Al28 | 1-Naphthaleneethanol | Ald |
Al11 | 4-Methylcyclohexanol | WAKO | Al29 | 2-Hydroxymethyl-1,4-benzodioxan | WAKO |
Al12 | 1-Pheny-2-propanol | TCI | Al30 | 2-(Phenylthio)ethanol | WAKO |
Al13 | 2-Phenylpropane-1-ol | Al31 | (1-Methyl-1H-imidazol-5yl)methanol | MAYB | |
Al14 | 1-(2-Fluorophenyl)-2-Propylalcohol | Al32 | (1,5-Dimethyl-1H-pyrazol-3-yl)methanol | MAYB | |
Al15 | 1-(3-Trifluoromethylphenyl)-2-Propylalcohol | Al33 | 4-Pyridinemethanol | TCI | |
Al16 | 3-Pheny-1-butanol | Ald | Al34 | 6-Methyl-2-pyridinemethanol | TCI |
Al17 | 1-Indanol | TCI | Al35 | 2-Quinolinylmethanol | MAYB |
Al18 | 2-Hydroxyindan | TCI | Al36 | 3-(2-Hydroxyethyl)pyridine | WAKO |
Table-Hal | ||
Reagent | The name of reagent | Manufacture |
Hal1 | Benzyl bromide | TCI |
Hal2 | Cyclohexylmathyl bromide | TCI |
Hal3 | n-Propyl bromide | TCI |
Hal4 | Isopropyl bromide | TCI |
Hal5 | n-Butyl bromide | TCI |
Hal6 | Isobutyl bromide | WAKO |
Hal7 | 2-Fluorobenzyl bromide | TCI |
Hal8 | 3-Fluorobenzyl bromide | TCI |
Hal9 | 4-Fluorobenzyl bromide | TCI |
Hal10 | 2-Chlorobenzyl bromide | TCI |
Hal11 | 3-Chlorobenzyl bromide | TCI |
Hal12 | 4-Methylbenzyl chloride | TCI |
Hal13 | 4-(Trifluoromethyl)benzyl bromide | TCI |
Table-Int.A-1 | |||||||||
|
Exp. | Syn. | SM | Reagent | Rx | V1' | V2' | LCMS | ||
method | RTime | Mass | |||||||
Int.A-10 | 4f-2 | Int.A-7 | Al2 | cPenMeO | H | H | C | 303 (M++1) | |
Int.A-11 | 4-h | Int.A-10 | cPenMeO | H | Br | C | 381 (M+) | ||
Int.A-15 | 4f-1 | Int.A-14 | Hal2 | cHexMeO | H | Br | C | 395 (M+) | |
Int.A-16 | 4f-2 | Int.A-14 | Al3 | cHexO | H | Br | C | 381 (M+) | |
Int.A-17 | 4f-2 | Int.A-14 | Al4 | cHepO | H | Br | C | 395 (M+) | |
Int.A-18 | 4f-1 | Int.A-14 | Hal3 | nPrO | H | Br | C | 341 (M+) | |
Int.A-19 | 4f-1 | Int.A-14 | Hal4 | iPrO | H | Br | C | 341 (M+) | |
Int.A-20 | 4f-1 | Int.A-14 | Hal5 | nBuO | H | Br | C | 355 (M+) | |
Int.A-21 | 4f-1 | Int.A-14 | Hal6 | iBuO | H | Br | C | 355 (M+) |
Example A-a-1
Synthesis of ethyl 2-[5-cyclopentyloxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-a-1) (Preparation Method 4, Step e-1)
Example A-a-2
Synthesis of 2-[5-cyclopentyloxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-a-2) (Preparation Method 1, Step a)
Example A-a-21
Synthesis of ethyl 2-[6-(benzo[b]thiazol-5-yl)5-cyclopentyloxy-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-a-21) (Preparation Method 4, Step e-2)
Example A-a-22
Synthesis of 2-[6-(benzo[b]thiazol-5-yl)5-cyclopentyloxy-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-a-22) (Preparation Method 1, Step a)
Example A-a-107
Synthesis of ethyl 2-[5-hydroxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Intermediate A-22)
Synthesis of ethyl 2-[5-(2-fluorobenzyloxy)-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-a-107) (Preparation Method 4, Step f-1)
Example A-a-108
Synthesis of 2-[5-(2-fluorobenzyloxy)-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-a-108) (Preparation Method 1, Step a)
Example A-a-153
Synthesis of ethyl 2-[5-(4-dimethylaminophenyloxy)-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-a-153) (Preparation Method 4, Step f-2)
Example A-a-154
Synthesis of 2-[5-(4-dimethylaminophenyloxy)-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-a-154) (Preparation Method 1, Step a)
Table-BRA-1 | |||||
Reagent | The name of reagent | Manufacture | Reagent | The name of reagent | Manufacture |
BRA1 | 2-Naphthalene boronic acid | TCI | BRA30 | 4-Isopropyloxyphenyl boronic acid | Ald |
BRA2 | 5-1H-Indole boronic acid | Frontier | BRA31 | 3-n-Propyloxyphenyl boronic acid | Ald |
BRA3 | 1-Methyl-5-Indole boronic acid | Frontier | BRA32 | 4-n-Propyloxyphenyl boronic acid | Ald |
BRA4 | 1-Ethyl-5-Indole boronic acid | BRA33 | 3-n-Butyloxyphenyl boronic | Ald | |
BRA5 | 1-Methyl-4-indiole boronic | BRA34 | 4-n-Butyloxyphenyl boronic | Ald | |
BRA6 | 1-Methyl-6-indiole boronic acid | BRA35 | 3-(Dimethylamino) phenyl boronic acid | Frontier | |
BRA7 | 5-1 H-Indazole boronic acid | BRA36 | 4-(Dimethylamino) phenyl boronic acid | Ald | |
BRA8 | 1-Methyl-5-1H-Indazole-boronic acid | BRA37 | 2-Fluoropheny boronic acid | Ald | |
BRA9 | 1-Ethyll-5-1H-Indazole-boronic acid | BRA38 | 3-Fluoropheny boronic acid | Ald | |
BRA10 | 2-Methyl-5-2H-indazole boronic acid | BRA39 | 4-Fluoropheny boronic acid | Ald | |
BRA11 | 5-Benzofurane boronic acis | Maybridg | BRA40 | 2-Chlorophenyl boronic acid | Aid |
BRA12 | 5-Benzothiophene boronic | Ald | BRA41 | 3-Chlorophenyl boronic acid | Ald |
BRA13 | 6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinoline | Ald | BRA42 | 4-Chlorophenyl boronic acid | Ald |
BRA14 | Phenyl boronic acid | Ald | BRA43 | 2-(Trifluoromethyl) phenyl boronic acid | TCI |
BRA15 | 2-Methylphenyl boronic acid | Ald | BRA44 | 3-(Trifluoromethyl) phenyl boronic acid | TCI |
BRA16 | 3-Methylphenyl boronic acid | Ald | BRA45 | 4-(Trifluoromethyl) phenyl boronic acid | Ald |
BRA17 | 4-Methylphenyl boronic acid | Ald | BRA46 | 2,3-Difluorophenyl boronic | Ald |
BRA18 | 2-Ethylphenyl boronic acid | Ald | BRA47 | 2,4-Difluorophenyl boronic | Ald |
BRA19 | 4-Ethylphenyl boronic acid | Ald | BRA48 | 2,5-Difluorophenyl boronic | Ald |
BRA20 | 2-Isopropylphenyl boronic | Ald | BRA49 | 2,6-Difluorophenyl boronic | Ald |
BRA21 | 4-Isopropylphenyl boronic | WAKO | BRA50 | 3,4-Difluorophenyl boronic | Ald |
BRA22 | 1-n-Butylphenyl boronic acid | Ald | BRA51 | 3.5-Difluorophenyl boronic | Ald |
BRA23 | 4-t-Butylphenyl boronic acid | Ald | BRA52 | 2,4-Dichlorophenyl boronic | Ald |
BRA24 | 2-Methoxypheny boronic acid | Ald | BRA53 | 3,5-Dichlorophenyl boronic | Ald |
BRA25 | 3-Methoxyphenyl boronic acid | Ald | BRA54 | 3,4-Dichlorophenyl boronic | Ald |
BRA26 | 4-Methoxypheny boronic acid | Ald | BRA55 | 2,3-Dimethylphenyl boronic | Lancaster |
