EP 0975593 A1 20000202 - INDOLE DERIVATIVES HAVING COMBINED 5HT1A, 5HT1B AND 5HT1D RECEPTOR ANTAGONIST ACTIVITY
Title (en)
INDOLE DERIVATIVES HAVING COMBINED 5HT1A, 5HT1B AND 5HT1D RECEPTOR ANTAGONIST ACTIVITY
Title (de)
INDOLDERIVATE MIT GLEICHZEITIGER 5HT1A, 5HT1B UND 5HT1D REZEPTOR ANTAGONISTISCHER AKTIVITÄT
Title (fr)
DERIVES INDOLIQUES A ACTIVITE DE RECEPTEUR ANTAGONISTE 5HT1A, 5HT1B, 5HT1D
Publication
Application
Priority
- EP 9802262 W 19980414
- GB 9707829 A 19970418
- GB 9801882 A 19980129
Abstract (en)
[origin: WO9850358A1] Compounds of formula (I), processes for their preparation and their use as CNS agents are disclosed, in which R<a> is a group of formula (i), in which P<1> is phenyl, bicyclic aryl, a 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or a bicyclic heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur; R<1> is hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, nitro, trifluoromethyl, cyano, SR<9>, SOR<9>, SO2R<9>, SO2NR<1O>R<11>, CO2R<10>, CONR<10>R<11>, CO2NR<10>R<11>, CONR<10>(CH2)cCO2R<11>, (CH2)cNR<10>R<11>, (CH2)cCONR<10>R<11>, (CH2)cNR<10>COR<11>, (CH2)cCO2C1-6alkyl, CO2(CH2)cOR<10>, NR<10>R<11>, NR<10>CO2R<11>, NR<10>CONR<10>R<11>, CR<10>=NOR<11>, NR<10>COOR<11>, CNR<10>=NOR<11>, where R<10> and R<11> are independently hydrogen or C1-6alkyl and c is 1 to 4; R<2> is hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkenyl, C1-6alkoxy, acyl, aryl, acyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO2R<10>, CONR<10>R<11>, NR<10>R<11> where R<10> and R<11> are as defined for R<1>; a is 1, 2 or 3; or R<a> is a group of formula (ii), wherein P<2> and P<3> are independently phenyl, bicyclic aryl, a 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or a bicyclic heterocyclic group containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; A is a bond or oxygen, S(O)m where m is 0 to 2, carbonyl, CH2 or NR<4> where R<4> is hydrogen or C1-6alkyl; R<1> is as defined above for formula (I) or R<1> is an optionally substituted 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; R<2> and R<3> are independently hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkenyl, C1-6alkoxy, acyl, aryl, acyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO2R<10>, CONR<10>R<11>, NR<10>R<11> where R<10> and R<11> are as defined for R<1>; and a and b are independently 1, 2 or 3; Y is -NH-, NR<5> where R<5> is C1-6alkyl, or Y is -CH2- or -O-; V is oxygen or sulphur; D is nitrogen, carbon or a CH group; W is (CR<16>R<17>)t where t is 2, 3 or 4 and R<16> and R<17> are independently hydrogen or C1-6alkyl or W is (CR<16>R<17>)u-J where u is 0, 1, 2 or 3 and J is oxygen, sulphur, CR<16>=CR<17>, CR<16>=N, =CR<16>O, =CR<16>S or =CR<16>-NR<17>; X is nitrogen or carbon; R<b> is hydrogen, halogen, hydroxy, C1-6alkyl, trifluoromethyl, C1-6alkoxy, C2-6alkenyl, C3-7cycloalkyl optionally substituted by C1-4alkyl, or aryl; R<c> is hydrogen or C1-6alkyl; and <o>.....</o> is a single bond when X is nitrogen or a single or double bond when X is carbon.
IPC 1-7
C07D 209/08; C07D 401/12; C07D 403/12; C07D 417/12; C07D 413/12; A61K 31/40
IPC 8 full level
A61K 31/4545 (2006.01); A61K 31/496 (2006.01); A61K 31/497 (2006.01); A61K 31/501 (2006.01); A61K 31/506 (2006.01); A61P 25/00 (2006.01); A61P 43/00 (2006.01); C07D 209/08 (2006.01); C07D 401/10 (2006.01); C07D 401/12 (2006.01); C07D 401/14 (2006.01); C07D 403/12 (2006.01); C07D 405/12 (2006.01); C07D 409/12 (2006.01); C07D 413/12 (2006.01); C07D 417/12 (2006.01); C07D 521/00 (2006.01)
CPC (source: EP KR)
A61P 25/00 (2018.01 - EP); A61P 43/00 (2018.01 - EP); C07D 209/08 (2013.01 - EP KR); C07D 231/12 (2013.01 - EP); C07D 233/56 (2013.01 - EP); C07D 249/08 (2013.01 - EP); C07D 401/10 (2013.01 - EP); C07D 401/12 (2013.01 - EP); C07D 403/12 (2013.01 - EP); C07D 405/12 (2013.01 - EP); C07D 409/12 (2013.01 - EP); C07D 413/12 (2013.01 - EP); C07D 417/12 (2013.01 - EP)
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9850358 A1 19981112; AR 013076 A1 20001213; AU 732863 B2 20010503; AU 7431098 A 19981127; BR 9809092 A 20020122; CA 2288662 A1 19981112; CN 1260781 A 20000719; CO 4950608 A1 20000901; EP 0975593 A1 20000202; HU P0001123 A2 20010428; HU P0001123 A3 20020429; IL 132409 A0 20010319; JP 2001524116 A 20011127; KR 20010006487 A 20010126; NO 995065 D0 19991015; NO 995065 L 19991015; NZ 500252 A 20010727; PL 336317 A1 20000619; TR 199902590 T2 20000621; TW 509687 B 20021111
DOCDB simple family (application)
EP 9802262 W 19980414; AR P980101760 A 19980416; AU 7431098 A 19980414; BR 9809092 A 19980414; CA 2288662 A 19980414; CN 98806185 A 19980414; CO 98021149 A 19980417; EP 98921462 A 19980414; HU P0001123 A 19980414; IL 13240998 A 19980414; JP 54766098 A 19980414; KR 19997009577 A 19991016; NO 995065 A 19991015; NZ 50025298 A 19980414; PL 33631798 A 19980414; TR 9902590 T 19980414; TW 87105843 A 19980417