The present invention relates to the use of CCR5 antagonists in the manufacture of a medicament for the treatment of diseases associated with CCR5 selected from the group consisting of rejection after organ transplantation, graft-versus host diseases and diabetes.

The CCR5 is a receptor for MIP-1α (an abbreviation for macrophage inflammatory protein-1α), MIP-1β (an abbreviation for macrophage inflammatory protein-1β) or RANTES (an abbreviation for regulated upon activation normal T-cell expressed and secreted) and is known to be expressed in lymphoid tissues such as thymus and spleen, monocytes/macrophages, T-cells or the like (see, for example, Samson, M. et al., Boichemistry, 1996, 35, 3362; Raport, C.J. et al., J. Biol. Chem., 1996, 271, 17161, and Combadiere, C. et al., J. Leukoc. Biol., 1996, 60, 147).

As to information about the relationship between the CCR5 and diseases, it has been reported that the CCR5 was expressed in leukocytes such as T-cells in arthrosynovial tissues and synovial fluid of patients suffering from rheumatoid arthritis (see Loetscher, P. et al., Nature, 1998, 391, 344; Mack, M. et al., Arthritis Rheum., 1999, 42, 981 and the like), CCR5 deficient homozygotes were not found in patients suffering from rheumatoid arthritis (see Gomez-Reino, J.J. et al., Arthritis Rheum., 1999, 42, 989), CCR5 was expressed in T-cells in renal biopsy samples of patients suffering from glomerulonephritis, interstitial nephritis and rejection after transplantation (see Segerer, S. et al., Kidney Int., 1999, 56, 52), many T-cells expressing CCR5 were found in blood of patients suffering from multiple sclerosis (see Balashov, K.E., Proc. Natl. Acad. Sci. USA, 1999, 96, 6873), CCR5 was expressed in T-cells infiltrated into liver injury sites of a mouse graft-versus-host disease (GVHD) model and the infiltration of the T-cells was suppressed by administration of an anti-CCR5 antibody (see Murai, M. et al., J. Clin. Invest., 1999, 104, 49), the progression of morbid states in a mouse diabetes model was associated with MIP-1α and CCR5 (see Cameron, M.J. et al., J. Immunol., 2000, 165, 1102) and the like.

Accordingly, CCR5 is thought to be associated with initiation, progression and maintenance of diseases in which the accumulation and activation of monocytes/macrophages and/or T-cells in disease sites can be assumed to be deeply associated with progression of lesions, for example rheumatoid arthritis, nephritis (nephropathy), multiple sclerosis, rejection after organ transplantation, graft-versus-host diseases (GVHD) and diabetes.

Furthermore, based on a report that the CCR5 is specifically expressed in Th1 cells among the T-cells, CCR5 is thought to be associated with initiation, progression and maintenance of many autoimmune diseases and inflammatory diseases such as chronic obstructive pulmonary diseases (COPD), asthma, atopic dermatitis, sarcoidosis, fibrosis, atherosclerosis, psoriasis and inflammatory bowl diseases in which Th1 cells can be assumed to be associated with morbid states including the above diseases (see Bonecchi, R. et al., J. Exp. Med., 1998, 187, 129; Loetscher, P. et al., Nature, 1998, 391, 344 and the like).

On the other hand, although CD4 is known as a receptor when a host cell is infected with HIV (human immunodeficiency virus), it has been suggested that a second receptor (a coreceptor receptor) is necessary because the infection of HIV is not established only with the CD4. Usually, HIV-1 is roughly classified into a macrophage-tropic (M-tropic) strain and a T-cell-tropic (T-trophic) strain depending on the species of cells that the virus can infect, and it has been elucidated that a coreceptor essential to the infection of the macrophage-tropic strain is CCR5 (see, for example, Deng, H. et al., Nature, 1996, 381, 661; Dragic, T. et al., Nature, 1996, 381, 667; Alkhatib, G. et al., Science, 1996, 272, 1955; Choe, H. et al., Cell, 1996, 85,1135; and Doranz, B.J. et al., Cell, 1996, 85,1149).

Therefore, drugs capable of inhibiting the binding of HIV-1 to CCR5 are thought to be effective as new remedies and/or prophylactics for AIDS (acquired immunodeficiency syndrome) (see Michael, N.L. et al., Nature Med., 1999, 5, 740; Proudfoot, A.E.I. et al., Biochem. Pharmacol., 1999, 57, 451; Murakami et al., Protein, Nucleic Acid and Enzyme, 1998, 43, 677 and the like). As information supporting the above inference, it has been reported that RANTES, MIP-1α and MIP-1β which are ligands of CCR5 were suppressive factors for HIV-1 infection (see Cocchi, F. et al., Science, 1995, 270, 1811), humans without expressing normal CCR5 at all by deficiency of 32 base pairs of CCR5 gene had resistance to HIV-1 infection and any other abnormality in health is not caused by the deficiency (see Liu, R. et al., Cell, 1996, 86, 367; Samson, M. et al., Nature, 1996, 382, 722; Dean, M. et al., Science, 1996, 273, 1856 and the like), anti-CCR5 monoclonal antibodies inhibited the infection of peripheral blood monocytes by macrophage-tropic HIV-1 (see Wu, L. et al., J. Exp. Med., 1997, 185, 1681), RANTES in which the amino terminals were missing or modified was an antagonist of the RANTES to inhibit the infection with macrophage-tropic HIV-1 (see Arenzana-Seisdedos, F. et al., Nature, 1996, 383, 400; Proost, P. et al., J. Biol. Chem., 1998, 273, 7222; Simmons, G. et al., Science, 1997, 276, 276 and the like) and the like.

As mentioned above, a compound which inhibits the binding of MIP-1α, MIP-1β or RANTES that is an in vivo ligand of the CCR5 to the CCR5 or the binding of HIV-1 which is a pathogenic virus of AIDS to the CCR5, i.e. a CCR5 antagonist is thought to be useful as a remedy and/or prophylactic for diseases such as AIDS, rheumatoid arthritis, nephritis (nephropathy), multiple sclecrosis, rejection after organ transplantation, graft-versus-host diseases (GVHD), diabetes, chronic obstructive pulmonary diseases (COPD), asthma, atopic dermatitis, sarcoidosis, fibrosis, atherosclerosis, psoriasis or inflammatory bowel diseases.

It has recently been reported that substituted bis-acridine derivatives (see W09830218), substituted anilide derivatives (see WO9901127; WO0006085; WO0006146; WO0006153; WO0040239;and W00042852), substituted alkenanilide derivatives (see WO9932100; WO0010965; WO0037455; and Baba, et al., Proc. Natl. Acad. Sci. USA, 1999, 96, 5698), 3-(4-piperidinyl)indole derivatives (see WO9917773 and W0042045), azacycloalkane derivatives (see EP1013276; WO0038680; and WO0039125), benzodipyran derivatives (see W00053175) and pyrrolidine derivatives (see WO0059497; WO0059498; WO0059502; and WO0059503) have an antagonistic activity against CCR5. These compounds, however, are different from the compounds used in the present invention.

On the other hand, although the compounds used in the present invention are the same as those described in WO9925686, the compounds are not known to have the antagonistic activity against the CCR5.

It is an object of the present invention to provide the use of a CCR5 antagonist in the manufacture of a medicament for the treatment of diseases associated with CCR5 selected from the group consisting of rejection after organ transplantation, graft-versus host diseases and diabetes.

As a result of intensive studies, the inventors have found that cyclic amine derivatives having an arylalkyl group, pharmaceutically acceptable C₁-C₆ alkyl addition salts thereof or pharmaceutically acceptable acid addition salts thereof have the CCR5 antagonistic activity. Furthermore, studies have been promoted according to findings that those compounds can be useful as remedies or prophylactics for diseases considered to be in association with CCR5. Thereby, the present invention has been accomplished.

Namely, according to the present invention, there are provided the use of a compound having the CCR5 antagonistic activity represented by the following formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C_1-C₆ alkyl addition salt thereof, as an active ingredient: wherein, R¹ is a phenyl group, a C₃-C₈ cycloalkyl group or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms; the phenyl group or the aromatic heterocyclic group in the above R¹ may be condensed with a benzene ring, or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms to form a condensed ring; the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹ may be substituted with an optional number of halogen atoms, hydroxy groups, cyano groups, nitro groups, carboxy groups, carbamoyl groups, C₁-C₆ alkyl groups, C₃-C₈ cycloalkyl groups, C₂-C₆ alkenyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, C₃-C₅ alkylene groups, C₂-C₄ alkylenoxy groups, C₁-C₃ alkylenedioxy groups, phenyl groups, phenoxy groups, phenylthio groups, benzyl groups, benzyloxy groups, benzoylamino groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₄-C₉ N-cycloalkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, C₃-C₈ (alkoxycarbonyl)methyl groups, N-phenylcarbamoyl groups, piperidinocarbonyl groups, morpholinocarbonyl groups; 1-pyrrolidinylcarbonyl groups, bivalent groups represented by the formula: -NH(C=O)O-, bivalent groups represented by the formula:
-NH(C=S)O-, amino groups, mono(C₁-C₆ alkyl)amino groups or di(C₁-C₆ alkyl)amino groups; the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring may further be substituted with an optional number of halogen atoms, hydroxy groups, amino groups, trifluoromethyl groups, C₁-C₆ alkyl groups or C₁-C₆ alkoxy groups;
R² is a hydrogen atom, a C₁-C₆ alkyl group, a C₂-C₇ alkoxycarbonyl group, a hydroxy group or a phenyl group; the C₁-C₆ alkyl group or the phenyl group in the R² may be substituted with an optional number of halogen atoms, hydroxy groups, C₁-C₆ alkyl groups or C₁-C₆ alkoxy groups, with the proviso that R² is not a hydroxy group when j is 0;
j is an integer of 0 to 2;
k is an integer of 0 to 2;
m is an integer of 2 to 4;
n is 0 or 1;
R³ is a hydrogen atom or a C₁-C₆ alkyl group which may be substituted with (one or two phenyl groups which may respectively be substituted with the same or different optional number of halogen atoms, hydroxy groups, C₁-C₆ alkyl groups or C₁-C₆ alkoxy groups);
R⁴ and R⁵ are the same or different and are each a hydrogen atom, a hydroxy group, a phenyl group or a C₁-C₆ alkyl group; the C₁-C₆ alkyl group in the R⁴ and R⁵ may be substituted with an optional number of halogen atoms, hydroxy groups, cyano groups, nitro groups, carboxy groups, carbamoyl groups, mercapto groups, guanidino groups, C₃-C₈ cycloalkyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, phenyl groups (which may be substituted with an optional number of halogen atoms, hydroxy groups, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups or benzyloxy groups), phenoxy groups, benzyloxy groups, benzyloxycarbonyl groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, amino groups, mono(C₁-C₆ alkyl)amino groups, di(C₁-C₆ alkyl)amino groups or (aromatic heterocyclic groups having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms or condensed rings formed by condensation of the aromatic heterocyclic groups having the one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as the heteroatoms with a benzene ring), or both R⁴ and R⁶ together may form a three- to a six-membered cyclic hydrocarbon;
p is 0 or 1;
q is 0 or 1;
G is a group represented by -CO-, -SO₂-, -CO-O-, -NR⁷-CO-, -CO-NR⁷-, -NH-CO-NH-, -NH-CS-NH-, -NR⁷-SO₂-, -SO₂-NR⁷-, -NH-CO-O- or -O-CO-NH-, wherein, R⁷ is a hydrogen atom or a C₁-C₆ alkyl group or R⁷, together with R⁶, may form a C₂-C₆ alkylene group;
R⁶ is a phenyl group, a C₃-C₈ cycloalkyl group, a C₃-C₆ cycloalkenyl group, a benzyl group or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms; the phenyl group, the benzyl group or the aromatic heterocyclic group in the R⁶ may be condensed with a benzene ring or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms to form a condensed ring; the phenyl group, the C₃-C₈ cycloalkyl group, the C₃-C₆ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed ring in the above R⁶ may further be substituted with an optional number of halogen atoms, hydroxy groups; mercapto groups, cyano groups, nitro groups, thiocyanato groups, carboxy groups, carbamoyl groups, trifluoromethyl groups, C₁-C₆ alkyl groups, C₃-C₈ cycloalkyl groups, C₂-C₆ alkenyl groups, C₁-C₆ alkoxy groups, C₃-C₈ cycloalkyloxy groups, C₁-C₆ alkylthio groups, C₁-C₃ alkylenedioxy groups, phenyl groups, phenoxy groups, phenylamino groups, benzyl groups, benzoyl groups, phenylsulfinyl groups, phenylsulfonyl groups, 3-phenylureido groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, phenylcarbamoyl groups, N,N-di(C₁-C₆ alkyl)sulfamoyl groups, amino groups, mono(C₁-C₆ alkyl)amino groups, di(C₁-C₆ alkyl)amino groups, benzylamino groups, C_2-C₇ (alkoxycarbonyl)amino groups, C₁-C₆ (alkylsulfonyl)amino groups or bis(C₁-C₆ alkylsulfonyl)amino groups; the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the C₃-C₈ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed ring may further be substituted with an optional number of halogen atoms, cyano groups, hydroxy groups, amino groups, trifluoromethyl groups, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, mono(C₁-C₆ alkyl)amino groups or di(C₁-C₆ alkyl)amino groups, in the manufacture of a medicament for the treatment of diseases associated with CCR5 selected from the group consisting of rejection after organ transplantation, graft-versus-host diseases and diabetes.