BRA27 | 2-Ethyloxypheny boronic acid | Ald | BRA56 | 2,4-Dimethylphenyl boronic | WAKO |
BRA28 | 3-Ethyloxypheny boronic acid | Ald | BRA57 | 2,6-Dimethylphenyl boronic | Ald |
BRA29 | 3-Isopropyloxyphenyl boronic acid | Ald |
Table-BRA-2 | |||||
Reagent | The name of reagent | Manufacture | Reagent | The name of reagent | Manufacture |
BRA58 | 2-Furyl boronic acid | Ald | BRA68 | Trans-2-(4-Chlorophenyl)vinylboronic acid | Ald |
BRA59 | 3-Furyl boronic acid | Ald | BRA69 | 2-Cyclohexylvinylboronic acid | Ald |
BRA60 | 2-Thienyl boronic acid | Ald | BRA70 | Trans-2-{4(Trifluoromethyl)-phenyl}vinylboronic acid | Ald |
BRA61 | 3-Thienyl boronic acid | Ald | BRA71 | Trans-2-(4-Methylphenyl)vinylboronic acid | Ald |
BRA62 | Pyridine-3-boronic acid | Ald | BRA72 | (E)-2-(3-Methoxyphenyl)-4,4,5,5-tetramethyl-(1,3,2)-dioxaborolate | Aid |
BRA63 | Pyridine-4-boronic acid | Ald | BRA73 | 2-(cis-1-ethyl-1-butenyl)benzo- | Ald |
BRA64 | Biphenyl-3-boronic acid | Ald | BRA74 | trans-1-Propen-1-ylboronic acid | Ald |
BRA65 | Biphenyl-4-boronic acid | Ald | BRA75 | Cis-1-Propen-1-ylboronic | Ald |
BRA66 | Trans-1-Hexene-1-ylboronic acid | Ald | BRA76 | 1-Pentenylboronic acid | Ald |
BRA67 | Trans-2-(4-Fluorophenyl)vinylboronic acid | Ald | BRA77 | Trimethylboroxine | Ald |
Table-Het | ||
Reagent | The name of reagent | manufacture |
Het1 | 5-Bromobenzothiazole | TCI |
Het2 | 3-Bromoquinoline | TCI |
Het3 | 6-Bromoisoquinoline |
Table-IntA-2 | |||||||||
|
Exp. | Syn. | SM | Reagent | Rx | V1' | V2' | LCMS | ||
method | RTime | Mass | |||||||
Int.A-22 | A-a-29 | HO | H | 2-Nap | C | 347 (M++1) | |||
Int.A-23 | A-a-31 | HO | H | 5-Ind | C | 336 (M++1) | |||
Int.A-24 | A-a-33 | HO | H | 1Me-5-Ind | C | 350(M++1) | |||
Int.A-25 | A-a-35 | HO | H | 5-1Idz | C | 337(M++1) | |||
Int.A-26 | A-a-37 | HO | H | 1Me-5-Idz | C | 351(M++1) | |||
Int.A-27 | A-a-39 | HO | H | 1Et-5-Idz | C | 365(M++1) | |||
Int.A-28 | A-a-41 | HO | H | 5-BF | C | 337(M++1) | |||
Int.A-29 | A-a-43 | HO | H | 6-Qu | C | 348(M++1) |
Table-A-a-1 | ||||||||||
|
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-1 | 4e-1 | Int.A-4 | BRA1 | cPenO | Et | H | 2-Nap | C | 415(M++1) | |
A-a-2 | 1-a | A-a-1 | cPenO | H | H | 2-Nap | C | 387(M++1) | ||
A-a-3 | 4e-1 | Int.A-4 | BRA2 | cPenO | Et | H | 5-Ind | C | 404(M++1) | |
A-a-4 | 1-a | A-a-3 | cPenO | H | H | 5-Ind | C | 376(M++1) | ||
A-a-5 | 4e-1 | Int.A-4 | BRA3 | cPenO | Et | H | 1Me-5-Ind | C | 418(M++1) | |
A-a-6 | 1-a | A-a-5 | cPenO | H | H | 1Me-5-Ind | C | 390(M++1) | ||
A-a-7 | 4e-1 | Int.A-4 | BRA4 | cPenO | Et | H | 1Et-5-Ind | C | 432(M++1) | |
A-a-8 | 1-a | A-a-7 | cPenO | H | H | 1Et-5-Ind | C | 404(M++1) | ||
A-a-9 | 4e-1 | Int.A-4 | BRA7 | cPenO | Et | H | 5-1Idz | C | 405M++1) | |
A-a-10 | 1-a | A-a-9 | cPenO | H | H | 5-1Idz | C | 377(M++1) | ||
A-a-11 | 4e-1 | Int.A-4 | BRA8 | cPenO | Et | H | 1Me-5-Idz | C | 419M++1) | |
A-a-12 | 1-a | A-a-11 | cPenO | H | H | 1Me-5-Idz | C | 391(M++1) | ||
A-a-13 | 4e-1 | Int.A-4 | BRA9 | cPenO | Et | H | 1Et-5-Idz | C | 433(M++1) | |
A-a-14 | 1-a | A-a-13 | cPenO | H | H | 1Et-5-Idz | C | 405(M++1) | ||
A-a-15 | 4e-1 | Int.A-4 | BRA10 | cPenO | Et | H | 2Me-5-Idz | C | 419(M++1) | |
A-a-16 | 1-a | A-a-15 | cPenO | H | H | 2Me-5-Idz | C | 391(M++1) | ||
A-a-17 | 4e-1 | Int.A-4 | BRA11 | cPenO | Et | H | 5-BF | C | 405(M++1) | |
A-a-18 | 1-a | A-a-17 | cPenO | H | H | 5-BF | C | 377(M++1) | ||
A-a-19 | 4e-1 | Int.A-4 | BRA12 | cPenO | Et | H | 5-BT | C | 421(M++1) | |
A-a-20 | 1-a | A-a-19 | cPenO | H | H | 5-BT | C | 393(M++1) | ||
A-a-21 | 4e-2 | Int.A-4 | Het1 | cPenO | Et | H | 5-Bzt | C | 422(M++1) | |
A-a-22 | 1-a | A-a-21 | cPenO | H | H | 5-Bzt | C | 394(M++1) | ||
A-a-23 | 4e-2 | Int.A-4 | Het2 | cPenO | Et | H | 3-Qu | C | 416(M++1) | |
A-a-24 | 1-a | A-a-23 | cPenO | H | H | 3-Qu | C | 388(M++1) | ||
A-a-25 | 4e-1 | Int.A-4 | BRA13 | cPenO | Et | H | 6-Qu | C | 416(M++1) | |
A-a-26 | 1-a | A-a-25 | cPenO | H | H | 6-Qu | C | 388(M++1) | ||
A-a-27 | 4e-2 | Int.A-4 | Het3 | cPenO | Et | H | 6-IQ | C | 416(M++1) | |
A-a-28 | 1-a | A-a-27 | cPenO | H | H | 6-IQ | C | 388(M++1) | ||
A-a-29 | 4e-1 | Int.A-9 | BRA1 | BnO | Et | H | 2-Nap | C | 437(M++1) | |
A-a-30 | 1-a | A-a-29 | BnO | H | H | 2-Nap | C | 409(M++1) | ||
A-a-31 | 4e-1 | Int.A-9 | BRA2 | BnO | Et | H | 5-Ind | C | 426(M++1) | |
A-a-32 | 1-a | A-a-31 | BnO | H | H | 5-Ind | C | 398(M++1) | ||
A-a-33 | 4e-1 | Int.A-9 | BRA3 | BnO | Et | H | 1Me-5-Ind | C | 440(M++1) | |
A-a-34 | 1-a | A-a-33 | BnO | H | H | 1Me-5-Ind | C | 412(M++1) | ||
A-a-35 | 4e-1 | Int.A-9 | BRA7 | BnO | Et | H | 5-1Idz | C | 427(M++1) | |
A-a-36 | 1-a | A-a-35 | BnO | H | H | 5-1Idz | C | 399(M++1) | ||
A-a-37 | 4e-1 | Int.A-9 | BRA8 | BnO | Et | H | 1Me-5-Idz | C | 441(M++1) | |
A-a-38 | 1-a | A-a-37 | BnO | H | H | 1Me-5-Idz | C | 413(M++1) | ||
A-a-39 | 4e-1 | Int.A-9 | BRA9 | BnO | Et | H | 1Et-5-Idz | C | 455(M++1) | |
A-a-40 | 1-a | A-a-39 | BnO | H | H | 1Et-5-Idz | C | 427(M++1) | ||
A-a-41 | 4e-1 | Int.A-9 | BRA11 | BnO | Et | H | 5-BF | C | 427(M++1) | |
A-a-42 | 1-a | A-a-41 | BnO | H | H | 5-BF | C | 399(M++1) | ||
A-a-43 | 4e-2 | Int.A-9 | BRA13 | BnO | Et | H | 6-Qu | C | 438(M++1) | |
A-a-44 | 1-a | A-a-43 | BnO | H | H | 6-Qu | C | 410(M++1) | ||
A-a-45 | 4e-1 | Int.A-11 | BRA2 | cPenMeO | Et | H | 5-Ind | C | 418(M++1) | |
A-a-46 | 1-a | A-a-45 | cPenMeO | H | H | 5-Ind | C | 390(M++1) |
Table-A-a-2 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-47 | 4e-1 | Int.A-11 | BRA4 | cPenMeO | Et | H | 1 Et-5-Ind | C | 446(M++1) | |
A-a-48 | 1-a | A-a-47 | cPenMeO | H | H | 1 Et-5-Ind | C | 418M++1) | ||
A-a-49 | 4e-1 | Int.A-11 | BRA8 | cPenMeO | Et | H | 1Me-5-Idz | C | 433(M++1) | |
A-a-50 | 1-a | A-a-49 | cPenMeO | H | H | 1Me-5-Idz | C | 405(M++1) | ||
A-a-51 | 4e-2 | Int.A-11 | Het2 | cPenMeO | Et | H | 3-Qu | C | 430(M++1) | |
A-a-52 | 1-a | A-a-51 | cPenMeO | H | H | 3-Qu | C | 402(M++1) | ||
A-a-53 | 4e-1 | Int.A-15 | BRA1 | cHexMeO | Et | H | 2-Nap | C | 443(M++1) | |
A-a-54 | 1-a | A-a-53 | cHexMeO | H | H | 2-Nap | C | 415(M++1) | ||
A-a-55 | 4e-1 | Int.A-15 | BRA3 | cHexMeO | Et | H | 1Me-5-Ind | C | 446(M++1) | |
A-a-56 | 1-a | A-a-55 | cHexMeO | H | H | 1Me-5-Ind | C | 418(M++1) | ||
A-a-57 | 4e-1 | Int.A-15 | BRA7 | cHexMeO | Et | H | 5-1Idz | C | 433(M++1) | |
A-a-58 | 1-a | A-a-57 | cHexMeO | H | H | 5-1Idz | C | 405(M++1) | ||
A-a-59 | 4e-2 | Int.A-15 | Het3 | cHexMeO | Et | H | 6-IQ | C | 444(M++1) | |
A-a-60 | 1-a | A-a-59 | cHexMeO | H | H | 6-IQ | C | 416(M++1) | ||
A-a-61 | 4e-1 | Int.A-16 | BRA3 | cHexO | Et | H | 1Me-5-Ind | C | 432(M++1) | |
A-a-62 | 1-a | A-a-61 | cHexO | H | H | 1Me-5-Ind | C | 404(M++1) | ||
A-a-63 | 4e-1 | Int.A-16 | BRA8 | cHexO | Et | H | 1Me-5-Idz | C | 433(M++1) | |
A-a-64 | 1-a | A-a-63 | cHexO | H | H | 1Me-5-Idz | C | 405(M++1) | ||
A-a-65 | 4e-2 | Int.A-16 | Het2 | cHexO | Et | H | 3-Qu | C | 430(M++1) | |
A-a-66 | 1-a | A-a-65 | cHexO | H | H | 3-Qu | C | 402(M++1) | ||
A-a-67 | 4e-1 | Int.A-16 | BRA13 | cHexO | Et | H | 6-Qu | C | 430(M++1) | |
A-a-68 | 1-a | A-a-67 | cHexO | H | H | 6-Qu | C | 402(M++1) | ||
A-a-69 | 4e-1 | Int.A-17 | BRA1 | cHepO | Et | H | 2-Nap | C | 443(M++1) | |
A-a-70 | 1-a | A-a-69 | cHepO | H | H | 2-Nap | C | 415(M++1) | ||
A-a-71 | 4e-1 | Int.A-17 | BRA2 | cHepO | Et | H | 5-Ind | C | 432(M++1) | |
A-a-72 | 1-a | A-a-71 | cHepO | H | H | 5-Ind | C | 404(M++1) | ||
A-a-73 | 4e-1 | Int.A-17 | BRA8 | cHepO | Et | H | 1Me-5-Idz | C | 447(M++1) | |
A-a-74 | 1-a | A-a-73 | cHepO | H | H | 1Me-5-Idz | C | 419(M++1) | ||
A-a-75 | 4e-1 | Int.A-17 | BRA13 | cHepO | Et | H | 6-Qu | C | 444(M++1) | |
A-a-76 | 1-a | A-a-75 | cHepO | H | H | 6-Qu | C | 416(M++1) | ||
A-a-77 | 4e-1 | Int.A-18 | BRA2 | nPrO | Et | H | 5-Ind | C | 378(M++1) | |
A-a-78 | 1-a | A-a-77 | nPrO | H | H | 5-Ind | C | 350(M++1) | ||
A-a-79 | 4e-1 | Int.A-18 | BRA3 | nPrO | Et | H | 1Me-5-Ind | C | 392(M++1) | |
A-a-80 | 1-a | A-a-79 | nPrO | H | H | 1Me-5-Ind | C | 364(M++1) | ||
A-a-81 | 4e-1 | Int.A-18 | BRA7 | nPrO | Et | H | 5-1Idz | C | 379(M++1) | |
A-a-82 | 1-a | A-a-81 | nPrO | H | H | 5-1Idz | C | 351(M++1) | ||
A-a-83 | 4e-1 | Int.A-18 | BRA8 | nPrO | Et | H | 1Me-5-Idz | C | 393(M++1) | |
A-a-84 | 1-a | A-a-83 | nPrO | H | H | 1Me-5-Idz | C | 365(M++1) | ||
A-a-85 | 4e-1 | Int.A-19 | BRA1 | iPrO | Et | H | 2-Nap | C | 389(M++1) | |
A-a-86 | 1-a | A-a-85 | iPrO | H | H | 2-Nap | C | 361(M++1) | ||
A-a-87 | 4e-1 | Int.A-19 | BRA3 | iPrO | Et | H | 1Me-5-Ind | C | 392(M++1) | |
A-a-88 | 1-a | A-a-87 | iPrO | H | H | 1Me-5-Ind | C | 364(M++1) | ||
A-a-89 | 4e-1 | Int.A-19 | BRA8 | iPrO | Et | H | 1Me-5-Idz | C | 393(M++1) | |
A-a-90 | 1-a | A-a-89 | iPrO | H | H | 1Me-5-Idz | C | 365(M++1) | ||
A-a-91 | 4e-1 | Int.A-19 | BRA13 | iPrO | Et | H | 6-Qu | C | 390(M++1) | |
A-a-92 | 1-a | A-a-91 | iPrO | H | H | 6-Qu | C | 362(M++1) | ||
A-a-93 | 4e-1 | Int.A-20 | BRA2 | nBuO | Et | H | 5-Ind | C | 392(M++1) | |
A-a-94 | 1-a | A-a-93 | nBuO | H | H | 5-Ind | C | 364(M++1) |
Table-A-a-3 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-95 | 4e-1 | Int.A-20 | BRA3 | nBuO | Et | H | 1Me-5-Ind | C | 406(M++1) | |
A-a-96 | 1-a | A-a-95 | nBuO | H | H | 1Me-5-Ind | C | 378(M++1) | ||
A-a-97 | 4e-1 | Int.A-20 | BRA8 | nBuO | Et | H | 1Me-5-Idz | C | 407(M++1) | |
A-a-98 | 1-a | A-a-97 | nBuO | H | H | 1Me-5-Idz | C | 379(M++1) | ||
A-a-99 | 4e-1 | Int.A-21 | BRA1 | iBuO | Et | H | 2-Nap | C | 403(M++1) | |
A-a-100 | 1-a | A-a-99 | iBuO | H | H | 2-Nap | C | 375(M++1) | ||
A-a-101 | 4e-1 | Int.A-21 | BRA3 | iBuO | Et | H | 1Me-5-Ind | C | 406(M++1) | |
A-a-102 | 1-a | A-a-101 | iBuO | H | H | 1Me-5-Ind | C | 378(M++1) | ||
A-a-103 | 4e-1 | Int.A-21 | BRA7 | iBuO | Et | H | 5-1Idz | C | 393(M++1) | |
A-a-104 | 1-a | A-a-103 | iBuO | H | H | 5-1Idz | C | 365(M++1) | ||
A-a-105 | 4e-2 | Int.A-21 | Het3 | iBuO | Et | H | 6-IQ | C | 404(M++1) | |
A-a-106 | 1-a | A-a-105 | iBuO | H | H | 6-IQ | C | 376(M++1) | ||
A-a-107 | 4f-1 | Int.A-22 | Hal7 | 2FBnO | Et | H | 2-Nap | C | 455(M++1) | |
A-a-108 | 1-a | A-a-107 | 2FBnO | H | H | 2-Nap | C | 427(M++1) | ||
A-a-109 | 4f-1 | Int.A-23 | Hal7 | 2FBnO | Et | H | 5-Ind | C | 444(M++1) | |
A-a-110 | 1-a | A-a-109 | 2FBnO | H | H | 5-Ind | C | 416(M++1) | ||
A-a-111 | 4f-1 | Int.A-26 | Hal7 | 2FBnO | Et | H | 1Me-5-Idz | C | 459(M++1) | |
A-a-112 | 1-a | A-a-111 | 2FBnO | H | H | 1Me-5-Idz | C | 430(M++1) | ||
A-a-113 | 4f-1 | Int.A-24 | Hal8 | 3FBnO | Et | H | 1Me-5-Ind | C | 458(M++1) | |
A-a-114 | 1-a | A-a-113 | 3FBnO | H | H | 1Me-5-Ind | C | 430(M++1) | ||
A-a-115 | 4f-1 | Int.A-26 | Hal8 | 3FBnO | Et | H | 1Me-5-Idz | C | 459(M++1) | |
A-a-116 | 1-a | A-a-115 | 3FBnO | H | H | 1Me-5-Idz | C | 431(M++1) | ||
A-a-117 | 4f-1 | Int.A-29 | Hal8 | 3FBnO | Et | H | 6-Qu | C | 456(M++1) | |
A-a-118 | 1-a | A-a-117 | 3FBnO | H | H | 6-Qu | C | 428(M++1) | ||
A-a-119 | 4f-1 | Int.A-22 | Hal9 | 4FBnO | Et | H | 2-Nap | C | 455(M++1) | |
A-a-120 | 1-a | A-a-119 | 4FBnO | H | H | 2-Nap | C | 427(M++1) | ||
A-a-121 | 4f-1 | Int.A-27 | Hal9 | 4FBnO | Et | H | 1Et-5-Idz | C | 473(M++1) | |
A-a-122 | 1-a | A-a-121 | 4FBnO | H | H | 1Et-5-Idz | C | 445(M++1) | ||
A-a-123 | 4f-1 | Int.A-28 | Hal9 | 4FBnO | Et | H | 5-BF | C | 445(M++1) | |
A-a-124 | 1-a | A-a-123 | 4FBnO | H | H | 5-BF | C | 417(M++1) | ||
A-a-125 | 4f-1 | Int.A-29 | Hal9 | 4FBnO | Et | H | 6-Qu | C | 456(M++1) | |
A-a-126 | 1-a | A-a-125 | 4FBnO | H | H | 6-Qu | C | 428(M++1) | ||