The compound represented by the above formula (I) has the CCR5 antagonistic activity and the inhibitory activity against physiological actions of in vivo ligands of CCR5 on target cells, i.e. the compound represented by the above formula (I) are a CCR5 antagonist.

In the above formula (I), R¹ is a phenyl group, a C₃-C₈ cycloalkyl group or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms; the phenyl group or the aromatic heterocyclic group in the above R¹ may be condensed with a benzene ring or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms to form a condensed ring; the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹ may further be substituted with an optional number of halogen atoms, hydroxy groups, cyano groups, nitro groups, carboxy groups, carbamoyl groups, C₁-C₆ alkyl groups, C₃-C₈ cycloalkyl groups, C₂-C₆aLkenyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, C₃-C₅ alkylene groups, C₂-C₄ alkylenoxy groups, C_1-C₃ alkylenedioxy groups, phenyl groups, phenoxy groups, phenylthio groups, benzyl groups, benzyloxy groups, benzoylamino groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₄-C₉ N-cycloalkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, C₃-C₈ (alkoxycarbonyl)methyl groups, N-phenylcarbamoyl groups, piperidinocarbonyl groups, morpholinocarbonyl groups, 1-pyrrolidinylcarbonyl groups, bivalent groups represented by the formula: -NH(C=O)O-, bivalent groups represented by the formula: -NH(C=S)O-, amino groups, mono(C₁-C₆ alkyl)amino groups or di(C₁-C₆ alkyl)amino groups.

The "C₃-C₈ cycloalkyl group" in R¹ means a cyclic alkyl group, and includes for example cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclooctyl group and the like. The "C₃-C₈ cycloalkyl group" is preferably cyclopropyl group, cyclopentyl group, cyclohexyl group and the like.

The "aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms" in R¹ means an aromatic heterocyclic group, and includes for example thienyl group, furyl group, pyrrolyl group, imidazolyl group, pyrazolyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, pyridyl group, pyrimidinyl group, triazinyl group, triazolyl group, oxadiazolyl (furazanyl) group, thiadiazolyl group and the like. The "aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms" is preferably thienyl group, furyl group, pyrrolyl group, isoxazolyl group, pyridyl group and the like.

The "condensed ring" in R¹ means a bicyclic aromatic heterocyclic group formed by condensing the phenyl group or the aromatic heterocyclic group with a benzene ring or the aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms in an optional position, and includes for example naphthyl group, indolyl group, benzofuranyl group, benzothienyl group, quinolyl group, benzimidazolyl group, benzoxazolyl group, benzotriazolyl group, benzoxadiazolyl (benzofurazanyl), group, benzothiadiazolyl group and the like.

Among them, it is especially preferable for R¹ to be a phenyl group, a thienyl group, a pyrrolyl group, a pyrazolyl group, an isoxazolyl group or an indolyl group.

The "halogen atoms" as the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in R¹ mean a fluorine atom, a chlorine atom, a bromine atom, an iodine atom and the like, and fluorine atom, chlorine atom, bromine atom and iodine atom are specifically preferable.

The "C₁-C₆ alkyl groups" as the substituents of R¹ mean C₁-C₆ straight or branched alkyl groups, and include for example, methyl group, ethyl group, n-propyl group; n-butyl group, n-pentyl group, n-hexyl group, n-heptyl group, n-octyl group, isopropyl group, isobutyl group, sec-butyl group, tert-butyl group, isopentyl group, neopentyl group, tert-pentyl group, isohexyl group, 2-methylpentyl group, 1-ethylbutyl group and the like. The "C₁-C₆ alkyl groups" are, as specifically preferable concrete examples, methyl group, ethyl group, propyl group, isopropyl group, tert-butyl group and the like.

The "C₃-C₈ cycloalkyl groups" as the substituents of R¹ are the same as defined in the "C₃-C₈ cycloalkyl group" in the above R¹, and specifically preferably include for example the same groups.

The "C₂-C₆ alkenyl groups" as the substituents of R¹ mean C₂-C₆ straight or branched alkenyl groups, and include for example vinyl group, allyl group, 1-propenyl group, 2-butenyl group, 3-butenyl group, 2-methyl-1-propenyl group, 4-pentenyl group, 5-hexenyl group, 4-methyl-3-pentenyl group and the like. The "C₂-C₆ alkenyl groups" are specifically preferably vinyl group and 2-methyl-1-propenyl group or the like.

The "C₁-C₆ alkoxy groups" as the substituents of R¹ mean groups composed of the above C₁-C₆ alkyl groups and oxy group, and methoxy group, ethoxy group or the like is specifically preferable.

The "C₁-C₆ alkylthio groups" as the substituents of R¹ mean groups composed of the above C₁-C₆ alkyl groups and thio group, and methylthio group, ethylthio group or the like is specifically preferable.

The "C₃-C₅ alkylene groups" as the substituents of R¹ mean C₃-C₅ bivalent alkylene groups, and include for example, trimethylene group, tetramethylene group, pentamethylene group, 1-methyltrimethylene group and the like. The "C₃-C₅ alkylene groups" are specifically preferably trimethylene group, tetramethylene group or the like.

The "C₂-C₄ alkylenoxy groups" as the substituents of R¹ mean groups composed of C₂-C₄ bivalent alkylene groups and oxy group and include, for example, ethylenoxy group (-CH₂CH₂O-), trimethylenoxy group (-CH₂CH₂CH₂O-), tetramethylenoxy group (-CH₂CH₂CH₂CH₂O-), 1,1-dimethylethylenoxy group (-CH₂C(CH₃)₂O-) and the like. The "C₂-C₄ alkylenoxy groups" are specifically preferably ethylenoxy group, trimethylenoxy group or the like.

The "C₁-C₃ alkylenedioxy groups" as the substituents of R¹ mean groups composed of C₁-C₃ bivalent alkylene groups and two oxy groups and include, for example, methylenedioxy group (-OCH₂O-), ethylenedioxy group (-OCH₂CH₂O-), trimethylenedioxy (-OCH₂CH₂CH₂O-) group and propylenedioxy (-OCH₂CH(CH₃)O-) group and the like. The "C₁-C₃ alkylenedioxy groups" are specifically preferably methylenedioxy group, ethylenedioxy group or the like.

The "C₂-C₇ alkanoyl groups" as the substituents of R¹ mean C₂-C₇ straight or branched alkanoyl groups, and include for example, acetyl group, propanoyl group, butanoyl group, pentanoyl group, hexanoyl group, heptanoyl group, isobutyryl group, 3-methylbutanoyl group, 2-methylbutanoyl group, pivaloyl group, 4-methylpentanoyl group, 3,3-dimethylbutanoyl group, 5-methylhexanoyl group and the like, and acetyl group or the like is specifically preferable.

The "C₂-C₇ alkoxycarbonyl groups" as the substituents of R¹ mean groups composed of the above C₁-C₆ alkoxy groups and carbonyl group, and methoxycarbonyl group, ethoxycarbonyl group or the like is specifically preferable.

The "C₂-C₇ alkanoyloxy groups" as the substituents of R¹ mean groups composed of the above C₂-C₇ alkanoyl groups and oxy group, and acetyloxy group or the like is specifically preferable.

The "C₂-C₇ alkanoylamino groups" as the substituents of R¹ mean groups composed of the above C₂-C₇ alkanoyl groups and amino group, and acetylamino group or the like is specifically preferable.

The "C₂-C₇ alkylcarbamoyl groups" as the substituents of R¹ mean groups composed of the above C₁-C₆ alkyl groups and carbamoyl group, and N-methylcarbamoyl group, N-ethylcarbamoyl group or the like is specifically preferable.

The "C₄-C₉ N-cycloalkylcarbamoyl groups" as the substituents of R¹ mean the above C₃-C₈ cycloalkyl groups and carbamoyl group, and N-cyclopentylcarbamoyl group, N-cyclohexylcarbamoyl group or the like is preferable.

The "C₁-C₆ alkylsulfonyl groups" as the substituents of R¹ mean groups composed of the above C₁-C₆ alkyl groups and sulfonyl group, and methylsulfonyl group or the like is specifically preferable.

The "C₃-C₈ (alkoxycarbonyl)methyl groups" as the substituents of R¹ mean groups composed of the above C₂-C₇ alkoxycarbonyl groups and methyl group, and (methoxycarbonyl)methyl group, (ethoxycarbonyl)methyl group or the like is specifically preferable.

The "mono(C₁-C₆ alkyl)amino groups" as the substituents of R¹ mean amino groups substituted with the above C₁-C₆ alkyl groups, and methylamino group, ethylamino group or the like is specifically preferable.

The "di(C₁-C₆ alkyl)amino groups" as the substituents of R¹ mean amino groups substituted with the same or different two C₁-C₆ alkyl groups described above, and dimethylamino group, diethylamino group, N-ethyl-N-methylamino group or the like is specifically preferable.

Among those described above, examples of the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in R¹ are specifically preferably halogen atoms, hydroxy groups, cyano groups, C₁-C₆ alkyl groups, C₂-C₆ alkenyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, C₃-C₅ alkylene groups, C₂-C₄ alkylenoxy groups, alkylenedioxy groups, acetyl groups, phenyl groups, amino groups and di(C₁-C₆ alkyl)amino groups, and halogen atoms, hydroxy groups, cyano groups, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups, Cs-C₅ alkylene groups, methylenedioxy groups and amino groups are especially preferable.

Moreover, the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in R¹, may further be substituted with an optional number of halogen atoms, hydroxy groups, amino groups, trifluoromethyl groups, C₁-C₆ alkyl groups or C₁-C₆ alkoxy groups. The halogen atoms, C₁-C₆ alkyl groups and C₁-C₆ alkoxy groups are the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in R¹, and the same groups are specifically preferable.

In the above formula (I), R² is a hydrogen atom, a C₁-C₆ alkyl group, a C₂-C₇ alkoxycarbonyl group, a hydroxy group or a phenyl group; and the C₁-C₆ alkyl group or phenyl group in R² may be substituted with an optional number of halogen atoms, hydroxy groups, C₁-C₆ alkyl groups or C₁-C₆ alkoxy groups, with the proviso that R² is not a hydroxy group when j is 0.

The C₁-C₆ alkyl group and C₂-C₇ alkoxycarbonyl group in R² are each the same as defined for the substituents of the phenyl group, the C_3-Cs cycloalkyl group, the aromatic heterocyclic group or the condensed ring in R¹, and the same examples are specifically preferable.

The halogen atoms, C₁-C₆ alkyl groups and C₁-C₆ alkoxy groups as the substituents of the C₁-C₆ alkyl group or the phenyl, group in R² are the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

Among them, it is especially preferable for R² to be a hydrogen atom.

In the above formula (I), j is an integer of 0 to 2, and it is especially preferable for j to be 0.

In the above formula (I), k is an integer of 0 to 2; m is an integer of 2 to 4. Among them, it is especially preferable for the compounds to be 2-substituted pyrrolidines wherein k is 0 and m is 3; 3-substituted pyrrolidines wherein k is 1 and m is 2; 3-substituted piperidines wherein k is 1 and m is 3; 4-substituted piperidines wherein k is 2 and m is 2; or 3-substituted hexahydroazepines wherein k is 1 and m is 4, and 3-substituted pyrrolidines wherein k is 1 and m is 2 and 4-substituted piperidines wherein k is 2 and m is 2 are especially preferable.

In the above formula (I), n is 0 or 1.

In particular, 3-amidopyrrolidines wherein k is 1; m is 2 and n is 0 and 4-(amidomethyl)piperidines wherein k is 2; m is 2 and n is 1 are especially preferable.

In the above formula (I), R³ is a hydrogen atom or a C₁-C₆ alkyl group which may be substituted with (one or two phenyl groups which may respectively be substituted with an optional number of the same or different halogen atoms, hydroxy groups, C₁-C₆ alkyl groups or C₁-C₆ alkoxy groups).

The C₁-C₆ alkyl group in R³ is the same as defined for the substituent of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and methyl group, ethyl group and propyl group are specifically preferable.

The halogen atoms, C₁-C₆ alkyl groups and C₁-C₆ alkoxy groups as the substituents of the phenyl groups as the substituents of the C₁-C₆ alkyl group in R³ are each the same as defined for substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

Among them, it is especially preferable for R³ to be a hydrogen atom and an unsubstituted C₁-C₆ alkyl group.

In the above formula (I), R⁴ and R⁵ are each the same or different and are each a hydrogen atom, a hydroxy group, a phenyl group or a C₁-C₆ alkyl group; and the C₁-C₆ alkyl group in R⁴ and R⁵ may be substituted with an optional number of halogen atoms, hydroxy groups, cyano groups, nitro groups, carboxy groups, carbamoyl groups, mercapto groups, guanidino groups, C₃-C₈ cycloalkyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, (phenyl groups which may be substituted with an optional number of halogen atoms, hydroxy groups, C₁-C₆ alkyl groups, C_1-C₆ alkoxy groups or benzyloxy groups), phenoxy groups, benzyloxy groups, benzyloxycarbonyl groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, amino groups, mono(C₁-C₆ alkyl)amino groups, di(C₁-C₆ alkyl)amino groups or (aromatic heterocyclic groups having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms or condensed rings formed by condensation thereof with benzene rings) or both R⁴ and R⁵ together may form a three- to a six-membered cyclic hydrocarbon.