A-a-127 | 4f-1 | Int.A-22 | Hal10 | 2ClBnO | Et | H | 2-Nap | C | 471(M++1) | |
A-a-128 | 1-a | A-a-127 | 2ClBnO | H | H | 2-Nap | C | 443(M++1) | ||
A-a-129 | 4f-1 | Int.A-27 | Hal10 | 2ClBnO | Et | H | 1Et-5-Idz | C | 489(M++1) | |
A-a-130 | 1-a | A-a-129 | 2ClBnO | H | H | 1Et-5-Idz | C | 461(M++1) | ||
A-a-131 | 4f-1 | Int.A-28 | Hal10 | 2ClBnO | Et | H | 5-BF | C | 461(M++1) | |
A-a-132 | 1-a | A-a-131 | 2ClBnO | H | H | 5-BF | C | 433(M++1) | ||
A-a-133 | 4f-1 | Int.A-22 | Hal11 | 3ClBnO | Et | H | 2-Nap | C | 471(M++1) | |
A-a-134 | 1-a | A-a-133 | 3ClBnO | H | H | 2-Nap | C | 443(M++1) | ||
A-a-135 | 4f-1 | Int.A-23 | Hal11 | 3ClBnO | Et | H | 5-Ind | C | 460(M++1) | |
A-a-136 | 1-a | A-a-135 | 3ClBnO | H | H | 5-Ind | C | 432(M++1) | ||
A-a-137 | 4f-1 | Int.A-24 | Hal11 | 3ClBnO | Et | H | 1Me-5-Ind | C | 474(M++1) | |
A-a-138 | 1-a | A-a-137 | 3ClBnO | H | H | 1Me-5-Ind | C | 446(M++1) | ||
A-a-139 | 4f-1 | Int.A-26 | Hal11 | 3ClBnO | Et | H | 1Me-5-Idz | C | 475(M++1) | |
A-a-140 | 1-a | A-a-139 | 3ClBnO | H | H | 1Me-5-Idz | C | 447(M++1) | ||
A-a-141 | 4f-1 | Int.A-23 | Hal12 | 4MeBnO | Et | H | 5-Ind | C | 440(M++1) | |
A-a-142 | 1-a | A-a-141 | 4MeBnO | H | H | 5-Ind | C | 412(M++1) |
Table-A-a-4 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-143 | 4f-1 | Int.A-24 | Hal12 | 4MeBnO | Et | H | 1Me-5-Ind | C | 454(M++1) | |
A-a-144 | 1-a | A-a-143 | 4MeBnO | H | H | 1Me-5-Ind | C | 426(M++1) | ||
A-a-145 | 4f-1 | Int.A-26 | Hal12 | 4MeBnO | Et | H | 1Me-5-Idz | C | 455(M++1) | |
A-a-146 | 1-a | A-a-145 | 4MeBnO | H | H | 1Me-5-Idz | C | 427(M++1) | ||
A-a-147 | 4f-1 | Int.A-22 | Hal13 | 4CF3BnO | Et | H | 2-Nap | C | 505(M++1) | |
A-a-148 | 1-a | A-a-147 | 4CF3BnO | H | H | 2-Nap | C | 477(M++1) | ||
A-a-149 | 4f-1 | Int.A-24 | Hal13 | 4CF3BnO | Et | H | 1Me-5-Ind | C | 508(M++1) | |
A-a-150 | 1-a | A-a-149 | 4CF3BnO | H | H | 1Me-5-Ind | C | 480(M++1) | ||
A-a-151 | 4f-1 | Int.A-25 | Hal13 | 4CF3BnO | Et | H | 5-1Idz | C | 495(M++1) | |
A-a-152 | 1-a | A-a-151 | 4CF3BnO | H | H | 5-1Idz | C | 467(M++1) | ||
A-a-153 | 4f-2 | Int.A-22 | Al5 | 2EtBuO | Et | H | 2-Nap | C | 431(M++1) | |
A-a-154 | 1-a | A-a-153 | 2EtBuO | H | H | 2-Nap | C | 403(M++1) | ||
A-a-155 | 4f-2 | Int.A-23 | Al5 | 2EtBuO | Et | H | 5-Ind | C | 420(M++1) | |
A-a-156 | 1-a | A-a-155 | 2EtBuO | H | H | 5-Ind | C | 392(M++1) | ||
A-a-157 | 4f-2 | Int.A-26 | Al5 | 2EtBuO | Et | H | 1Me-5-Idz | C | 435(M++1) | |
A-a-158 | 1-a | A-a-157 | 2EtBuO | H | H | 1Me-5-Idz | C | 407(M++1) | ||
A-a-159 | 4f-2 | Int.A-23 | Al6 | 2(4DMAPh)EtO | Et | H | 5-Ind | C | 483(M++1) | |
A-a-160 | 1-a | A-a-159 | 2(4DMAPh)EtO | H | H | 5-Ind | C | 455(M++1) | ||
A-a-161 | 4f-2 | Int.A-24 | Al6 | 2(4DMAPh)EtO | Et | H | 1Me-5-Ind | C | 497(M++1) | |
A-a-162 | 1-a | A-a-161 | 2(4DMAPh)EtO | H | H | 1Me-5-Ind | C | 469(M++1) | ||
A-a-163 | 4f-2 | Int.A-27 | Al6 | 2(4DMAPh)EtO | Et | H | 1Et-5-Idz | C | 512(M++1) | |
A-a-164 | 1-a | A-a-163 | 2(4DMAPh)EtO | H | H | 1Et-5-Idz | C | 484(M++1) | ||
A-a-165 | 4f-2 | Int.A-22 | Al7 | 2(PhO)EtO | Et | H | 2-Nap | C | 467(M++1) | |
A-a-166 | 1-a | A-a-165 | 2(PhO)EtO | H | H | 2-Nap | C | 439(M++1) | ||
A-a-167 | 4f-2 | Int.A-24 | Al7 | 2(PhO)EtO | Et | H | 1Me-5-Ind | C | 470(M++1) | |
A-a-168 | 1-a | A-a-167 | 2(PhO)EtO | H | H | 1Me-5-Ind | C | 442(M++1) | ||
A-a-169 | 4f-2 | Int.A-29 | Al7 | 2(PhO)EtO | Et | H | 6-Qu | C | 468(M++1) | |
A-a-170 | 1-a | A-a-169 | 2(PhO)EtO | H | H | 6-Qu | C | 440(M++1) | ||
A-a-171 | 4f-2 | Int.A-22 | Al8 | 1PhEtO | Et | H | 2-Nap | C | 451(M++1) | |
A-a-172 | 1-a | A-a-171 | 1PhEtO | H | H | 2-Nap | C | 423(M++1) | ||
A-a-173 | 4f-2 | Int.A-24 | Al8 | 1PhEtO | Et | H | 1Me-5-Ind | C | 454(M++1) | |
A-a-174 | 1-a | A-a-173 | 1PhEtO | H | H | 1Me-5-Ind | C | 426(M++1) | ||
A-a-175 | 4f-2 | Int.A-25 | Al8 | 1PhEtO | Et | H | 5-1Idz | C | 441(M++1) | |
A-a-176 | 1-a | A-a-175 | 1PhEtO | H | H | 5-1Idz | C | 413(M++1) | ||
A-a-177 | 4f-2 | Int.A-23 | Al9 | 1(2FPh)EtO | Et | H | 5-Ind | C | 458(M++1) | |
A-a-178 | 1-a | A-a-177 | 1(2FPh)EtO | H | H | 5-Ind | C | 430(M++1) | ||
A-a-179 | 4f-2 | Int.A-27 | Al9 | 1(2FPh)EtO | Et | H | 1Et-5-Idz | C | 487(M++1) | |
A-a-180 | 1-a | A-a-179 | 1(2FPh)EtO | H | H | 1Et-5-Idz | C | 459(M++1) | ||
A-a-181 | 4f-2 | Int.A-29 | Al9 | 1(2FPh)EtO | Et | H | 6-Qu | C | 470(M++1) | |
A-a-182 | 1-a | A-a-181 | 1(2FPh)EtO | H | H | 6-Qu | C | 442(M++1) | ||
A-a-183 | 4f-2 | Int.A-23 | Al10 | 1(4ClPh)EtO | Et | H | 5-Ind | C | 475(M++1) | |
A-a-184 | 1-a | A-a-183 | 1(4ClPh)EtO | H | H | 5-Ind | C | 446(M++1) | ||
A-a-185 | 4f-2 | Int.A-24 | Al10 | 1(4ClPh)EtO | Et | H | 1Me-5-Ind | C | 489(M++1) | |
A-a-186 | 1-a | A-a-185 | 1(4ClPh)EtO | H | H | 1Me-5-Ind | C | 460(M++1) | ||
A-a-187 | 4f-2 | Int.A-27 | Al10 | 1(4ClPh)EtO | Et | H | 1Et-5-Idz | C | 504(M++1) | |
A-a-188 | 1-a | A-a-187 | 1(4ClPh)EtO | H | H | 1Et-5-Idz | C | 476(M++1) | ||
A-a-189 | 4f-2 | Int.A-22 | Al11 | 4Me,cHexO | Et | H | 2-Nap | C | 443(M++1) | |
A-a-190 | 1-a | A-a-189 | 4Me,cHexO | H | H | 2-Nap | C | 415(M++1) |
Table-A-a-5 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-191 | 4f-2 | Int.A-24 | Al11 | 4Me,cHexO | Et | H | 1Me-5-Ind | C | 446(M++1) | |
A-a-192 | 1-a | A-a-191 | 4Me,cHexO | H | H | 1Me-5-Ind | C | 418(M++1) | ||
A-a-193 | 4f-2 | Int.A-23 | Al12 |
|
Et | H | 5-Ind | C | 454(M++1) | |
A-a-194 | 1-a | A-a-193 |
|
H | H | 5-Ind | C | 426(M++1) | ||
A-a-195 | 4f-2 | Int.A-26 | Al12 |
|
Et | H | 1Me-5-Idz | C | 469(M++1) | |
A-a-196 | 1-a | A-a-195 |
|
H | H | 1Me-5-Idz | C | 441(M++1) | ||
A-a-197 | 4f-2 | Int.A-22 | Al13 |
|
Et | H | 2-Nap | C | 465(M++1) | |
A-a-198 | 1-a | A-a-197 |
|
H | H | 2-Nap | C | 437(M++1) | ||
A-a-199 | 4f-2 | Int.A-27 | Al13 |
|
Et | H | 1Et-5-Idz | C | 483(M++1) | |
A-a-200 | 1-a | A-a-199 |
|
H | H | 1Et-5-Idz | C | 455(M++1) | ||
A-a-201 | 4f-2 | Int.A-23 | Al14 |
|
Et | H | 5-Ind | C | 472(M++1) | |
A-a-202 | 1-a | A-a-201 |
|
H | H | 5-Ind | C | 444(M++1) | ||
A-a-203 | 4f-2 | Int.A-24 | Al14 |
|
Et | H | 1Me-5-Ind | C | 486(M++1) | |
A-a-204 | 1-a | A-a-203 |
|
H | H | 1Me-5-Ind | C | 458(M++1) | ||
A-a-205 | 4f-2 | Int.A-23 | Al15 |
|
Et | H | 5-Ind | C | 522(M++1) | |
A-a-206 | 1-a | A-a-205 |
|
H | H | 5-Ind | C | 494(M++1) | ||
A-a-207 | 4f-2 | Int.A-24 | Al15 |
|
Et | H | 1Me-5-Ind | C | 536(M++1) | |
A-a-208 | 1-a | A-a-207 |
|
H | H | 1Me-5-Ind | C | 508(M++1) | ||
A-a-209 | 41-2 | Int.A-24 | Al16 |
|
Et | H | 1Me-5-Ind | C | 482(M++1) | |
A-a-210 | 1-a | A-a-209 |
|
H | H | 1Me-5-Ind | C | 454(M++1) | ||
A-a-211 | 4f-2 | Int.A-26 | Al16 |
|
Et | H | 1Me-5-Idz | C | 483(M++1) | |
A-a-212 | 1-a | A-a-211 |
|
H | H | 1Me-5-Idz | C | 455(M++1) | ||
A-a-213 | 4f-2 | Int.A-22 | Al17 | 1IndanO | Et | H | 2-Nap | C | 463(M++1) | |
A-a-214 | 1-a | A-a-213 | 1IndanO | H | H | 2-Nap | C | 435(M++1) | ||
A-a-215 | 4f-2 | Int.A-24 | Al17 | 1IndanO | Et | H | 1Me-5-Ind | C | 466(M++1) | |
A-a-216 | 1-a | A-a-215 | 1IndanO | H | H | 1Me-5-Ind | C | 438(M++1) | ||
A-a-217 | 4f-2 | Int.A-25 | Al17 | 1IndanO | Et | H | 5-1Idz | C | 453(M++1) | |
A-a-218 | 1-a | A-a-217 | 1IndanO | H | H | 5-1Idz | C | 425(M++1) |
Table-A-a-6 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-219 | 4f-2 | Int.A-22 | Al18 | 2IndanO | Et | H | 2-Nap | C | 463(M++1) | |
A-a-220 | 1-a | A-a-219 | 2IndanO | H | H | 2-Nap | C | 435(M++1) | ||
A-a-221 | 4f-2 | Int.A-23 | Al18 | 2IndanO | Et | H | 5-Ind | C | 452(M++1) | |
A-a-222 | 1-a | A-a-221 | 2IndanO | H | H | 5-Ind | C | 424(M++1) | ||
A-a-223 | 4f-2 | Int.A-26 | Al18 | 2IndanO | Et | H | 1Me-5-Idz | C | 467(M++1) | |
A-a-224 | 1-a | A-a-223 | 2IndanO | H | H | 1Me-5-Idz | C | 439(M++1) | ||
A-a-225 | 4f-2 | Int.A-24 | Al19 | 5OMe-2-IndanO | Et | H | 1Me-5-Ind | C | 496(M++1) | |
A-a-226 | 1-a | A-a-225 | 5OMe-2-IndanO | H | H | 1Me-5-Ind | C | 468(M++1) | ||
A-a-227 | 4f-2 | Int.A-25 | Al19 | 5OMe-2-IndanO | Et | H | 5-1Idz | C | 483(M++1) | |
A-a-228 | 1-a | A-a-227 | 5OMe-2-IndanO | H | H | 5-1Idz | C | 455(M++1) | ||
A-a-229 | 4f-2 | Int.A-27 | Al19 | 5OMe-2-IndanO | Et | H | 1Et-5-Idz | C | 511(M++1) | |
A-a-230 | 1-a | A-a-229 | 5OMe-2-IndanO | H | H | 1Et-5-Idz | C | 483(M++1) | ||
A-a-231 | 4f-2 | Int.A-22 | Al20 | 5,6D(OMe)-2-IndanO | Et | H | 2-Nap | C | 523(M++1) | |
A-a-232 | 1-a | A-a-231 | 5,6D(OMe)-2-IndanO | H | H | 2-Nap | C | 495(M++1) | ||
A-a-233 | 4f-2 | Int.A-23 | Al20 | 5,6D(OMe)-2-IndanO | Et | H | 5-Ind | C | 512(M++1) | |
A-a-234 | 1-a | A-a-233 | 5,6D(OMe)-2-IndanO | H | H | 5-Ind | C | 484(M++1) | ||
A-a-235 | 4f-2 | Int.A-22 | Al21 | 5F-2-IndanO | Et | H | 2-Nap | C | 481(M++1) | |
A-a-236 | 1-a | A-a-235 | 5F-2-IndanO | H | H | 2-Nap | C | 453(M++1) | ||
A-a-237 | 4f-2 | Int.A-24 | Al21 | 5F-2-IndanO | Et | H | 1Me-5-Ind | C | 484(M++1) | |
A-a-238 | 1-a | A-a-237 | 5F-2-IndanO | H | H | 1Me-5-Ind | C | 456(M++1) | ||
A-a-239 | 4f-2 | Int.A-26 | Al21 | 5F-2-IndanO | Et | H | 1Me-5-Idz | C | 485(M++1) | |
A-a-240 | 1-a | A-a-239 | 5F-2-IndanO | H | H | 1Me-5-Idz | C | 457(M++1) | ||
A-a-241 | 4f-2 | Int.A-27 | Al21 | 5F-2-IndanO | Et | H | 1Et-5-Idz | C | 499(M++1) | |
A-a-242 | 1-a | A-a-241 | 5F-2-IndanO | H | H | 1Et-5-Idz | C | 471(M++1) | ||
A-a-243 | 4f-2 | Int.A-23 | Al22 |
|
Et | H | 5-Ind | C | 466(M++1) | |
A-a-244 | 1-a | A-a-243 |
|
H | H | 5-Ind | C | 438(M++1) | ||
A-a-245 | 4f-2 | Int.A-24 | Al22 |
|
Et | H | 1Me-5-Ind | C | 480(M++1) | |
A-a-246 | 1-a | A-a-245 |
|
H | H | 1Me-5-Ind | C | 452(M++1) | ||
A-a-247 | 4f-2 | Int.A-22 | Al23 |
|
Et | H | 2-Nap | C | 477(M++1) | |
A-a-248 | 1-a | A-a-247 |
|
H | H | 2-Nap | C | 449(M++1) | ||
A-a-249 | 4f-2 | Int.A-25 | Al23 |
|
Et | H | 5-1Idz | C | 467(M++1) | |
A-a-250 | 1-a | A-a-249 |
|
H | H | 5-1Idz | C | 439(M++1) | ||
A-a-251 | 4f-2 | Int.A-24 | Al24 | 2(2MePh)EtO | Et | H | 1Me-5-Ind | C | 468(M++1) | |
A-a-252 | 1-a | A-a-251 | 2(2MePh)EtO | H | H | 1Me-5-Ind | C | 440(M++1) | ||
A-a-253 | 4f-2 | Int.A-29 | Al24 | 2(2MePh)EtO | Et | H | 6-Qu | C | 466(M++1) | |
A-a-254 | 1-a | A-a-253 | 2(2MePh)EtO | H | H | 6-Qu | C | 438(M++1) |
Table-A-a-7 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-255 | 4f-2 | Int.A-22 | Al25 | 2(3FPh)EtO | Et | H | 2-Nap | C | 469(M++1) | |
A-a-256 | 1-a | A-a-255 | 2(3FPh)EtO | H | H | 2-Nap | C | 441(M++1) | ||
A-a-257 | 4f-2 | Int.A-23 | Al25 | 2(3FPh)EtO | Et | H | 5-Ind | C | 458(M++1) | |
A-a-258 | 1-a | A-a-257 | 2(3FPh)EtO | H | H | 5-Ind | C | 430(M++1) | ||
A-a-259 | 4f-2 | Int.A-26 | Al26 | 2(2ClPh)EtO | Et | H | 1 Me-5-Idz | C | 490(M++1) | |
A-a-260 | 1-a | A-a-259 | 2(2ClPh)EtO | H | H | 1Me-5-Idz | C | 461(M++1) | ||
A-a-261 | 4f-2 | Int.A-29 | Al26 | 2(2ClPh)EtO | Et | H | 6-Qu | C | 487(M++1) | |
A-a-262 | 1-a | A-a-261 | 2(2ClPh)EtO | H | H | 6-Qu | C | 458(M++1) | ||
A-a-263 | 4f-2 | Int.A-22 | Al28 | 2(1-Nap)EtO | Et | H | 2-Nap | C | 501(M++1) | |
A-a-264 | 1-a | A-a-263 | 2(1-Nap)EtO | H | H | 2-Nap | C | 473(M++1) | ||
A-a-265 | 4f-2 | Int.A-23 | Al28 | 2(1-Nap)EtO | Et | H | 5-Ind | C | 490(M++1) | |
A-a-266 | 1-a | A-a-265 | 2(1-Nap)EtO | H | H | 5-Ind | C | 462(M++1) | ||
A-a-267 | 4f-2 | Int.A-24 | Al27 | 2(2-Nap)EtO | Et | H | 1Me-5-Ind | C | 504(M++1) | |
A-a-268 | 1-a | A-a-267 | 2(2-Nap)EtO | H | H | 1Me-5-Ind | C | 476(M++1) | ||
A-a-269 | 4f-2 | Int.A-25 | Al27 | 2(2-Nap)EtO | Et | H | 5-1Idz | C | 491(M++1) | |
A-a-270 | 1-a | A-a-269 | 2(2-Nap)EtO | H | H | 5-1Idz | C | 463(M++1) | ||
A-a-271 | 4f-2 | Int.A-22 | Al29 |
|
Et | H | 2-Nap | C | 495(M++1) | |
A-a-272 | 1-a | A-a-271 |
|