The C₁-C₆ alkyl group in R⁴ and R⁵ is the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

The halogen atoms, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, mono(C₁-C₆ alkyl)amino groups and di(C₁-C₆ alkyl)amino groups as the substituents of the C₁-C₆ alkyl group in R⁴ and R⁵ are the same as defined for the substituents of the phenyl group, the C_3-Cs cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

The C₃-C₈ cycloalkyl groups and the aromatic heterocyclic groups having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms as the substituents of the C₁-C₆ alkyl group in R⁴ and R⁵ are the same as defined for the above R¹, and the same examples are preferable.

The halogen atoms, C₁-C₆ alkyl groups and C₁-C₆ alkoxy groups as the substituents of the phenyl groups as the substituents of the C₁-C₆ alkyl group in R⁴ and R⁵ are the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

The "three- to a six-membered cyclic hydrocarbon" composed of R⁴, R⁵ and the adjacent carbon atoms are specifically preferably cyclopropane, cyclobutane, cyclopentane, cyclohexane and the like.

Among them, the hydrogen atom and C₁-C₆ alkyl group are especially preferable for R⁴ and R⁵.

In the above formula (I), p is 0 or 1; and q is 0 or 1. Both p and q are especially preferably 0.

In the above formula (I), G is a group represented by -CO-, -SO₂-, -CO-O-, -NR⁷-CO-, -CO-NR⁷-, -NH-CO-NH-, -NH-CS-NH-, -NR⁷-SO₂-, -SO₂-NR⁷-, -NH-CO-O- or -O-CO-NH-,
wherein, R⁷ is a hydrogen atom or a C₁-C₆ alkyl group or R⁷, together with R⁵, may form a C₂-C₅ alkylene group,
wherein, -CO- is a carbonyl group, -SO₂- is a sulfonyl group and -CS- is a thiocarbonyl group. G is especially preferably the group represented by -NR⁷-CO- or -NH-CO-NH-.

The C₁-C₆ alkyl group in R⁷ is the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

The "C₂-C₅ alkylene group" composed of R⁵ and R⁷ means a C₂-C₅ straight or branched alkylene group, for example, methylene group, ethylene group, propylene group, trimethylene group, tetramethylene group, 1-methyltrimethylene group, pentamethylene group and the like, and ethylene group, trimethylene group, tetramethylene group or the like is specifically preferable.

Among them, it is especially preferable for R⁷ to be a hydrogen atom.

In the above formula (I), R⁶ is a phenyl group, a C₃-C₈ cycloalkyl group, a C₃-C₆ cycloalkenyl group, a benzyl group or an aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms; and the phenyl group, the benzyl group or the aromatic heterocyclic group in the above R⁶ may be condensed with a benzene ring or the aromatic heterocyclic group having one to three oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms to form a condensed ring; and the phenyl group, the C₃-C₈ cycloalkyl group, the C₃-C₆ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed ring in the above R⁶ may be substituted with an optional number of halogen atoms, hydroxy groups, mercapto groups, cyano groups, nitro groups, thiocyanato groups, carboxy groups, carbamoyl groups, trifluoromethyl groups, C₁-C₆ alkyl groups, C₃-C₈ cycloalkyl groups, C₂-C₆ alkenyl groups, C₁-C₆ alkoxyl groups, C₃-C₈ cycloalkyloxy groups, C₁-C₆ alkylthio groups, C₁-C₃ alkylenedioxy groups, phenyl groups, phenoxy groups, phenylamino groups, benzyl groups, benzoyl groups, phenylsulfinyl groups, phenylsulfonyl groups, 3-phenylureido groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, phenylcarbamoyl groups, N,N-di(C₁-C₆ alkyl)sulfamoyl groups, amino groups, mono(C₁-C₆ alkyl)amino groups, di(C₁-C₆ alkyl)amino groups, benzylamino groups, C₂-C₇ (alkoxycarbonyl)amino groups, C₁-C₆ (alkylsulfonyl)amino groups or bis(C₁-C₆ alkylsulfonyl)amino groups.

The C₃-C₈ cycloalkyl groups, aromatic heterocyclic groups having oxygen atoms, sulfur atoms and/or nitrogen atoms as heteroatoms, or condensed rings in R⁶ are the same as defined for the above R¹, and the same examples are specifically preferable.

The "C₃-C₈ cycloalkenyl groups" in R⁶ mean cycloalkenyl groups, for example, cyclobutenyl group, cyclopentenyl group, cyclohexenyl group, cycloheptenyl group and cyclooctenyl group, and 1-cyclopentenyl group, 1-cyclohexenyl group or the like is specifically preferable.

Among them, it is especially preferable for R⁶ to be a phenyl group, a furyl group, a thienyl group, a pyrazolyl group, a benzothienyl group and an indolyl group.

The halogen atoms, C₁-C₆ alkyl groups, C₁-C₆ alkenyl groups, C_1-C₆ alkoxy groups, C₁-C₆ alkylthio groups, C₁-C₃ alkylenedioxy groups, C₂-C₇ alkanoyl groups, C₂-C₇ alkoxycarbonyl groups, C₂-C₇ alkanoyloxy groups, C₂-C₇ alkanoylamino groups, C₂-C₇ N-alkylcarbamoyl groups, C₁-C₆ alkylsulfonyl groups, mono(C₁-C₆ alkyl)amino groups and di(C₁-C₆ alkyl)amino groups as the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the C₃-C₈ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed ring in R⁶ are the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

The C₃-C₈ cycloalkyl groups as the substituents of R⁶ are the same as defined for the C₃-C₈ cycloalkyl groups in the above R¹, and the same examples are specifically preferable.

The "C₃-C₈ cycloalkyloxy groups" as the substituents of R⁶ mean groups composed of the above C₃-C₈ cycloalkyl groups and oxy groups, and cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group or the like is specifically preferable.

The "N,N-di(C₁-C₆ alkyl)sulfamoyl groups" as the substituents of R⁶ mean sulfamoyl groups substituted with the same or different two C₁-C₆ alkyl groups described above, and N,N-dimethylsulfamoyl group, N,N-diethylsulfamoyl group, N-ethyl-N-methylsulfamoyl group or the like is specifically preferable.

The "C₂-C₇ (alkoxycarbonyl)amino groups" as the substituents of R⁶ mean groups composed of the above C₂-C₇ alkoxycarbonyl groups and amino groups, and (methoxycarbonyl)amino group, (ethoxycarbonyl)amino group or the like is specifically preferable.

The "C₁-C₆ (alkylsulfonyl)amino groups" as the substituents of R⁶ mean groups composed of the above C₁-C₆ alkylsulfonyl groups and amino groups, and (methylsulfonyl)amino group or the like is specifically preferable.

The "bis(C₁-C₆ alkylsulfonyl)amino groups" as the substituents of R⁶ mean amino groups substituted with the same or different two C₁-C₆ alkylsulfonyl groups described above, and bis(methylsulfonyl)amino group or the like is specifically preferable.

Among them, halogen atoms, nitro groups, trifluoromethyl groups, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups, phenyl groups, phenylsulfonyl groups, amino groups, benzylamino groups and the like are preferable for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the C₃-C₈ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed group in R⁶, and halogen atoms, nitro groups, trifluoromethyl groups, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups, phenylsulfonyl groups and amino group are especially preferable.

Furthermore, the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the C₃-C₈ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed ring in such R⁶ may further be substituted with an optional number of halogen atoms, cyano groups, hydroxy groups, amino groups, trifluoromethyl groups, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, mono(C₁-C₆ alkyl)amino groups or di(C₁-C₆ alkyl)amino groups.

The halogen atoms, C₁-C₆ alkyl groups, C₁-C₆ alkoxy groups, C₁-C₆ alkylthio groups, mono(C₁-C₆ alkyl)amino groups and di(C₁-C₆ alkyl)amino groups as the substituents of the substituents of the phenyl group, the C_3-C₈ cycloalkyl group, the C₃-C₈ cycloalkenyl group, the benzyl group, the aromatic heterocyclic group or the condensed ring in R⁶ are the same as defined for the substituents of the phenyl group, the C₃-C₈ cycloalkyl group, the aromatic heterocyclic aromatic group or the condensed ring in the above R¹, and the same examples are specifically preferable.

A pharmaceutical composition, which is prepared with the remedially effective amount of the compound represented by the above formula (I), the pharmaceutically acceptable acid addition salt thereof or the pharmaceutically acceptable C₁-C₆ alkyl-addition salt thereof together with a pharmaceutically acceptable carrier and/or diluent, can be the medicine capable of inhibiting the binding of an in vivo ligand of CCR5 and/or HIV to the CCR5 on target cells, the medicine having inhibitory actions on physiological actions of the ligand of CCR5 on the target cells, or further the remedy or prophylactic for diseases considered to be in association with the CCR5.

Namely, the cyclic amine derivative represented by the above formula (I), the pharmaceutically acceptable acid addition salt thereof or the pharmaceutically acceptable C₁-C₆ alkyl addition salt thereof can be administered orally or parenterally such as intravenously, subcutaneously, intramuscularly, percutaneously or intrarectally.

For example, a tablet, a pill, a granule, a powder, a liquid, a suspension or a capsule can be cited as the dosage form of the oral administration.

The tablet can be prepared by using a vehicle, for example, lactose, starch or crystalline cellulose; a binder, for example, carboxymethylcellulose, methylcellulose or polyvinylpyrrolidone; or a disintegrator, for example, sodium alginate, sodium bicarbonate or sodium lauryl sulfate or the like according to a conventional method.

The pill, powder and granule can similarly be prepared with using the above vehicle or the like according to a conventional method. The liquid and suspension are prepared with using glycerin esters, for example, tricaprylin or triacetin or alcohols, for example, ethanol according to a conventional method. The capsule is prepared with filling a granule, powder or liquid in a capsule made from gelatin on the like.

A parenteral injection such as the form of an aqueous or a nonaqueous solution formulation is cited as the dosage form of subcutaneous, intramuscular or intravenous administration. For example, an isotonic sodium chloride solution is used as the aqueous solution. Propylene glycol, poly(ethylene glycol), olive oil or ethyl oleate is, for example, used for the nonaqueous solution. An antiseptic, a stabilizer or the like, if necessary, is added thereto. The parenteral injection is sterilized by suitably carrying out treatment such as filtration through a bacterial filter or combination of a disinfectant.

For example, an ointment or a cream is cited as the dosage form of percutaneous administration. The ointment is prepared by using fats and fatty oils such as castor oil or olive oil or vaseline, and the cream is prepared by using a fatty oil or an emulsifying agent such as di(ethylene glycol) or sorbitan mono-fatty acid ester according to a conventional method.

A usual suppository such as a gelatin soft capsule is used for intrarectal administration.

The dose of the cyclic amine derivative, pharmaceutically acceptable acid addition salt thereof or pharmaceutically acceptable C₁-C₆ alkyl addition salt thereof, in the present invention, varies with the types of diseases, routes of administration, age and sex of patients and severity of diseases and the like, but is usually 1 to 500 mg/day for an adult.

Concrete examples of the cyclic amine derivative represented by the above formula (I) preferably includes compounds having respective substituents shown in the following Tables 1.1 to 1.221.