H | H | 2-Nap | C | 467(M++1) | ||
A-a-273 | 4f-2 | Int.A-23 | Al29 |
|
Et | H | 5-Ind | C | 484(M++1) | |
A-a-274 | 1-a | A-a-273 |
|
H | H | 5-Ind | C | 456(M++1) | ||
A-a-275 | 4f-2 | Int.A-22 | Al30 | 2(PhS)EtO | Et | H | 2-Nap | C | 483(M++1) | |
A-a-276 | 1-a | A-a-275 | 2(PhS)EtO | H | H | 2-Nap | C | 454(M++1) | ||
A-a-277 | 4f-2 | Int.A-23 | Al30 | 2(PhS)EtO | Et | H | 5-Ind | C | 472(M++1) | |
A-a-278 | 1-a | A-a-277 | 2(PhS)EtO | H | H | 5-Ind | C | 444(M++1) | ||
A-a-279 | 4f-2 | Int.A-24 | Al31 |
|
Et | H | 1Me-5-Ind | C | 444(M++1) | |
A-a-280 | 1-a | A-a-279 |
|
H | H | 1Me-5-Ind | C | 416(M++1) | ||
A-a-281 | 4f-2 | Int.A-27 | Al32 |
|
Et | H | 1Et-5-Idz | C | 458(M++1) | |
A-a-282 | 1-a | A-a-281 |
|
H | H | 1Et-5-Idz | C | 430(M++1) |
Table-A-a-8 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-a-283 | 4f-2 | Int.A-22 | Al33 |
|
Et | H | 2-Nap | C | 438(M++1) | |
A-a-284 | 1-a | A-a-283 |
|
H | H | 2-Nap | C | 410(M++1) | ||
A-a-285 | 4f-2 | Int.A-23 | Al34 |
|
Et | H | 5-Ind | C | 441(M++1) | |
A-a-286 | 1-a | A-a-285 |
|
H | H | 5-Ind | C | 413(M++1) | ||
A-a-287 | 4f-2 | Int.A-23 | Al35 |
|
Et | H | 5-Ind | C | 477(M++1) | |
A-a-288 | 1-a | A-a-287 |
|
H | H | 5-Ind | C | 449(M++1) | ||
A-a-289 | 4f-2 | Int.A-26 | Al36 |
|
Et | H | 1Me-5-Idz | C | 456(M++1) | |
A-a-290 | 1-a | A-a-289 |
|
H | H | 1Me-5-Idz | C | 428(M++1) | ||
A-a-291 | 4e-1 | Int.A-4 | BRA5 | cPen | Et | H | 1Me-4-Ind | C | 402(M++1) | |
A-a-292 | 1-a | A-a-291 | cPen | H | H | 1Me-4-Ind | C | 374(M++1) | ||
A-a-293 | 4e-1 | Int.A-4 | BRA6 | cPen | Et | H | 1Me-6-Ind | C | 402(M++1) | |
A-a-294 | 1-a | A-a-293 | cPen | H | H | 1Me-6-Ind | C | 374(M++1) |
Reference Example 4
Synthesis of ethyl 2-[4-chloro-5-hydroxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Intermediate A-30) (Preparation Method 4, Step h-1)
Reference Example 5
Synthesis of ethyl 2-[4-bromo-5-hydroxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Intermediate A-34) (Preparation Method 4, Step h-2)
Table-Int.A-3 | |||||||||
|
Exp. | Syn. | SM | Reagent | Rx | V1' | V2' | LCMS | ||
method | RTime | Mass | |||||||
Int.A-31 | 4h-1 | A-a-24 | HO | Cl | 1Me-5-Ind | C | 384(M++1) | ||
Int.A-32 | 4h-1 | A-a-26 | HO | Cl | 1Me-5-Idz | C | 385(M++1) | ||
Int.A-33 | 4h-1 | A-a-27 | HO | Cl | 1Et-5-Idz | C | 399(M++1) | ||
Int.A-35 | 4h-2 | A-a-24 | HO | Br | 1Me-5-Ind | C | 427(M+) | ||
Int.A-36 | 4h-2 | A-a-26 | HO | Br | 1Me-5-Idz | C | 428(M+) | ||
Int.A-37 | 4h-2 | A-a-27 | HO | Br | 1Et-5-Idz | C | 442(M+) |
Example A-b-1
Synthesis of ethyl 2-[4-chloro-5-cyclopentyloxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-b-1) (Preparation Method 4, Step f-2)
Example A-b-2
Synthesis of 2-[4-chloro-5-cyclopentyloxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-b-2) (Preparation Method 1, Step a)
Example A-b-243
Synthesis of ethyl 2-[4-bromo-5-cyclopentyloxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-b-243) (Preparation Method 4, Step f-2)
Example A-b-244
Synthesis of 2-[4-bromo-5-cyclopentyloxy-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-b-244) (Preparation Method 1, Step a)
Example A-b-445
Synthesis of ethyl 2-[5-cyclopentyloxy-4-methyl-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetate (Compound No. A-b-445) (Preparation Method 4, Step e-1)
Example A-b-446
Synthesis of 2-[5-cyclopentyloxy-4-methyl-6-(naphthalen-2-yl)-2,3-dihydro-1H-inden-1-yl]acetic acid (Compound No. A-b-446) (Preparation Method 1, Step a)
Table-A-b-1 | ||||||||||
|
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-b-1 | 4f-2 | Int.A-30 | Al1 | cPenO | Et | Cl | 2-Nap | C | 449(M++1) | |
A-b-2 | 1-a | A-b-1 | cPenO | H | Cl | 2-Nap | C | 421(M++1) | ||
A-b-3 | 4f-2 | Int.A-30 | Al2 | cPenMeO | Et | Cl | 2-Nap | C | 463(M++1) | |
A-b-4 | 1-a | A-b-3 | cPenMeO | H | Cl | 2-Nap | C | 431(M++1) | ||
A-b-5 | 4f-1 | Int.A-30 | Hal2 | cHexMeO | Et | Cl | 2-Nap | C | 477(M++1) | |
A-b-6 | 1-a | A-b-5 | cHexMeO | H | Cl | 2-Nap | C | 449(M++1) | ||
A-b-7 | 4f-2 | Int.A-30 | Al3 | cHexO | Et | Cl | 2-Nap | C | 463(M++1) | |
A-b-8 | 1-a | A-b-7 | cHexO | H | Cl | 2-Nap | C | 435(M++1) | ||
A-b-9 | 4f-2 | Int.A-30 | Al4 | cHepO | Et | Cl | 2-Nap | C | 477(M++1) | |
A-b-10 | 1-a | A-b-9 | cHepO | H | Cl | 2-Nap | C | 449(M++1) | ||
A-b-11 | 4f-1 | Int.A-30 | Hal3 | nPrO | Et | Cl | 2-Nap | C | 422(M++1) | |
A-b-12 | 1-a | A-b-11 | nPrO | H | Cl | 2-Nap | C | 394(M++1) | ||
A-b-13 | 4f-1 | Int.A-30 | Hal4 | iPrO | Et | Cl | 2-Nap | C | 422(M++1) | |
A-b-14 | 1-a | A-b-13 | iPrO | H | Cl | 2-Nap | C | 394(M++1) | ||
A-b-15 | 4f-1 | Int.A-30 | Hal5 | nBuO | Et | Cl | 2-Nap | C | 437(M++1) | |
A-b-16 | 1-a | A-b-15 | nBuO | H | Cl | 2-Nap | C | 409(M++1) | ||
A-b-17 | 4f-1 | Int.A-30 | Hal6 | iBuO | Et | Cl | 2-Nap | C | 437(M++1) | |
A-b-18 | 1-a | A-b-17 | iBuO | H | Cl | 2-Nap | C | 409(M++1) | ||
A-b-19 | 4f-1 | Int.A-30 | Hal1 | BnO | Et | Cl | 2-Nap | C | 471(M++1) | |
A-b-20 | 1-a | A-b-19 | BnO | H | Cl | 2-Nap | C | 443(M++1) | ||
A-b-21 | 4f-1 | Int.A-30 | Hal7 | 2FBnO | Et | Cl | 2-Nap | C | 489(M++1) | |
A-b-22 | 1-a | A-b-21 | 2FBnO | H | Cl | 2-Nap | C | 461(M++1) | ||
A-b-23 | 4f-1 | Int.A-30 | Hal8 | 3FBnO | Et | Cl | 2-Nap | C | 489(M++1) | |
A-b-24 | 1-a | A-b-23 | 3FBnO | H | Cl | 2-Nap | C | 461(M++1) | ||
A-b-25 | 4f-1 | Int.A-30 | Hal9 | 4FBnO | Et | Cl | 2-Nap | C | 489(M++1) | |
A-b-26 | 1-a | A-b-25 | 4FBnO | H | Cl | 2-Nap | C | 461(M++1) | ||
A-b-27 | 4f-1 | Int.A-30 | Hal10 | 2ClBnO | Et | Cl | 2-Nap | C | 505(M++1) | |
A-b-28 | 1-a | A-b-27 | 2ClBnO | H | Cl | 2-Nap | C | 487(M++1) | ||
A-b-29 | 4f-1 | Int.A-30 | Hal11 | 3ClBnO | Et | Cl | 2-Nap | C | 505(M++1) | |
A-b-30 | 1-a | A-b-29 | 3ClBnO | H | Cl | 2-Nap | C | 487(M++1) | ||