In Tables 1.1 to 1.221, and "Compd. No." means "compound number". "Chirality" means the "absolute configuration", and the "chirality (absolute configuration)" means the absolute configuration of asymmetric carbon on the ring of the cyclic amine. "R" means that the asymmetric carbon atom on the ring of the cyclic amine has the absolute configuration of R, and "S" means that the asymmetric carbon atom has the absolute configuration of S. "-" means that the compound is a racemate or the compound has no asymmetric carbon atom on the cyclic amines. Compd. No. k m n chirality R³ 1 1 2 0 - H 2 1 2 0 - H 3 1 2 0 - H 4 1 2 0 - H 5 1 2 0 S H 6 1 2 0 S H 7 1 2 0 S H 8 1 2 0 S H 9 1 2 0 S H 10 1 2 0 S H 11 1 2 0 S H Compd. No. k m n chirality R³ 12 1 2 0 S H 13 1 2 0 S H 14 1 2 0 S H 15 1 2 0 S H 16 1 2 0 S H 17 1 2 0 S H 18 1 2 0 S H 19 1 2 0 S H 20 1 2 0 S H 21 1 2 0 S H 22 1 2 0 S H Compd. No. k m n chirality R³ 23 1 2 0 S H 24 1 2 0 S H 25 1 2 0 S H 26 1 2 0 S H 27 1 2 0 S H 28 1 2 0 S H 29 1 2 0 R H 30 1 2 0 R H 31 1 2 0 R H 32 1 2 0 R H 33 1 2 0 R H Compd. No. k m n chirality R³ 34 1 2 0 R H 35 1 2 0 R H 36 1 2 0 R H 37 1 2 0 R H 38 1 2 0 R H 39 1 2 0 R H 40 1 2 0 R H 41 1 2 0 R H 42 1 2 0 R H 43 1 2 0 R H 44 1 2 0 R H Compd. No. k m n chirality R³ 45 1 2 0 R H 46 1 2 0 R H 47 1 2 0 R H 48 1 2 0 R H 49 1 2 0 R H 50 1 2 0 R H 51 1 2 0 R H 52 1 2 0 R H 53 1 2 0 R H 54 1 2 0 R H 55 1 2 0 R H Compd. No. k m n chirality R³ 56 1 2 0 R H 57 1 2 0 R H 58 1 2 0 R H 59 1 2 0 R H 60 1 2 0 R H 61 1 2 0 R H 62 1 2 0 R H 63 1 2 0 R H 64 1 2 0 R H 65 1 2 0 R H 66 1 2 0 R H Compd. No. k m n chirality R³ 67 1 2 0 R H 68 1 2 0 R H 69 1 2 0 R H 70 1 2 0 R H 71 1 2 0 R H 72 1 2 0 R H 73 1 2 0 R H 74 1 2 0 R H 75 1 2 0 R H 76 1 2 0 R H 77 1 2 0 R H Compd. No. k m n chirality R³ 78 1 2 0 R H 79 1 2 0 R H 80 1 2 0 R H 81 1 2 0 R H 82 1 2 0 - -CH₃ 83 1 2 0 R H 84 1 2 0 R H 85 1 2 0 - H 86 1 2 0 - H 87 1 2 0 S H 88 1 2 0 S H Compd. No. k m n chirality R³ 89 1 2 0 S H 90 1 2 0 S H 91 1 2 0 S H 92 1 2 0 S H 93 1 2 0 S H 94 1 2 0 S H 95 1 2 0 S H 96 1 2 0 S H 97 1 2 0 S H 98 1 2 0 S H 99 1 2 0 S H Compd. No. k m n chirality R³ 100 1 2 0 S H 101 1 2 0 S H 102 1 2 0 S H 103 1 2 0 S H 104 1 2 0 S H 105 1 2 0 S H 106 1 2 0 S H 107 1 2 0 S H 108 1 2 0 S H 109 1 2 0 S H 110 1 2 0 S H Compd. No. k m n chirality R³ 111 1 2 0 R H 112 1 2 0 R H 113 1 2 0 R H 114 1 2 0 R H 115 1 2 0 R H 116 1 2 0 R H 117 1 2 0 R H 118 1 2 0 R H 119 1 2 0 R H 120 1 2 0 R H 121 1 2 0 R H Compd. No. k m n chirality R³ 122 1 2 0 R H 123 1 2 0 R H 124 1 2 0 R H 125 1 2 0 R H 126 1 2 0 R H 127 1 2 0 R H 128 1 2 0 R H 129 1 2 0 R H 130 1 2 0 R H 131 1 2 0 R H 132 1 2 0 R H Compd. No. k m n chirality R³ 133 1 2 0 R H 134 1 2 0 R H 135 1 2 0 R H 136 1 2 0 R H 137 1 2 0 R H 138 1 2 0 R H 139 1 2 0 R H 140 1 2 0 R H 141 1 2 0 R H 142 1 2 0 R H 143 1 2 0 R H Compd. No. k m n chirality R³ 144 1 2 0 R H 145 1 2 0 R H 146 1 2 0 R H 147 1 2 0 R H 148 1 2 0 R H 149 1 2 0 R H 150 1 2 0 R H 151 1 2 0 R H 152 1 2 0 R H 153 1 2 0 R H 154 1 2 0 R H Compd. No. k m n chirality R³ 155 1 2 0 R H 156 1 2 0 R H 157 1 2 0 R H 158 1 2 0 R H 159 1 2 0 R H 160 1 2 0 R H 161 1 2 0 R H 162 1 2 0 R H 163 1 2 0 R H 164 1 2 0 R H 165 1 2 0 R H Compd. No. k m n chirality R³ 166 1 2 0 R H 167 1 2 0 R H 168 1 2 0 R H 169 1 2 0 R H 170 1 2 0 R H 171 1 2 0 R H 172 1 2 0 R H 173 1 2 0 R H 174 1 2 0 R H 175 1 2 0 R H 176 10 2 0 R H Compd. No. k m n chirality R³ 177 1 2 0 R H 178 1 2 0 R H 179 1 2 0 R H 180 1 2 0 R H 181 1 2 0 R H 182 1 2 0 R H 183 1 2 0 R H 184 1 2 0 R H 185 1 2 0 R H 186 1 2 0 R H 187 1 2 0 R H Compd. No. k m n chirality R³ 188 1 2 0 R H 189 1 2 0 R H 190 1 2 0 R H 191 1 2 0 R H 192 1 2 0 R H 193 1 2 0 R H 194 1 2 0 R H 195 1 2 0 R H 196 1 2 0 R H 197 1 2 0 R H 198 1 2 0 R H Compd. No. k m n chirality R³ 199 1 2 0 R H 200 1 2 0 R H 201 1 2 0 R H 202 1 2 0 R H 203 1 2 0 R H 204 1 2 0 R H 205 1 2 0 R H 206 1 2 0 R H 207 1 2 0 R H 208 1 2 0 R H 209 1 2 0 R H Compd. No. k m n chirality R³ 210 1 2 0 R H 211 1 2 0 R H 212 1 2 0 R H 213 1 2 0 R H 214 1 2 0 - H 215 1 2 0 - H 216 1 2 0 - H 217 1 2 0 - H 218 1 2 0 - H 219 1 2 0 - H 220 1 2 0 - H Compd. No. k m n chirality R³ 221 1 2 0 - H 222 1 2 0 - H 223 1 2 0 - H 224 1 2 0 - H 225 1 2 0 - H 226 1 2 0 - H 227 1 2 0 - H 228 1 2 0 - H 229 1 2 0 - H 230 1 2 0 - H 231 1 2 0 - H Compd. No. k m n chirality R³ 232 1 2 0 - H 233 1 2 0 - H 234 1 2 0 - H 235 1 2 0 - H 236 1 2 0 - H 237 1 2 0 - H 238 1 2 0 - H 239 1 2 0 S H 240 1 2 0 S H 241 1 2 0 S H 242 1 2 0 S H Compd. No. k m n chirality R³ 243 1 2 0 S H 244 1 2 0 S H 245 1 2 0 S H 246 1 2 0 S H 247 1 2 0 S H 248 1 2 0 S H 249 1 2 0 S H 250 1 2 0 S H 251 1 2 0 S H 252 1 2 0 S H 253 1 2 0 S H Compd. No. k m n chirality R³ 254 1 2 0 S H 255 1 2 0 S H 256 1 2 0 S H 257 1 2 0 S H 258 1 2 0 S H 259 1 2 0 S H 260 1 2 0 S H 261 1 2 0 S H 262 1 2 0 S H 263 1 2 0 S H 264 1 2 0 S H Compd. No. k m n chirality R³ 265 1 2 0 S H 266 1 2 0 S H 267 1 2 0 S H 268 1 2 0 S H 269 1 2 0 S H 270 1 2 0 S H 271 1 2 0 S H 272 1 2 0 S H 273 1 2 0 S H 274 1 2 0 S H 275 1 2 0 S H Compd. No. k m n chirality R³ 276 1 2 0 S H 277 1 2 0 S H 278 1 2 0 S H 279 1 2 0 S H 280 1 2 0 S H 281 1 2 0 S H 282 1 2 0 S H 283 1 2 0 S H 284 1 2 0 S H 285 1 2 0 R H 286 1 2 0 R H Compd. No. k m n chirality R³ 287 1 2 0 R H 288 1 2 0 R H 289 1 2 0 R H 290 1 2 0 R H 291 1 2 0 R H 292 1 2 0 R H 293 1 2 0 R H 294 1 2 0 R H 295 1 2 0 R H 296 1 2 0 R H 297 1 2 0 R H Compd. No. k m n chirality R³ 298 1 2 0 R H 299 1 2 0 R H 300 1 2 0 R H 301 1 2 0 R H 302 1 2 0 R H 303 1 2 0 R H 304 1 2 0 R H 305 1 2 0 R H 306 1 2 0 R H 307 1 2 0 R H 308 1 2 0 R H Compd. No. k m n chirality R³ 309 1 2 0 R H 310 1 2 0 R H 311 1 2 0 R H 312 1 2 0 R H 313 1 2 0 R H 314 1 2 0 R H 315 1 2 0 R H 316 1 2 0 R H 317 1 2 0 R H 318 1 2 0 R H 319 1 2 0 R H Compd. No. k m n chirality R³ 320 1 2 0 R H 321 1 2 0 R H 322 1 2 0 R H 323 1 2 0 R H 324 1 2 0 R H 325 1 2 0 R H 326 1 2 0 R H 327 1 2 0 R H 328 1 2 0 R H 329 1 2 0 R H 330 0 3 1 - H Compd. No. k m n chirality R³ 331 0 3 1 - H 332 0 3 1 - H 333 0 3 1 - H 334 0 3 1 - H 335 0 3 1 - H 336 0 3 1 - H 337 0 3 1 - H 338 0 3 1 - H 339 0 3 1 R H 340 0 3 1 S H 341 0 3 1 - H Compd. No. k m n chirality R³ 342 0 3 1 - H 343 0 3 1 - H 344 0 3 1 - H 345 0 3 1 - H 346 0 3 1 - H 347 0 3 1 - H 348 0 3 1 - H 349 0 3 1 - H 350 0 3 1 - H 351 0 3 1 - H 352 0 3 1 - H Compd. No. k m n chirality R³ 353 1 2 1 - H 354 1 3 0 - H 355 1 3 0 - H 356 1 3 0 - H 357 1 3 0 - H 358 1 3 0 - H 359 1 3 0 - H 360 1 3 0 - H 361 1 3 0 - H 362 1 3 0 - H 363 1 3 0 - H Compd. No. k m n chirality R³ 364 1 3 0 - H 365 1 3 0 - H 366 1 3 0 - H 367 1 3 0 - H 368 1 3 0 - H 369 1 3 0 - H 370 1 3 0 - H 371 1 3 0 - H 372 1 3 0 - H 373 1 3 0 - H 374 1 3 0 - H Compd. No. k m n chirality R³ 375 1 3 0 - H 376 1 3 0 - H 377 1 3 0 - H 378 1 3 0 - H 379 1 3 0 - H 380 1 3 0 - H 381 1 3 0 - H 382 1 3 0 - H 383 1 3 0 - H 384 2 2 0 - H 385 2 2 0 - H Compd. No. k m n chirality R³ 386 2 2 0 - H 387 2 2 0 - H 388 2 2 0 - H 389 2 2 0 - H 390 2 2 0 - H 391 2 2 0 - H 392 2 2 0 - H 393 2 2 0 - H 394 2 2 0 - H 395 2 2 0 - H 396 2 2 0 - H Compd. No. k m n chirality R³ 397 2 2 0 - H 398 2 2 0 - H 399 2 2 0 - H 400 2 2 0 - H 401 2 2 0 - H 402 2 2 0 - H 403 2 2 0 - H 404 2 2 0 - H 405 2 2 0 - H 406 2 2 0 - H 407 2 2 0 - H Compd. No. k m n chirality R³ 408 2 2 0 - H 409 2 2 0 - H 410 2 2 0 - H 411 2 2 0 - H 412 2 2 0 - H 413 2 2 0 - H 414 2 2 0 - H 415 2 2 0 - H 416 2 2 0 - H 417 2 2 0 - H 418 2 2 0 - H Compd. No. k m n chirality R³ 419 2 2 0 - H 420 2 2 0 - H 421 2 2 0 - H 422 2 2 0 - H 423 2 2 0 - H 424 2 2 0 - H 425 2 2 0 - H 426 2 2 0 - H 427 2 2 0 - H 428 2 2 0 - H 429 2 2 0 - H Compd. No. k m n chirality R³ 430 2 2 0 - H 431 2 2 0 - H 432 2 2 0 - H 433 2 2 0 - H 434 1 3 1 - H 435 1 3 1 - H 436 1 3 1 - H 437 1 3 1 - H 438 1 3 1 - H 439 1 3 1 - H 440 1 3 1 - H Compd. No. k m n chirality R³ 441 1 3 1 - H 442 1 3 1 - H 443 1 3 1 - H 444 1 3 1 - H 445 1 3 1 - H 446 1 3 1 - H 447 1 3 1 - H 448 1 3 1 - H 449 1 3 1 - H 450 1 3 1 - H 451 1 3 1 - H Compd. No. k m n chirality R³ 452 1 3 1 - H 453 1 3 1 - H 454 1 3 1 - H 455 1 3 1 - H 456 1 3 1 - H 457 1 3 1 - H 458 2 2 1 - H 459 2 2 1 - H 460 2 2 1 - H 461 2 2 1 - H 462 2 2 1 - H Compd. No. k m n chirality R³ 463 2 2 1 - H 464 2 2 1 - H 465 2 2 1 - H 466 2 2 1 - H 467 2 2 1 - H 468 2 2 1 - H 469 2 2 1 - H 470 2 2 1 - H 471 2 2 1 - H 472 2 2 1 - H 473 2 2 1 - H Compd. No. k m n chirality R³ 474 2 2 1 - H 475 2 2 1 - H 476 2 2 1 - H 477 2 2 1 - H 478 2 2 1 - H 479 2 2 1 - H 480 2 2 1 - H 481 2 2 1 - H 482 2 2 1 - H 483 2 2 1 - H 484 2 2 1 - H Compd No. k m n chirality R³ 485 2 2 1 - H 486 2 2 1 - H 487 2 2 1 - H 488 2 2 1 - H 489 2 2 1 - H 490 2 2 1 - H 491 2 2 1 - H 492 2 2 1 - H 493 2 2 1 - H 494 2 2 1 - H 495 2 2 1 - H Compd. No. k m n chirality R³ 496 2 2 1 - H 497 2 2 1 - H 498 2 2 1 - H 499 2 2 1 - H 500 2 2 1 - H 501 2 2 1 - H 502 2 2 1 - H 503 2 2 1 - H 504 2 2 1 - H 505 2 2 1 - H 506 2 2 1 - H Compd. No. k m n chirality R³ 507 2 2 1 - H 508 2 2 1 - H 509 2 2 1 - H 510 2 2 1 - H 511 2 2 1 - H 512 2 2 1 - H 513 2 2 1 - H 514 2 2 1 - H 515 2 2 1 - H 516 2 2 1 - H 517 2 2 1 - H Compd. No. k m n chirality R³ 518 2 2 1 - H 519 2 2 1 - H 520 2 2 1 - -CH₃ 521 2 2 1 - 522 2 2 1 - 523 2 2 1 - 524 2 2 1 - 525 2 2 1 - H 526 2 2 1 - H 527 2 2 1 - H 528 2 2 1 - H Compd. No. k m n chirality R³ 529 2 2 1 - H 530 2 2 1 - H 531 2 2 1 - H 532 2 2 1 - H 533 2 2 1 - H 534 2 2 1 - H 535 2 2 1 - H 536 2 2 1 - H 537 2 2 1 - H 538 2 2 1 - H 539 2 2 1 - H Compd. No. k m n chirality R³ 540 2 2 1 - H 541 2 2 1 - H 542 2 2 1 - H 543 2 2 1 - H 544 2 2 1 - H 545 2 2 1 - H 546 2 2 1 - H 547 2 2 1 - H 548 2 2 1 - H 549 2 2 1 - H 550 2 2 1 - H Compd. No. k m n chirality R³ 551 2 2 1 - H 552 2 2 1 - H 553 2 2 1 - H 554 2 2 1 - H 555 2 2 1 - H 556 2 2 1 - H 557 2 2 1 - H 558 2 2 1 - H 559 2 2 1 - H 560 2 2 1 - H 561 2 2 1 - H Compd. No. k m n chirality R³ 562 2 2 1 - H 563 2 2 1 - H 564 2 2 1 - H 565 2 2 1 - H 566 2 2 1 - H 567 2 2 1 - H 568 2 2 1 - H 569 2 2 1 - H 570 2 2 1 - H 571 2 2 1 - H 572 2 2 1 - H Compd. No. k m n chirality R³ 573 2 2 1 - H 574 2 2 1 - H 575 2 2 1 - H 576 2 2 1 - H 577 2 2 1 - H 578 2 2 1 - H 579 2 2 1 - H 580 2 2 1 - H 581 2 2 1 - H 582 2 2 1 - H 583 2 2 1 - H Compd. No. k m n chirality R³ 584 2 2 1 - H 585 2 2 1 - H 586 2 2 1 - H 587 2 2 1 - H 588 2 2 1 - H 589 2 2 1 - H 590 2 2 1 - H 591 2 2 1 - H 592 2 2 1 - H 593 2 2 1 - H 594 2 2 1 - H Compd. No. k m n chirality R³ 595 2 2 1 - H 596 2 2 1 - H 597 2 2 1 - H 598 2 2 1 - H 599 2 2 1 - H 600 2 2 1 - H 601 2 2 1 - H 602 2 2 1 - H 603 2 2 1 - H 604 2 2 1 - H 605 2 2 1 - H Compd. No. k m n chirality R³ 606 2 2 1 - H 607 2 2 1 - H 608 2 2 1 - H 609 2 2 1 - H 610 2 2 1 - H 611 2 2 1 - H 612 2 2 1 - H 613 2 2 1 - H 614 2 2 1 - H 615 2 2 1 - H 616 2 2 1 - H Compd. No. k m n chirality R³ 617 2 2 1 - H 618 2 2 1 - H 619 2 2 1 - H 620 2 2 1 - H 621 2 2 1 - H 622 2 2 1 - H 623 2 2 1 - H 624 2 2 1 - H 625 2 2 1 - H 626 2 2 1 - H 627 2 2 1 - H Compd. No. k m n chirality R³ 628 2 2 1 - H 629 2 2 1 - H 630 2 2 1 - H 631 2 2 1 - H 632 2 2 1 - H 633 2 2 1 - H 634 2 2 1 - H 635 2 2 1 - H 636 2 2 1 - H 637 2 2 1 - H 638 2 2 1 - H Compd. No. k m n chirality R³ 639 2 2 1 - H 640 2 2 1 - H 641 2 2 1 - H 642 2 2 1 - H 643 2 2 1 - H 644 2 2 1 - H 645 2 2 1 - H 646 2 2 1 - H 647 2 2 1 - H 648 2 2 1 - H 649 2 2 1 - H Compd. No. k m n chirality R³ 650 2 2 1 - H 651 2 2 1 - H 652 2 2 1 - H 653 2 2 1 - H 654 2 2 1 - H 655 2 2 1 - H 656 2 2 1 - H 657 2 2 1 - H 658 2 2 1 - H 659 2 2 1 - H 660 2 2 1 - H Compd. No. k m n chirality R³ 661 2 2 1 - H 662 2 2 1 - H 663 2 2 1 - H 664 2 2 1 - H 665 2 2 1 - H 666 2 2 1 - H 667 2 2 1 - H 668 2 2 1 - H 669 2 2 1 - H 670 2 2 1 - H 671 2 2 1 - H Compd. No. k m n chirality R³ 672 2 2 1 - H 673 2 2 1 - H 674 2 2 1 - H 675 2 2 1 - H 676 2 2 1 - H 677 2 2 1 - H 678 2 2 1 - H 679 2 2 1 - H 680 2 2 1 - H 681 2 2 1 - H 682 2 2 1 - H Compd. No. k m n chirality R³ 683 2 2 1 - H 684 2 2 1 - H 685 2 2 1 - H 686 2 2 1 - H 687 2 2 1 - H 688 2 2 1 - H 689 2 2 1 - H 690 2 2 1 - H 691 2 2 1 - H 692 2 2 1 - H 693 2 2 1 - H Compd. No. k m n chirality R³ 694 2 2 1 - H 695 2 2 1 - H 696 2 2 1 - H 697 2 2 1 - H 698 2 2 1 - H 699 2 2 1 - H 700 2 2 1 - H 701 2 2 1 - H 702 2 2 1 - H 703 2 2 1 - H 704 2 2 1 - H Compd. No. k m n chirality R³ 705 2 2 1 - H 706 2 2 1 - H 707 2 2 1 - H 708 2 2 1 - H 709 2 2 1 - H 710 2 2 1 - H 711 2 2 1 - H 712 2 2 1 - H 713 2 2 1 - H 714 2 2 1 - H 715 2 2 1 - H Compd. No. k m n chirality R³ 716 2 2 1 - H 717 2 2 1 - H 718 2 2 1 - H 719 2 2 1 - H 720 2 2 1 - H 721 2 2 1 - H 722 2 2 1 - H 723 2 2 1 - H 724 2 2 1 - H 725 2 2 1 - H 726 2 2 1 - H Compd. No. k m n chirality R³ 727 2 2 1 - H 728 2 2 1 - H 729 2 2 1 - H 730 2 2 1 - H 731 2 2 1 - H 732 2 2 1 - H 733 2 2 1 - H 734 2 2 1 - H 735 2 2 1 - H 736 2 2 1 - H 737 2 2 1 - H Compd. No. k m n chirality R³ 738 2 2 1 - H 739 2 2 1 - H 740 2 2 1 - H 741 2 2 1 - H 742 2 2 1 - H 743 2 2 1 - H 744 2 2 1 - H 745 2 2 1 - H 746 2 2 1 - H 747 2 2 1 - H 748 2 2 1 - H Compd. No. k m n chirality R³ 749 2 2 1 - H 750 2 2 1 - H 751 2 2 1 - H 752 2 2 1 - H 753 2 2 1 - H 754 2 2 1 - H 755 2 2 1 - H 756 2 2 1 - H 757 2 2 1 - H 758 2 2 1 - H 759 2 2 1 - H Compd. No. k m n chirality R³ 760 2 2 1 - H 761 2 2 1 - H 762 2 2 1 - H 763 2 2 1 - H 764 2 2 1 - H 765 2 2 1 - H 766 2 2 1 - H 767 2 2 1 - H 768 2 2 1 - H 769 2 2 1 - H 770 2 2 1 - H Compd. No. k m n chirality R³ 771 2 2 1 - H 772 2 2 1 - H 773 2 2 1 - H 774 2 2 1 - H 775 2 2 1 - H 776 2 2 1 - H 777 2 2 1 - H 778 2 2 1 - H 779 2 2 1 - H 780 2 2 1 - H 781 2 2 1 - H Compd. No. k m n chirality R³ 782 2 2 1 - H 783 2 2 1 - H 784 2 2 1 - H 785 2 2 1 - H 786 2 2 1 - H 787 2 2 1 - H 788 2 2 1 - H 789 2 2 1 - H 790 2 2 1 - H 791 2 2 1 - H 792 2 2 1 - H Compd. No. k m n chirality R³ 793 2 2 1 - H 794 2 2 1 - H 795 2 2 1 - H 796 2 2 1 - H 797 2 2 1 - H 798 2 2 1 - H 799 2 2 1 - H 800 2 2 1 - H 801 2 2 1 - H 802 2 2 1 - H 803 2 2 1 - H Compd. No. k m n chirality R³ 804 2 2 1 - H 805 2 2 1 - H 806 2 2 1 - H 807 2 2 1 - H 808 2 2 1 - H 809 2 2 1 - H 810 2 2 1 - H 811 2 2 1 - H 812 2 2 1 - H 813 2 2 1 - H 814 2 2 1 - H Compd No. k m n chirality R³ 815 2 2 1 - H 816 2 2 1 - H 817 2 2 1 - H 818 2 2 1 - H 819 2 2 1 - H 820 2 2 1 - H 821 2 2 1 - H 822 2 2 1 - H 823 2 2 1 - H 824 2 2 1 - H 825 2 2 1 - H Compd. No. k m n chirality R³ 826 2 2 1 - H 827 2 2 1 - H 828 2 2 1 - H 829 2 2 1 - H 830 2 2 1 - H 831 2 2 1 - H 832 2 2 1 - H 833 2 2 1 - H 834 2 2 1 - H 835 2 2 1 - H 836 2 2 1 - H Compd. No. k m n chirality R³ 837 2 2 1 - H 838 2 2 1 - H 839 2 2 1 - H 840 2 2 1 - H 841 2 2 1 - H 842 2 2 1 - H 843 2 2 1 - H 844 2 2 1 - H 845 2 2 1 - H 846 2 2 1 - H 847 2 2 1 - H Compd. No. k m n chirality R³ 848 2 2 1 - H 849 2 2 1 - H 850 2 2 1 - H 851 2 2 1 - H 852 2 2 1 - H 853 2 2 1 - H 854 2 2 1 - H 855 2 2 1 - H 856 2 2 1 - H 857 2 2 1 - H 858 2 2 1 - H Compd. No. k m n chirality R³ 859 2 2 1 - H 860 2 2 1 - H 861 2 2 1 - H 862 2 2 1 - H 863 2 2 1 - H 864 2 2 1 - H 865 2 2 1 - H 866 2 2 1 - H 867 2 2 1 - H 868 2 2 1 - H 869 2 2 1 - H Compd. No. k m n chirality R³ 870 2 2 1 - H 871 2 2 1 - H 872 2 2 1 - H 873 2 2 1 - H 874 2 2 1 - H 875 2 2 1 - H 876 2 2 1 - H 877 2 2 1 - H 878 2 2 1 - H 879 2 2 1 - H 880 2 2 1 - H Compd. No. k m n chirality R³ 881 2 2 1 - H 882 2 2 1 - H 883 2 2 1 - H 884 2 2 1 - H 885 2 2 1 - H 