A-b-31 | 4f-1 | Int.A-30 | Hal12 | 4MeBnO | Et | Cl | 2-Nap | C | 485(M++1) | |
A-b-32 | 1-a | A-b-31 | 4MeBnO | H | Cl | 2-Nap | C | 457(M++1) | ||
A-b-33 | 4f-1 | Int.A-30 | Hal13 | 4CF3BnO | Et | Cl | 2-Nap | C | 538(M++1) | |
A-b-34 | 1-a | A-b-33 | 4CF3BnO | H | Cl | 2-Nap | C | 510(M++1) | ||
A-b-35 | 4f-2 | Int.A-30 | Al5 | 2EtBuO | Et | Cl | 2-Nap | C | 465(M++1) | |
A-b-36 | 1-a | A-b-35 | 2EtBuO | H | Cl | 2-Nap | C | 437(M++1) | ||
A-b-37 | 4f-2 | Int.A-30 | Al6 | 2(4DMAPh)EtO | Et | Cl | 2-Nap | C | 528(M++1) | |
A-b-38 | 1-a | A-b-37 | 2(4DMAPh)EtO | H | Cl | 2-Nap | C | 500(M++1) | ||
A-b-39 | 4f-2 | Int.A-30 | Al7 | 2(PhO)EtO | Et | Cl | 2-Nap | C | 501(M++1) | |
A-b-40 | 1-a | A-b-39 | 2(PhO)EtO | H | Cl | 2-Nap | C | 473(M++1) | ||
A-b-41 | 4f-2 | Int.A-30 | Al8 | 1PhEtO | Et | Cl | 2-Nap | C | 485(M++1) | |
A-b-42 | 1-a | A-b-41 | 1PhEtO | H | Cl | 2-Nap | C | 457(M++1) | ||
A-b-43 | 4f-2 | Int.A-30 | Al11 | 4Me,cHexO | Et | Cl | 2-Nap | C | 477(M++1) | |
A-b-44 | 1-a | A-b-43 | 4Me,cHexO | H | Cl | 2-Nap | C | 449(M++1) |
Table-A-b-2 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-b-45 | 4f-2 | Int.A-30 | Al17 | 1IndanO | Et | Cl | 2-Nap | C | 497(M++1) | |
A-b-46 | 1-a | A-b-45 | 1IndanO | H | Cl | 2-Nap | C | 469(M++1) | ||
A-b-47 | 4f-2 | Int.A-30 | Al18 | 2IndanO | Et | Cl | 2-Nap | C | 497(M++1) | |
A-b-48 | 1-a | A-b-47 | 2IndanO | H | Cl | 2-Nap | C | 469(M++1) | ||
A-b-49 | 4f-2 | Int.A-30 | Al19 | 5OMe-2-IndanO | Et | Cl | 2-Nap | C | 527(M++1) | |
A-b-50 | 1-a | A-b-49 | 5OMe-2-IndanO | H | Cl | 2-Nap | C | 499(M++1) | ||
A-b-51 | 4f-2 | Int.A-30 | Al20 | 5,6D(OMe)-2-IndanO | Et | Cl | 2-Nap | C | 557(M++1) | |
A-b-52 | 1-a | A-b-51 | 5,6D(OMe)-2-IndanO | H | Cl | 2-Nap | C | 529(M++1) | ||
A-b-53 | 4f-2 | Int.A-30 | Al21 | 5F-2-IndanO | Et | Cl | 2-Nap | C | 515(M++1) | |
A-b-54 | 1-a | A-b-53 | 5F-2-IndanO | H | Cl | 2-Nap | C | 487(M++1) | ||
A-b-55 | 4f-2 | Int.A-30 | Al22 |
|
Et | Cl | 2-Nap | C | 511(M++1) | |
A-b-56 | 1-a | A-b-55 |
|
H | Cl | 2-Nap | C | 483(M++1) | ||
A-b-57 | 4f-2 | Int.A-30 | Al23 |
|
Et | Cl | 2-Nap | C | 511(M++1) | |
A-b-58 | 1-a | A-b-57 |
|
H | Cl | 2-Nap | C | 483(M++1) | ||
A-b-59 | 4f-2 | Int.A-30 | Al25 | 2(3FPh)EtO | Et | Cl | 2-Nap | C | 503(M++1) | |
A-b-60 | 1-a | A-b-59 | 2(3FPh)EtO | H | Cl | 2-Nap | C | 475(M++1) | ||
A-b-61 | 4f-2 | Int.A-30 | Al27 | 2(2-Nap)EtO | Et | Cl | 2-Nap | C | 535(M++1) | |
A-b-62 | 1-a | A-b-61 | 2(2-Nap)EtO | H | Cl | 2-Nap | C | 507(M++1) | ||
A-b-63 | 4f-2 | Int.A-31 | Al1 | cPenO | Et | Cl | 1Me-5-Ind | C | 452(M++1) | |
A-b-64 | 1-a | A-b-63 | cPenO | H | Cl | 1Me-5-Ind | C | 424(M++1) | ||
A-b-65 | 4f-2 | Int.A-31 | Al2 | cPenMeO | Et | Cl | 1Me-5-Ind | C | 466(M++1) | |
A-b-66 | 1-a | A-b-65 | cPenMeO | H | Cl | 1Me-5-Ind | C | 438(M++1) | ||
A-b-67 | 4f-1 | Int.A-31 | Hal2 | cHexMeO | Et | Cl | 1Me-5-Ind | C | 480(M++1) | |
A-b-68 | 1-a | A-b-67 | cHexMeO | H | Cl | 1Me-5-Ind | C | 452(M++1) | ||
A-b-69 | 4f-2 | Int.A-31 | Al3 | cHexO | Et | Cl | 1Me-5-Ind | C | 466(M++1) | |
A-b-70 | 1-a | A-b-69 | cHexO | H | Cl | 1Me-5-Ind | C | 438(M++1) | ||
A-b-71 | 4f-2 | Int.A-31 | Al4 | cHepO | Et | Cl | 1Me-5-Ind | C | 480(M++1) | |
A-b-72 | 1-a | A-b-71 | cHepO | H | Cl | 1Me-5-Ind | C | 452(M++1) | ||
A-b-73 | 4f-1 | Int.A-31 | Hal3 | nPrO | Et | Cl | 1Me-5-Ind | C | 425(M++1) | |
A-b-74 | 1-a | A-b-73 | nPrO | H | Cl | 1Me-5-Ind | C | 397(M++1) | ||
A-b-75 | 4f-1 | Int.A-31 | Hal4 | iPrO | Et | Cl | 1Me-5-Ind | C | 425(M++1) | |
A-b-76 | 1-a | A-b-75 | iPrO | H | Cl | 1Me-5-Ind | C | 397(M++1) | ||
A-b-77 | 4f-1 | Int.A-31 | Hal5 | nBuO | Et | Cl | 1Me-5-Ind | C | 440(M++1) | |
A-b-78 | 1-a | A-b-77 | nBuO | H | Cl | 1Me-5-Ind | C | 412(M++1) | ||
A-b-79 | 4f-1 | Int.A-31 | Hal6 | iBuO | Et | Cl | 1Me-5-Ind | C | 440(M++1) | |
A-b-80 | 1-a | A-b-79 | iBuO | H | Cl | 1Me-5-Ind | C | 412(M++1) | ||
A-b-81 | 4f-1 | Int.A-31 | Hal1 | BnO | Et | Cl | 1Me-5-Ind | C | 474(M++1) | |
A-b-82 | 1-a | A-b-81 | BnO | H | Cl | 1Me-5-Ind | C | 446(M++1) | ||
A-b-83 | 4f-1 | Int.A-31 | Hal7 | 2FBnO | Et | Cl | 1Me-5-Ind | C | 492(M++1) | |
A-b-84 | 1-a | A-b-83 | 2FBnO | H | Cl | 1Me-5-Ind | C | 464(M++1) | ||
A-b-85 | 4f-1 | Int.A-31 | Hal9 | 4FBnO | Et | Cl | 1Me-5-Ind | C | 492(M++1) | |
A-b-86 | 1-a | A-b-85 | 4FBnO | H | Cl | 1Me-5-Ind | C | 464(M++1) | ||
A-b-87 | 4f-1 | Int.A-31 | Hal11 | 3ClBnO | Et | Cl | 1Me-5-Ind | C | 508(M++1) | |
A-b-88 | 1-a | A-b-87 | 3ClBnO | H | Cl | 1Me-5-Ind | C | 480(M++1) |
Table-A-b-3 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-b-89 | 4f-1 | Int.A-31 | Hal12 | 4MeBnO | Et | Cl | 1Me-5-Ind | C | 488(M++1) | |
A-b-90 | 1-a | A-b-89 | 4MeBnO | H | Cl | 1Me-5-Ind | C | 460(M++1) | ||
A-b-91 | 4f-1 | Int.A-31 | Hal13 | 4CF3BnO | Et | Cl | 1Me-5-Ind | C | 541(M++1) | |
A-b-92 | 1-a | A-b-91 | 4CF3BnO | H | Cl | 1Me-5-Ind | C | 513(M++1) | ||
A-b-93 | 4f-2 | Int.A-31 | Al5 | 2EtBuO | Et | Cl | 1Me-5-Ind | C | 468(M++1) | |
A-b-94 | 1-a | A-b-93 | 2EtBuO | H | Cl | 1Me-5-Ind | C | 440(M++1) | ||
A-b-95 | 4f-2 | Int.A-31 | Al6 | 2(4DMAPh)EtO | Et | Cl | 1Me-5-Ind | C | 531(M++1) | |
A-b-96 | 1-a | A-b-95 | 2(4DMAPh)EtO | H | Cl | 1Me-5-Ind | C | 503(M++1) | ||
A-b-97 | 4f-2 | Int.A-31 | Al8 | 1PhEtO | Et | Cl | 1Me-5-Ind | C | 488(M++1) | |
A-b-98 | 1-a | A-b-97 | 1PhEtO | H | Cl | 1Me-5-Ind | C | 460(M++1) | ||
A-b-99 | 4f-2 | Int.A-31 | Al11 | 4Me,cHexO | Et | Cl | 1Me-5-Ind | C | 480(M++1) | |
A-b-100 | 1-a | A-b-99 | 4Me,cHexO | H | Cl | 1Me-5-Ind | C | 452(M++1) | ||
A-b-101 | 4f-2 | Int.A-31 | Al17 | 1IndanO | Et | Cl | 1Me-5-Ind | C | 500(M++1) | |
A-b-102 | 1-a | A-b-101 | 1IndanO | H | Cl | 1Me-5-Ind | C | 472(M++1) | ||
A-b-103 | 4f-2 | Int.A-31 | Al18 | 2IndanO | Et | Cl | 1Me-5-Ind | C | 500(M++1) | |