886 2 2 1 - H 887 2 2 1 - H 888 2 2 1 - H 889 2 2 1 - H 890 2 2 1 - H 891 2 2 1 - H Compd. No. k m n chirality R³ 892 2 2 1 - H 893 2 2 1 - H 894 2 2 1 - H 895 2 2 1 - H 896 2 2 1 - H 897 2 2 1 - H 898 2 2 1 - H 899 2 2 1 - H 900 2 2 1 - H 901 2 2 1 - H 902 2 2 1 - H Compd. No. k m n chirality R³ 903 2 2 1 - H 904 2 2 1 - H 905 2 2 1 - H 906 2 2 1 - H 907 2 2 1 - H 908 2 2 1 - H 909 2 2 1 - H 910 2 2 1 - H 911 2 2 1 - H 912 2 2 1 - H 913 2 2 1 - H Compd. No. k m n chirality R³ 914 2 2 1 - H 915 2 2 1 - H 916 2 2 1 - H 917 2 2 1 - H 918 2 2 1 - H 919 2 2 1 - H 920 2 2 1 - H 921 2 2 1 - H 922 2 2 1 - H 923 2 2 1 - H 924 2 2 1 - H Compd. No. k m n chirality R³ 925 2 2 1 - H 926 2 2 1 - H 927 2 2 1 - H 928 2 2 1 - H 929 2 2 1 - H 930 2 2 1 - H 931 2 2 1 - H 932 2 2 1 - H 933 2 2 1 - H 934 2 2 1 - H 935 2 2 1 - H Compd. No. k m n chirality R³ 936 2 2 1 - H 937 2 2 1 - H 938 2 2 1 - H 939 2 2 1 - H 940 2 2 1 - H 941 2 2 1 - H 942 2 2 1 - H 943 1 4 0 - H 944 1 4 0 - H 945 1 4 0 - H 946 1 4 0 - H Compd. No. k m n chirality R³ 947 1 4 0 - H 948 1 4 0 - H 949 1 4 0 - H 950 0 4 1 - H 951 1 2 0 R H 952 1 2 0 R H 953 1 2 0 R H 954 1 2 0 R H 955 1 2 0 R H 956 1 2 0 R H 957 1 2 0 R H Compd. No. k m n chirality R³ 958 1 2 0 R H 959 1 2 0 R H 960 1 2 0 R H 961 1 2 0 R H 962 1 2 0 R H 963 1 2 0 R H 964 1 2 0 R H 965 1 2 0 R H 966 1 2 0 R H 967 1 2 0 R H 968 1 2 0 R H Compd. No. k m n chirality R³ 969 1 2 0 R H 970 1 2 0 R H 971 1 2 0 R H 972 1 2 0 R H 973 1 2 0 R H 974 1 2 0 R H 975 1 2 0 R H 976 1 2 0 R H 977 1 2 0 R H 978 1 2 0 R H 979 1 2 0 R H Compd: No. k m n chirality R³ 980 1 2 0 R H 981 1 2 0 R H 982 1 2 0 R H 983 1 2 0 R H 984 1 2 0 R H 985 1 2 0 R H 986 1 2 0 R H 987 2 2 1 - H 988 1 4 0 - H 989 1 4 0 - H 990 1 4 0 - H Compd. No. k m n chirality R³ 991 1 4 0 - H 992 1 4 0 - H 993 1 4 0 - H 994 1 4 0 - H 995 1 4 0 - H 996 1 4 0 - H 997 2 2 1 - H 998 2 2 1 - H 999 2 2 1 - H 1000 2 2 1 - H 1001 2 2 1 - H Compd. No. k m n chirality R³ 1002 2 2 1 - H 1003 2 2 1 - H 1004 2 2 1 - H 1005 2 2 1 - H 1006 2 2 1 - H 1007 2 2 1 - H 1008 2 2 1 - H 1009 2 2 1 - H 1010 2 2 1 - H 1011 2 2 1 - H 1012 2 2 1 - H Compd. No. k m n chirality R³ 1013 2 2 1 - H 1014 2 2 1 - H 1015 2 2 1 - H 1016 2 2 0 - H 1017 2 2 0 - H 1018 2 2 1 - H 1019 2 2 1 - H 1020 2 2 1 - H 1021 2 2 1 - H 1022 2 2 1 - H 1023 2 2 1 - H Compd. No. k m n chirality R³ 1024 2 2 1 - H 1025 2 2 1 - H 1026 2 2 1 - H 1027 2 2 1 - H 1028 2 2 1 - H 1029 2 2 1 - H 1030 2 2 1 - H 1031 2 2 1 - H 1032 2 2 1 - H 1033 2 2 1 - H 1034 2 2 1 - H Compd. No. k m n chirality R³ 1035 2 2 1 - H 1036 2 2 1 - H 1037 2 2 1 - H 1038 2 2 1 - H 1039 2 2 1 - H 1040 2 2 1 - H 1041 2 2 1 - H 1042 2 2 1 - H 1043 2 2 1 - H 1044 2 2 1 - H 1045 2 2 1 - H Compd. No. k m n chirality R³ 1046 2 2 1 - H 1047 2 2 1 - H 1048 2 2 1 - H 1049 2 2 1 - H 1050 2 2 1 - H 1051 2 2 1 - H 1052 2 2 1 - H 1053 2 2 1 - H 1054 2 2 1 - H 1055 2 2 1 - H 1056 2 2 1 - H Compd. No. k m n chirality R³ 1057 2 2 1 - H 1058 2 2 1 - H 1059 2 2 1 - H 1060 2 2 1 - H 1061 2 2 1 - H 1062 2 2 1 - H 1063 2 2 1 - H 1064 2 2 1 - H 1065 2 2 1 - H 1066 2 2 1 - H 1067 2 2 1 - H Compd. No. k m n chirality R³ 1068 2 2 1 - H 1069 2 2 1 - H 1070 2 2 1 - H 1071 2 2 1 - H 1072 2 2 1 - H 1073 2 2 1 - H 1074 2 2 1 - H 1075 2 2 1 - H 1076 2 2 1 - H 1077 2 2 1 - H 1078 2 2 1 - H Compd. No. k m n chirality R³ 1079 2 2 1 - H 1080 2 2 1 - H 1081 2 2 1 - H 1082 2 2 1 - H 1083 2 2 1 - H 1084 1 2 0 R H 1085 1 2 0 R H 1086 1 2 0 R H 1087 1 2 0 R H 1088 1 2 0 R H 1089 1 2 0 R H Compd. No. k m n chirality R³ 1090 1 2 0 R H 1091 1 2 0 R H 1092 1 2 0 R H 1093 1 2 0 R H 1094 1 2 0 R H 1095 1 2 0 R H 1096 1 2 0 R H 1097 1 2 0 R H 1098 1 2 0 R H 1099 1 2 0 R H 1100 1 2 0 R H Compd. No. k m n chirality R³ 1101 1 2 0 R H 1102 1 2 0 R H 1103 1 2 0 R H 1104 1 2 0 R H 1105 1 2 0 R H 1106 1 2 0 R H 1107 1 2 0 R H 1108 1 2 0 R H 1109 1 2 0 R H 1110 1 2 0 R H 1111 1 2 0 R H Compd. No. k m n chirality R³ 1112 1 2 0 R H 1113 2 2 1 - H 1114 2 2 1 - H 1115 2 2 1 - H 1116 2 2 1 - H 1117 2 2 1 - H 1118 1 2 0 R H 1119 1 2 0 R H 1120 1 2 0 R H 1121 1 2 0 R H 1122 1 2 0 R H Compd. No. k m n chirality R³ 1123 1 2 0 R H 1124 1 2 0 R H 1125 2 2 1 - H 1126 2 2 1 - H 1127 2 2 1 - H 1128 2 2 1 - H 1129 2 2 1 - H 1130 2 2 1 - H 1131 2 2 1 - H 1132 2 2 1 - H 1133 1 2 0 R H Compd. No. k m n chirality R³ 1134 1 2 0 R H 1135 1 2 0 R H 1136 1 2 0 R H 1137 1 2 0 R H 1138 1 2 0 R H 1139 1 2 0 R H 1140 1 2 0 R H 1141 1 2 0 R H 1142 1 2 0 R H 1143 1 2 0 R H 1144 1 2 0 R H Compd. No. k m n chirality R³ 1145 1 2 0 R H 1146 1 2 0 R H 1147 1 2 0 R H 1148 1 2 0 R H 1149 1 2 0 R H 1150 1 2 0 R H 1151 1 2 0 R H 1152 1 2 0 R H 1153 1 2 0 R H 1154 1 2 0 R H 1155 1 2 0 R H Compd. No. k m n chirality R³ 1156 1 2 0 R H 1157 1 2 0 R H 1158 1 2 0 R H 1159 1 2 0 R H 1160 1 2 0 R H 1161 1 2 0 R H 1162 1 2 0 R H 1163 1 2 0 R H 1164 1 2 0 R H 1165 1 2 0 R H 1166 1 2 0 R H Compd. No. k m n chirality R³ 1167 2 2 1 - H 1168 1 2 0 R H 1169 1 2 0 R H 1170 1 2 R H 1171 1 2 0 R H 1172 1 2 0 R H 1173 1 2 0 R H 1174 1 2 0 R H 1175 1 2 0 R H 1176 1 2 0 R H 1177 1 2 0 R H Compd. No. k m n chirality R³ 1178 1 2 0 R H 1179 1 2 0 R H 1180 1 2 0 R H 1181 1 2 0 R H 1182 1 2 0 R H 1183 1 2 0 R H 1184 1 2 0 R H 1185 1 2 0 R H 1186 1 2 0 R H 1187 2 2 1 - H 1188 2 2 1 - H Compd. No. k m n chirality R³ 1189 2 2 1 - H 1190 2 2 1 - H 1191 1 2 0 R H 1192 1 2 0 R H 1193 1 2 0 R H 1194 1 2 0 R H 1195 1 2 0 R H 1196 1 2 0 R H 1197 1 2 0 R H 1198 1 2 0 R H 1199 1 2 0 R H Compd. No. k m n chirality R³ 1200 1 2 0 R H 1201 1 2 0 R H 1202 1 2 0 R H 1203 1 2 0 R H 1204 1 2 0 R H 1205 1 2 0 R H 1206 1 2 0 R H 1207 1 2 0 R H 1208 1 2 0 R H 1209 1 2 0 R H 1210 1 2 0 R H Compd. No. k m n chirality R³ 1211 1 2 0 R H 1212 1 2 0 R H 1213 2 2 1 - H 1214 2 2 1 - H 1215 2 2 1 - H 1216 2 2 1 - H 1217 1 2 0 R H 1218 1 2 0 R H 1219 1 2 0 R H 1220 1 2 0 R H 1221 1 2 0 R H Compd. No. k m n chirality R³ 1222 1 2 0 R H 1223 1 2 0 R H 1224 1 2 0 R H 1225 1 2 0 R H 1226 1 2 0 R H 1227 1 2 0 R H 1228 1 2 0 R H 1229 1 2 0 R H 1230 1 2 0 R H 1231 1 2 0 R H 1232 1 2 0 R H Compd. No. k m n chirality R³ 1233 1 2 0 R H 1234 1 2 0 R H 1235 1 2 0 R H 1236 1 2 0 R H 1237 1 2 0 R H 1238 1 2 0 R H 1239 1 2 0 R H 1240 1 2 0 R H 1241 2 2 1 - H 1242 2 2 1 - H 1243 2 2 1 - H Compd. No. k m n chirality R³ 1244 2 2 1 - H 1245 2 2 1 - H 1246 2 2 1 - H 1247 2 2 1 - H 1248 2 2 1 - H 1249 1 2 0 R H 1250 1 2 0 R H 1251 1 2 0 R H 1252 1 2 0 R H 1253 1 2 0 R H 1254 1 2 0 R H Compd. No. k m n chirality R³ 1255 1 2 0 R H 1256 1 2 0 R H 1257 1 2 0 R H 1258 1 2 0 R H 1259 1 2 0 R H 1260 1 2 0 R H 1261 1 2 0 R H 1262 1 2 0 R H 1263 1 2 0 R H 1264 1 2 0 R H 1265 1 2 0 R H Compd. No. k m n chirality R³ 1266 1 2 0 R H 1267 1 2 0 R H 1268 1 2 0 R H 1269 1 2 0 R H 1270 1 2 0 R H 1271 1 2 0 R H 1272 1 2 0 R H 1273 1 2 0 R H 1274 1 2 0 R H 1275 1 2 0 R H 1276 1 2 0 R H Compd. No. k m n chirality R³ 1277 1 2 0 R H 1278 1 2 0 R H 1279 1 2 0 R H 1280 1 2 0 R H 1281 1 2 0 R H 1282 2 2 1 - H 1283 2 2 1 - H 1284 2 2 1 - H 1285 2 2 1 - H 1286 1 2 0 R H 1287 1 2 0 R H Compd. No. k m n chirality R³ 1288 1 2 0 R H 1289 1 2 0 R H 1290 1 2 0 R H 1291 1 2 0 R H 1292 1 2 0 R H 1293 1 2 0 R H 1294 1 2 0 R H 1295 1 2 0 R H 1296 1 2 0 R H 1297 1 . 2 0 R H 1298 1 2 0 R H Compd. No. k m n chirality R³ 1299 1 2 0 R H 1300 1 2 0 R H 1301 1 2 0 R H 1302 1 2 0 R H 1303 1 2 0 R H 1304 1 2 0 R H 1305 1 2 0 R H 1306 1 2 0 R H 1307 1 2 0 R H 1308 1 2 0 R H 1309 1 2 0 R H Compd. No. k m n chirality R³ 1310 1 2 0 R ^H 1311 1 2 0 R H 1312 1 2 0 R H 1313 1 2 0 R H 1314 1 2 0 R H 1315 1 2 0 R H 1316 1 2 0 R H 1317 1 2 0 R H 1318 1 2 0 R H 1319 1 2 0 R H 1320 1 2 0 R H Compd. No. k m n chirality R³ 1321 1 2 0 R H 1322 1 2 0 R H 1323 1 2 0 R H 1324 1 2 0 R H 1325 1 2 0 R H 1326 1 2 0 R H 1327 1 2 0 R H 1328 1 2 0 R H 1329 1 2 0 R H 1330 1 2 0 R H 1331 1 2 0 R H Compd. No. k m n chirality R³ 1332 1 2 0 R H 1333 1 2 0 R H 1334 1 2 0 R H 1335 1 2 0 R H 1336 1 2 0 R H 1337 1 2 0 R H 1338 1 2 0 R H 1339 1 2 0 R H 1340 1 2 0 R H 1341 1 2 0 R H 1342 2 2 1 H Compd. No. k m n chirality R³ 1343 2 2 1 - H 1344 2 2 1 - H 1345 2 2 1 - H 1346 2 2 1 - H 1347 1 2 0 R H 1348 1 2 0 R H 1349 1 2 0 R H 1350 2 2 1 - H 1351 1 2 0 R H 1352 1 2 0 R H 1353 1 2 0 R H Compd. No. k m n chirality R³ 1354 2 2 1 - H 1355 1 2 0 R H 1356 1 2 0 R H 1357 1 2 0 R H 1358 2 2 1 - H 1359 1 2 0 R H 1360 1 2 0 R H 1361 1 2 0 R H 1362 1 2 0 R H 1363 1 2 0 R H 1364 1 2 0 R H Compd. No. K m n chirality R³ 1365 1 2 0 R H 1366 1 2 0 R H 1367 1 2 0 R H 1368 1 2 0 R H 1369 1 2 0 R H 1370 1 2 0 R H 1371 1 2 0 R H 1372 1 2 0 R H 1373 1 2 0 R H 1374 1 2 0 R H 1375 1 2 0 R H Compd. No. k m n chirality R³ 1376 1 2 0 R H 1377 1 2 0 R H 1378 1 2 0 R H 1379 1 2 0 R H 1380 1 2 0 R H 1381 1 2 0 R H 1382 1 2 0 R H 1383 2 2 1 - H 1384 2 2 1 - H 1385 2 2 1 - H 1386 2 2 1 - H Compd. No. k m n chirality R³ 1387 1 2 0 R H 1388 1 2 0 R H 1389 1 2 0 R H 1390 1 2 0 R H 1391 1 2 0 R H 1392 1 2 0 R H 1393 1 2 0 R H 1394 1 2 0 R H 1395 1 2 0 R H 1396 1 2 0 R H 1397 1 2 0 R H Compd. No. k m n chirality R³ 1398 1 2 0 R H 1399 1 2 0 R H 1400 1 2 0 R H 1401 1 2 0 R H 1402 1 2 0 R H 1403 1 2 0 R H 1404 1 2 0 R H 1405 1 2 0 R H 1406 1 2 0 R H 1407 I 2 0 R H 1408 2 0 R H Compd. No. k m n chirality R³ 1409 1 2 0 R H 1410 1 2 0 R H 1411 1 2 0 R H 1412 1 2 0 R H 1413 1 2 0 R H 1414 2 2 1 - H 1415 1 2 0 R H 1416 1 2 0 R H 1417 1 2 0 R H 1418 2 2 1 - H 1419 1 2 0 R H Compd. No. k m n chirality R³ 1420 1 2 0 R H 1421 1 2 0 R H 1422 2 2 1 - H 1423 1 2 0 R H 1424 1 2 0 R H 1425 1 2 0 R H 1426 2 2 1 - H 1427 2 2 1 - H 1428 2 2 1 - H 1429 2 2 1 - H 1430 2 2 1 - H Compd. No. k m n chirality R³ 1431 2 2 1 - H 1432 2 2 1 - H 1433 2 2 1 - H 1434 2 2 1 - H 1435 2 2 1 - H 1436 2 2 1 - H 1437 2 2 1 - H 1438 2 2 1 - H 1439 2 2 1 - H 1440 2 2 1 - H 1441 2 2 1 - H Compd. No. k m n chirality R³ 1442 2 2 1 - H 1443 2 2 1 - H 1444 2 2 1 - H 1445 2 2 1 - H 1446 2 2 1 - H 1447 2 2 1 - H 1448 2 2 1 - H 1449 2 2 1 - H 1450 2 2 1 - H 1451 2 2 1 - H 1452 2 2 1 - H Compd. No. k m n chirality R³ 1453 2 2 1 - H 1454 2 2 1 - H 1455 2 2 1 - H 1456 2 2 1 - H 1457 2 2 1 - H 1458 2 2 1 - H 1459 2 2 1 - H 1460 2 2 1 - H 1461 2 2 1 - H 1462 2 2 1 - H 1463 2 1 1 - H Compd. No. k m n chirality R³ 1464 2 1 1 - H 1465 2 1 1 - H 1466 2 1 1 - H 1467 2 1 1 - H 1468 2 1 1 - H 1469 2 1 1 - H 1470 2 1 1 - H 1471 2 1 1 - H 1472 1 2 0 R H 1473 1 2 0 R H 1474 1 2 0 R H Compd. No. k m n chirality R³ 1475 1 2 0 R H 1476 1 2 0 R H 1477 1 2 0 R H 1478 1 2 0 R H 1479 1 2 0 R H 1480 1 2 0 R H 1481 1 2 0 R H 1482 1 2 0 R H 1483 1 2 0 R H 1484 1 2 0 R H 1485 1 2 0 R H Compd. No. k m n chirality R³ 1486 1 2 0 R H 1487 1 2 0 R H 1488 1 2 0 R H 1489 1 2 0 R H 1490 1 2 0 R H 1491 1 2 0 R H 1492 1 2 0 R H 1493 1 2 0 R H 1494 1 2 0 R H 1495 1 2 0 R H 1496 1 2 0 R H Compd. No. k m n chirality R³ 1497 1 2 0 R H 1498 1 2 0 R H 1499 1 2 0 R H 1500 1 2 0 R H 1501 1 2 0 R H 1502 1 2 0 R H 1503 1 2 0 R H 1504 1 2 0 R H 1505 1 2 0 R H 1506 2 1 1 - H 1507 2 1 1 - H Compd. No. k m n chirality R³ 1508 2 1 1 - H 1509 2 1 1 - H 1510 2 1 1 - H 1511 2 1 1 - H 1512 2 1 1 - H 1513 2 1 1 - H 1514 2 2 1 - H 1515 2 2 1 - H 1516 2 2 1 - H 1517 2 2 1 - H 1518 2 2 1 - H Compd. No. k m n chirality R³ 1519 2 2 1 - H 1520 1 2 0 R H 1521 1 2 0 R H 1522 1 2 0 R H 1523 1 2 0 R H 1524 1 2 0 R H 1525 1 2 0 R H 1526 1 2 0 R H 1527 1 2 0 R H 1528 1 2 0 R H 1529 1 2 0 R H Compd. No. k m n chirality R³ 1530 1 2 0 R H 1531 1 2 0 R H 1532 1 2 0 R H 1533 1 2 0 R H 1534 1 2 0 R H 1535 1 2 0 R H 1536 1 2 0 R H 1537 1 2 0 R H 1538 1 2 0 R H 1539 1 2 0 R H 1540 1 2 0 R H Compd. No. k m n chirality R³ 1541 1 2 0 R H 1542 1 2 0 R H 1543 1 2 0 R H 1544 1 2 0 R H 1545 1 2 0 R H 1546 1 2 0 R H 1547 1 2 0 R H 1548 1 2 0 R H 1549 1 2 0 R H 1550 1 2 0 R H 1551 1 2 0 R H Compd. No. k m n chirality R³ 1552 1 2 0 R H 1553 1 2 0 R H 1554 1 2 0 R H 1555 1 2 0 R H 1556 1 2 0 R H 1557 1 2 0 R H 1558 1 2 0 R H 1559 1 2 0 R H 1560 1 2 0 R H 1561 1 2 0 R H 1562 1 2 0 R H Compd. No. k m n chirality R³ 1563 1 2 0 R H 1564 1 2 0 R H 1565 1 2 0 R H 1566 1 2 0 R H 1567 1 2 0 R H 1568 1 2 0 R H 1569 1 2 0 R H 1570 2 2 1 - H 1571 2 2 1 - H 1572 2 2 1 - H 1573 2 2 1 - H Compd. No. k m n chirality R³ 1574 2 2 1 - H 1575 2 2 1 - H 1576 2 2 1 - H 1577 2 2 1 - H 1578 2 2 1 - H 1579 2 2 1 - H 1580 2 2 1 - H 1581 2 2 1 - H 1582 2 2 1 - H 1583 1 2 0 R H 1584 1 2 0 R H Compd. No. k m n chirality R³ 1585 1 2 0 R H 1586 1 2 0 R H 1587 1 2 0 R H 1588 1 2 0 R H 1589 1 2 0 R H 1590 1 2 0 R H 1591 1 2 0 R H 1592 1 2 0 R H 1593 1 2 0 R H 1594 1 2 0 R H 1595 1 2 0 R H Compd. No. k m n chirality R³ 1596 1 2 0 R H 1597 1 2 0 R H 1598 1 2 0 R H 1599 1 2 0 R H 1600 2 2 1 - H 1601 2 2 1 - H 1602 2 2 1 - H 1603 2 2 1 - H 1604 2 2 1 - H 1605 2 2 1 - H 1606 1 2 0 R H Compd. No. k m n chirality R³ 1607 1 2 0 R H 1608 1 2 0 R H 1609 2 2 1 - H 1610 2 2 1 - H 1611 2 2 1 - H 1612 2 2 1 - H 1613 2 2 1 - H 1614 1 2 0 R H 1615 2 2 1 - H 1616 2 2 1 - H 1617 2 2 1 - H Compd. No. k m n chirality R³ 1618 1 2 0 R H 1619 1 2 0 R H 1620 1 2 0 R H 1621 1 2 0 R H 1622 1 2 0 R H 1623 1 2 0 R H 1624 1 2 0 R H 1625 1 2 0 R H 1626 1 2 0 R H 1627 1 2 0 R H 1628 1 2 0 R H Compd. No. k m n chirality R³ 1629 1 2 0 R H 1630 1 2 0 R H 1631 1 2 0 R H 1632 1 2 0 R H 1633 1 2 0 R H 1634 1 2 0 R H 1635 1 2 0 R H 1636 1 2 0 R H 1637 1 2 0 R H 1638 1 2 0 R H 1639 1 2 0 R H v Compd. No. k m n chirality R³ 1640 1 2 0 R H 1641 1 2 0 R H 1642 1 2 0 R H 1643 1 2 0 R H 1644 1 2 0 R H 1645 1 2 0 R H 1646 1 2 0 R H 1647 2 2 1 - H 1648 1 2 0 R H 1649 2 2 1 - H 1650 1 2 0 R H Compd. No. k m n chirality R³ 1651 2 2 1 - H 1652 2 2 1 - H 1653 2 2 1 - H 1654 2 2 1 - H 1655 2 2 1 - H 1656 2 2 1 - H 1657 2 2 1 - H 1658 2 2 1 - H 1659 2 2 1 - H 1660 1 2 0 R H 1661 1 2 0 R H Compd. No. k m n chirality R³ 1662 1 2 0 R H 1663 1 2 0 R H 1664 2 2 1 - H 1665 2 2 1 - H 1666 2 2 1 - H 1667 2 2 1 - H 1668 2 2 1 - H 1669 2 2 1 - H 1670 2 2 1 - H 1671 2 2 1 - H 1672 2 2 1 - H Compd. No. k m n chirality R³ 1673 2 2 1 - H 1674 2 2 1 - H 1675 2 2 1 - H 1676 2 2 1 - H 1677 2 2 1 - H 1678 2 2 1 - H 1679 2 2 1 - H 1680 2 2 1 - H 1681 2 2 1 - H 1682 2 2 1 - H 1683 2 2 1 - H Compd. No. k m n chirality R³ 1684 2 2 1 - H 1685 2 2 1 - H 1686 2 2 1 - H 1687 2 2 1 - H 1688 2 2 1 - H 1689 2 2 1 - H 1690 2 2 1 - H 1691 2 2 1 - H 1692 1 2 0 R H 1693 1 2 0 R H 1694 1 2 0 R H Compd. No. k m n chirality R³ 1695 1 2 0 R H 1696 1 2 0 R H 1697 1 2 0 R H 1698 1 2 0 R H 1699 1 2 0 R H 1700 1 2 0 R H 1701 1 2 0 R H 1702 1 2 0 R H 1703 1 2 0 R H 1704 1 2 0 R H 1705 1 2 0 R H Compd. No. k m n chirality R³ 1706 1 2 0 R H 1707 1 2 0 R H 1708 1 2 0 R H 1709 1 2 0 R H 1710 1 2 0 R H 1711 1 2 0 R H 1712 1 2 0 R H 1713 1 2 0 R H 1714 1 2 0 R H 1715 1 2 0 R H 1716 1 2 0 R H Compd. No. k m n chirality R³ 1717 1 2 0 R H 1718 1 2 0 R H 1719 1 2 0 R H 1720 1 2 0 R H 1721 1 2 0 R H 1722 1 2 0 R H 1723 1 2 0 R H 1724 1 2 0 R H 1725 1 2 0 R H 1726 1 2 0 R H 1727 1 2 0 R H Compd. No. k m n chirality R³ 1728 1 2 0 R H 1729 1 2 0 R H 1730 1 2 0 R H 1731 1 2 0 R H 1732 1 2 0 R H 1733 1 2 0 R H 1734 1 2 0 R H 1735 1 2 0 R H 1736 1 2 0 R H 1737 1 2 0 R H 1738 1 2 0 R H Compd. No. k m n chirality R³ 1739 1 2 0 R H 1740 1 2 0 R H 1741 1 2 0 R H 1742 1 2 0 R H 1743 1 2 0 R H 1744 1 2 0 R H 1745 1 2 0 R H 1746 1 2 0 R H 1747 1 2 0 R H 1748 1 2 0 R H 1749 1 2 0 R H Compd. No. k m n chirality R³ 1750 1 2 0 R H 1751 1 2 0 R H 1752 1 2 0 R