A-b-104 | 1-a | A-b-103 | 2IndanO | H | Cl | 1Me-5-Ind | C | 472(M++1) | ||
A-b-105 | 4f-2 | Int.A-31 | Al19 | 5OMe-2-IndanO | Et | Cl | 1Me-5-Ind | C | 530(M++1) | |
A-b-106 | 1-a | A-b-105 | 5OMe-2-IndanO | H | Cl | 1Me-5-Ind | C | 502(M++1) | ||
A-b-107 | 4f-2 | Int.A-31 | Al20 | 5,6D(OMe)-2-IndanO | Et | Cl | 1Me-5-Ind | C | 560(M++1) | |
A-b-108 | 1-a | A-b-107 | 5,6D(OMe)-2-IndanO | H | Cl | 1Me-5-Ind | C | 532(M++1) | ||
A-b-109 | 4f-2 | Int.A-31 | Al21 | 5F-2-IndanO | Et | Cl | 1Me-5-Ind | C | 518(M++1) | |
A-b-110 | 1-a | A-b-109 | 5F-2-IndanO | H | Cl | 1Me-5-Ind | C | 490(M++1) | ||
A-b-111 | 4f-2 | Int.A-31 | Al22 |
|
Et | Cl | 1Me-5-Ind | C | 514(M++1) | |
A-b-112 | 1-a | A-b-111 |
|
H | Cl | 1Me-5-Ind | C | 486(M++1) | ||
A-b-113 | 4f-2 | Int.A-31 | Al23 |
|
Et | Cl | 1Me-5-Ind | C | 514(M++1) | |
A-b-114 | 1-a | A-b-113 |
|
H | Cl | 1Me-5-Ind | C | 486(M++1) | ||
A-b-115 | 4f-2 | Int.A-31 | A25 | 2(3FPh)EtO | Et | Cl | 1Me-5-Ind | C | 506(M++1) | |
A-b-116 | 1-a | A-b-115 | 2(3FPh)EtO | H | Cl | 1Me-5-Ind | C | 478(M++1) | ||
A-b-117 | 4f-2 | Int.A-31 | Al27 | 2(2-Nap)EtO | Et | Cl | 1Me-5-Ind | C | 538(M++1) | |
A-b-118 | 1-a | A-b-117 | 2(2-Nap)EtO | H | Cl | 1Me-5-Ind | C | 510(M++1) | ||
A-b-119 | 4f-2 | Int.A-32 | Al1 | cPenO | Et | Cl | 1Me-5-Idz | C | 453(M++1) | |
A-b-120 | 1-a | A-b-119 | cPenO | H | Cl | 1Me-5-Idz | C | 425(M++1) | ||
A-b-121 | 4f-2 | Int.A-32 | Al2 | cPenMeO | Et | Cl | 1Me-5-Idz | C | 467(M++1) | |
A-b-122 | 1-a | A-b-121 | cPenMeO | H | Cl | 1Me-5-Idz | C | 439(M++1) | ||
A-b-123 | 4f-1 | Int.A-32 | Hal2 | cHexMeO | Et | Cl | 1Me-5-Idz | C | 481(M++1) | |
A-b-124 | 1-a | A-b-123 | cHexMeO | H | Cl | 1Me-5-Idz | C | 453(M++1) | ||
A-b-125 | 4f-2 | Int.A-32 | Al3 | cHexO | Et | Cl | 1Me-5-Idz | C | 467(M++1) | |
A-b-126 | 1-a | A-b-125 | cHexO | H | Cl | 1Me-5-Idz | C | 439(M++1) | ||
A-b-127 | 4f-2 | Int.A-32 | Al4 | cHepO | Et | Cl | 1Me-5-Idz | C | 481(M++1) | |
A-b-128 | 1-a | A-b-127 | cHepO | H | Cl | 1Me-5-Idz | C | 453(M++1) | ||
A-b-129 | 4f-1 | Int.A-32 | Hal3 | nPrO | Et | Cl | 1Me-5-Idz | C | 426(M++1) | |
A-b-130 | 1-a | A-b-129 | nPrO | H | Cl | 1Me-5-Idz | C | 398(M++1) | ||
A-b-131 | 4f-1 | Int.A-32 | Hal4 | iPrO | Et | Cl | 1Me-5-Idz | C | 426(M++1) | |
A-b-132 | 1-a | A-b-131 | iPrO | H | Cl | 1Me-5-Idz | C | 398(M++1) |
Table-A-b-4 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-b-133 | 4f-1 | Int.A-32 | Hal5 | nBuO | Et | Cl | 1Me-5-Idz | C | 440(M++1) | |
A-b-134 | 1-a | A-b-133 | nBuO | H | Cl | 1Me-5-Idz | C | 412(M++1) | ||
A-b-135 | 4f-1 | Int.A-32 | Hal6 | iBuO | Et | Cl | 1Me-5-Idz | C | 440(M++1) | |
A-b-136 | 1-a | A-b-135 | iBuO | H | Cl | 1Me-5-Idz | C | 412(M++1) | ||
A-b-137 | 4f-1 | Int.A-32 | Hal1 | BnO | Et | Cl | 1Me-5-Idz | C | 475(M++1) | |
A-b-138 | 1-a | A-b-137 | BnO | H | Cl | 1Me-5-Idz | C | 447(M++1) | ||
A-b-139 | 4f-1 | Int.A-32 | Hal7 | 2FBnO | Et | Cl | 1Me-5-Idz | C | 493(M++1) | |
A-b-140 | 1-a | A-b-139 | 2FBnO | H | Cl | 1Me-5-Idz | C | 465(M++1) | ||
A-b-141 | 4f-1 | Int.A-32 | Hal8 | 3FBnO | Et | Cl | 1Me-5-Idz | C | 493(M++1) | |
A-b-142 | 1-a | A-b-141 | 3FBnO | H | Cl | 1Me-5-Idz | C | 465(M++1) | ||
A-b-143 | 4f-1 | Int.A-32 | Hal9 | 4FBnO | Et | Cl | 1Me-5-Idz | C | 492(M++1) | |
A-b-144 | 1-a | A-b-143 | 4FBnO | H | Cl | 1Me-5-Idz | C | 464(M++1) | ||
A-b-145 | 4f-1 | Int.A-32 | Hal10 | 2ClBnO | Et | Cl | 1Me-5-Idz | C | 509(M++1) | |
A-b-146 | 1-a | A-b-145 | 2ClBnO | H | Cl | 1Me-5-Idz | C | 481(M++1) | ||
A-b-147 | 4f-1 | Int.A-32 | Hal11 | 3ClBnO | Et | Cl | 1Me-5-Idz | C | 509(M++1) | |
A-b-148 | 1-a | A-b-147 | 3ClBnO | H | Cl | 1Me-5-Idz | C | 481(M++1) | ||
A-b-149 | 4f-1 | Int.A-32 | Hal12 | 4MeBnO | Et | Cl | 1Me-5-Idz | C | 489(M++1) | |
A-b-150 | 1-a | A-b-149 | 4MeBnO | H | Cl | 1Me-5-Idz | C | 461(M++1) | ||
A-b-151 | 4f-1 | Int.A-32 | Hal13 | 4CF3BnO | Et | Cl | 1Me-5-Idz | C | 542(M++1) | |
A-b-152 | 1-a | A-b-151 | 4CF3BnO | H | Cl | 1Me-5-Idz | C | 514(M++1) | ||
A-b-153 | 4f-2 | Int.A-32 | Al5 | 2EtBuO | Et | Cl | 1Me-5-Idz | C | 469(M++1) | |
A-b-154 | 1-a | A-b-153 | 2EtBuO | H | Cl | 1Me-5-Idz | C | 441(M++1) | ||
A-b-155 | 4f-2 | Int.A-32 | Al6 | 2(4DMAPh)EtO | Et | Cl | 1Me-5-Idz | C | 533(M++1) | |
A-b-156 | 1-a | A-b-155 | 2(4DMAPh)EtO | H | Cl | 1Me-5-Idz | C | 505(M++1) | ||
A-b-157 | 4f-2 | Int.A-32 | Al7 | 2(PhO)EtO | Et | Cl | 1Me-5-Idz | C | 505(M++1) | |
A-b-158 | 1-a | A-b-157 | 2(PhO)EtO | H | Cl | 1Me-5-Idz | C | 477(M++1) | ||
A-b-159 | 4f-2 | Int.A-32 | Al8 | 1PhEtO | Et | Cl | 1Me-5-Idz | C | 489(M++1) | |
A-b-160 | 1-a | A-b-159 | 1PhEtO | H | Cl | 1Me-5-Idz | C | 461(M++1) | ||
A-b-161 | 4f-2 | Int.A-32 | Al9 | 1(2FPh)EtO | Et | Cl | 1Me-5-Idz | C | 507(M++1) | |
A-b-162 | 1-a | A-b-161 | 1(2FPh)EtO | H | Cl | 1Me-5-Idz | C | 479(M++1) | ||
A-b-163 | 4f-2 | Int.A-32 | Al10 | 1(4ClPh)EtO | Et | Cl | 1Me-5-Idz | C | 524(M++1) | |
A-b-164 | 1-a | A-b-163 | 1(4ClPh)EtO | H | Cl | 1Me-5-Idz | C | 496(M++1) | ||
A-b-165 | 4f-2 | Int.A-32 | Al11 | 4Me,cHexO | Et | Cl | 1Me-5-Idz | C | 481(M++1) | |
A-b-166 | 1-a | A-b-165 | 4Me,cHexO | H | Cl | 1Me-5-Idz | C | 453(M++1) | ||
A-b-167 | 4f-2 | Int.A-32 | Al12 |
|
Et | Cl | 1Me-5-Idz | C | 517(M++1) | |
A-b-168 | 1-a | A-b-167 |
|
H | Cl | 1Me-5-Idz | C | 489(M++1) | ||
A-b-169 | 4f-2 | Int.A-32 | Al13 |
|
Et | Cl | 1Me-5-Idz | C | 517(M++1) | |
A-b-170 | 1-a | A-b-169 |
|
H | Cl | 1Me-5-Idz | C | 489(M++1) | ||
A-b-171 | 4f-2 | Int.A-32 | Al15 |
|
Et | Cl | 1Me-5-Idz | C | 585(M++1) | |
A-b-172 | 1-a | A-b-171 |
|
H | Cl | 1Me-5-Idz | C | 557(M++1) | ||
A-b-173 | 4f-2 | Int.A-32 | Al16 |
|
Et | Cl | 1Me-5-Idz | C | 517(M++1) |
Table-A-b-5 | ||||||||||
Exp. | Syn. | SM | Reagent | Rx | Y | V1' | V2' | LCMS | ||
method | RTime | Mass | ||||||||
A-b-174 | 1-a | A-b-173 | & |