H 1753 1 2 0 R H 1754 1 2 0 R H 1755 1 2 0 R H 1756 1 2 0 R H 1757 1 2 0 R H 1758 1 2 0 R H 1759 1 2 0 R H 1760 1 2 0 R H Compd. No. k m n chirality R³ 1761 1 2 0 R H 1762 1 2 0 R H 1763 2 2 0 - H 1764 2 2 0 - H 1765 2 2 0 - H 1766 2 2 0 - H 1767 1 3 1 - H 1768 1 3 1 - H 1769 1 2 0 R H 1770 1 2 0 R H 1771 1 2 0 R H Compd. No. k m n chirality R³ 1772 1 2 0 R H 1773 1 2 0 R H 1774 1 2 0 R H 1775 1 2 0 R H 1776 1 2 0 R H 1777 2 2 1 - H 1778 2 2 1 - H 1779 2 2 1 - H 1780 2 2 1 - H 1781 2 2 1 - H 1782 2 2 1 - H Compd. No. k m n chirality R³ 1783 2 2 1 - H 1784 2 2 1 - H 1785 2 2 1 - H 1786 2 2 1 - H 1787 1 2 0 R H 1788 2 2 1 - H 1789 2 2 1 - H 1790 1 2 0 S H 1791 1 2 0 S H 1792 2 2 1 - H 1793 2 2 1 - H Compd. No. k m n chirality R³ 1794 2 2 1 - H 1795 2 2 1 - H 1796 2 2 1 - H 1797 2 2 1 - H 1798 2 2 1 - H 1799 2 2 1 - H 1800 2 2 1 - H 1801 2 2 1 - H 1802 1 2 0 R H 1803 1 2 0 R H 1804 2 2 1 - H Compd. No. k m n chirality R³ 1805 1 2 0 R H 1806 1 2 0 R H 1807 1 2 0 R H 1808 1 2 0 R H 1809 1 2 0 R H 1810 1 2 0 R H 1811 1 2 0 R H 1812 1 2 0 R H 1813 1 2 0 R H 1814 1 2 0 R H 1815 1 2 0 R H Compd. No. k m n chirality R³ 1816 1 2 0 R H 1817 1 2 0 R H 1818 1 2 0 R H 1819 1 2 0 R H 1820 1 2 0 R H 1821 1 2 0 R H 1822 1 2 0 R H 1823 1 2 0 R H 1824 1 2 0 R H 1825 1 2 0 R H 1826 1 2 0 R H Compd. No. k m n chirality R³ 1827 1 2 0 R H 1828 1 2 0 R H 1829 1 2 0 R H 1830 1 2 0 R H 1831 1 2 0 R H 1832 1 2 0 R H 1833 1 2 0 R H 1834 1 2 0 R H 1835 1 2 0 R H 1836 1 2 0 R H 1837 1 2 0 R H Compd. No. k m n chirality R³ 1838 1 2 0 R H 1839 1 2 0 R H 1840 1 2 0 R H 1841 1 2 0 R H 1842 1 2 0 R H 1843 1 2 0 R H 1844 1 2 0 R H 1845 1 2 0 R H 1846 1 2 0 R H 1847 1 2 0 R H 1848 1 2 0 R H Compd. No. k m n chirality R³ 1849 1 2 0 R H 1850 1 2 0 R H 1851 1 2 0 R H 1852 1 2 0 R H 1853 1 2 0 R H 1854 1 2 0 R H 1855 1 2 0 R H 1856 1 2 0 R H 1857 1 2 0 R H 1858 1 2 0 R H 1859 1 2 0 R H Compd. No. k m n chirality R³ 1860 1 2 0 R H 1861 1 2 0 R H 1862 1 2 0 R H 1863 1 2 0 R H 1864 1 2 0 R H 1865 1 2 0 R H 1866 1 2 0 R H 1867 1 2 0 R H 1868 1 2 0 R H 1869 1 2 0 R H 1870 1 2 0 R H Compd. No. k m n chirality R³ 1871 1 2 0 R H 1872 1 2 0 R H 1873 1 2 0 R H 1874 1 2 0 R H 1875 1 2 0 R H 1876 1 2 0 R H 1877 1 2 0 R H 1878 1 2 0 R H 1879 1 2 0 R H 1880 1 2 0 R H 1881 1 2 0 R H Compd. No. k m n chirality R³ 1882 1 2 0 R H 1883 1 2 0 R H 1884 1 2 0 R H 1885 1 2 0 R H 1886 1 2 0 R H 1887 1 2 0 R H 1888 1 2 0 R H 1889 1 2 0 R H 1890 1 2 0 R H 1891 1 2 0 R H 1892 1 2 0 R H Compd. No. k m n chirality R³ 1893 1 2 0 R H 1894 1 2 0 R H 1895 1 2 0 R H 1896 1 2 0 R H 1897 1 2 0 R H 1898 1 2 0 R H 1899 1 2 0 R H 1900 1 2 0 R H 1901 1 2 0 R H 1902 1 2 0 R H 1903 2 2 1 - H Compd. No. k m n chirality R³ 1904 2 2 1 - H 1905 1 2 0 R H 1906 1 2 0 R H 1907 1 2 0 R H 1908 1 2 0 R H 1909 1 2 0 R H 1910 2 2 1 - H 1911 2 2 1 - H 1912 2 2 1 - H 1913 2 2 1 - H 1914 2 2 1 - H Compd. No. k m n chirality R³ 1915 1 2 0 R H 1916 1 2 0 R H 1917 2 2 1 - H 1918 2 2 1 - H 1919 2 2 1 - H 1920 2 2 1 - H 1921 1 2 0 R H 1922 2 2 1 - H 1923 2 2 1 - H 1924 2 2 1 - H 1925 2 2 1 - H Compd. No. k m n chirality R³ 1926 2 2 1 - H 1927 2 2 1 - H 1928 2 2 1 - H 1929 2 2 1 - H 1930 2 2 1 - H 1931 2 2 1 - H 1932 2 2 1 - H 1933 2 2 1 - H 1934 2 2 1 - H 1935 2 2 1 - H 1936 2 2 1 - H Compd. No. k m n chirality _R3 1937 2 2 1 - H 1938 2 2 1 - H 1939 2 2 1 - H 1940 2 2 1 - H 1941 2 2 1 - H 1942 2 2 1 - H 1943 2 2 1 - H 1944 2 2 1 - H 1945 2 2 1 - H 1946 2 2 1 - H 1947 2 2 1 - H Compd. No. k m n chirality R³ 1948 2 2 1 - H 1949 2 2 1 - H 1950 2 2 1 - H 1951 2 2 1 - H 1952 2 2 1 - H 1953 2 2 1 - H 1954 2 2 1 - H 1955 2 2 1 - H 1956 2 2 1 - H 1957 2 2 1 - H 1958 2 2 1 - H Compd. No. k m n chirality R³ 1959 2 2 1 - H 1960 2 2 1 - H 1961 2 2 1 - H 1962 2 2 1 - H 1963 2 2 1 - H 1964 2 2 1 - H 1965 2 2 1 - H 1966 2 2 1 - H 1967 2 2 1 - H 1968 2 2 1 - H 1969 2 2 1 - H Compc No. k m n chirality R³ 1970 2 2 1 - H 1971 2 2 1 - H 1972 2 2 1 - H 1973 2 2 1 - H 1974 2 2 1 - H 1975 2 2 1 - H 1976 2 2 1 - H 1977 2 2 1 - H 1978 2 2 1 - H 1979 2 2 1 - H 1980 2 2 1 - H Compd. No. k m n chirality R³ 1981 2 2 1 - H 1982 2 2 1 - H 1983 2 2 1 - H 1984 2 2 1 - H 1985 2 2 1 - H 1986 2 2 1 - H 1987 2 2 1 - H 1988 2 2 1 - H 1989 2 2 1 - H 1990 2 2 1 - H 1991 2 2 1 - H Compd No. k m n chirality R³ 1992 2 2 1 - H 1993 2 2 1 - H 1994 2 2 1 - H 1995 2 2 1 - H 1996 2 2 1 - H 1997 2 2 1 - H 1998 2 2 1 - H 1999 2 2 1 - H 2000 2 2 1 - H 2001 2 2 1 - H 2002 2 2 1 - H Compd. No. k m n chirality R³ 2003 2 2 1 - H 2004 2 2 1 - H 2005 2 2 1 - H 2006 2 2 1 - H 2007 2 2 1 - H 2008 2 2 1 - H 2009 2 2 1 - H 2010 2 2 1 - H 2011 2 2 1 - H 2012 2 2 1 - H 2013 2 2 1 - H Compd. No. k m n chirality R³ 2014 2 2 1 - H 2015 2 2 1 - H 2016 2 2 1 - H 2017 2 2 1 - H 2018 2 2 1 - H 2019 2 2 1 - H 2020 2 2 1 - H 2021 2 2 1 - H 2022 2 2 1 - H 2023 2 2 1 - H 2024 2 2 1 - H Compd. No. k m n chirality R³ 2025 2 2 1 - H 2026 2 2 1 - H 2027 2 2 1 - H 2028 2 2 1 - H 2029 2 ,2 1 - H 2030 2 2 1 - H 2031 2 2 1 - H 2032 2 2 1 - H 2033 2 2 1 - H 2034 2 2 1 - H 2035 2 2 1 - H Compd. No. k m n chirality R³ 2036 2 2 1 - H 2037 2 2 1 - H 2038 2 2 1 - H 2039 2 2 1 - H 2040 1 2 0 R H 2041 1 2 0 R H 2042 1 2 0 R H 2043 1 2 0 R H 2044 1 2 0 R H. 2045 1 2 0 R H 2046 1 2 0 R H Compd. No. k m n c chirality R³ 2047 1 2 0 R H 2048 1 2 0 R H 2049 1 2 0 R H 2050 1 2 0 R H 2051 1 2 0 R H 2052 2 2 1 - H 2053 2 2 1 - H 2054 2 2 1 - H 2055 2 2 1 - H 2056 2 2 1 - H 2057 2 2 1 - H Compd. No. k m n chirality R³ 2058 2 2 1 - H 2059 2 2 1 - H 2060 2 2 1 - H 2061 2 2 1 - H 2062 2 2 1 - H 2063 2 2 1 - H 2064 2 2 1 - H 2065 2 2 1 - H 2066 2 2 1 - H 2067 2 2 1 - H 2068 2 2 1 - H Compd. No. k m n chirality R³ 2069 2 2 1 - H 2070 2 2 1 - H 2071 2 2 1 - H 2072 2 2 1 - H 2073 2 2 1 - H 2074 2 2 1 - H 2075 2 2 1 - H 2076 2 2 1 - H 2077 2 2 1 - H 2078 2 2 1 - H 2079 2 2 1 - H Compd. No. k m n chirality R³ 2080 2 2 1 - H 2081 2 2 1 - H 2082 2 2 1 - H 2083 1 2 0 R H 2084 1 2 0 R H 2085 1 2 0 R H 2086 1 2 0 R H 2087 1 2 0 R H 2088 1 2 0 R H 2089 1 2 0 R H 2090 1 2 0 R H Compd. No. k m n chirality R³ 2091 2 2 1 - H 2092 2 2 1 - H 2093 2 2 1 - H 2094 2 2 1 - H 2095 2 2 1 - H 2096 2 2 1 - H 2097 2 2 1 - H 2098 2 2 1 - H 2099 2 2 1 - H 2100 2 2 1 - H 2101 2 2 1 - H Compd. No. k m n chirality R³ 2102 2 2 1 - H 2103 2 2 1 - H 2104 2 2 1 - H 2105 2 2 1 - H 2106 2 2 1 - H 2107 2 2 1 - H 2108 2 2 1 - H 2109 2 2 1 - H 2110 2 2 1 - H 2111 2 2 1 - H 2112 2 2 1 - H Compd. No. k m n chirality R³ 2113 2 2 1 - H 2114 2 2 1 - H 2115 2 2 1 - H 2116 2 2 1 - H 2117 2 2 1 - H 2118 1 2 0 R H 2119 1 2 0 R H 2120 1 2 0 R H 2121 1 2 0 R H 2122 1 2 0 R H 2123 1 2 0 R H Compd. No. k m n chirality R³ 2124 1 2 0 R H 2125 1 2 0 R H 2126 1 2 0 R H 2127 1 2 0 R H 2128 1 2 0 R H 2129 1 2 0 R H 2130 2 2 1 - H 2131 2 2 1 - H 2132 1 2 0 R H 2133 1 2 0 R H 2134 1 2 0 R H Compd. No. k m n chirality R³ 2135 1 2 0 R H 2136 1 2 0 R H 2137 1 2 0 R H 2138 1 2 0 R H 2139 1 2 0 R H 2140 2 2 1 - H 2141 2 2 1 - H 2142 2 2 1 - H 2143 2 2 1 - H 2144 2 2 1 - H 2145 2 2 1 - H Compd. No. k m n chirality R³ 2146 2 2 1 - H 2147 2 2 1 - H 2148 2 2 1 - H 2149 1 2 0 R H 2150 1 2 0 R H 2151 1 2 0 R H 2152 1 2 0 R H 2153 1 2 0 R H 2154 2 2 1 - H 2155 2 2 1 - H 2156 2 2 1 - H Compd. No. k m n chirality R³ 2157 1 2 0 R H 2158 1 2 0 R H 2159 2 2 1 - H 2160 2 2 1 - H 2161 2 2 1 - H 2162 2 2 1 - H 2163 2 2 1 - H 2164 1 2 0 R H 2165 1 2 0 R H 2166 1 2 0 R H 2167 1 2 0 R H Compd. No. k m n chirality R³ 2168 1 2 0 R H 2169 1 2 0 R H 2170 1 2 0 R H 2171 1 2 0 R H 2172 1 2 0 R H 2173 1 2 0 R H 2174 1 2 0 R H 2175 1 2 0 R H 2176 1 2 0 R H 2177 1 2 0 R H 2178 1 2 0 R H Compd. No. k m n chirality R³ 2179 1 2 0 R H 2180 1 2 0 R H 2181 1 2 0 R H 2182 1 2 0 R H 2183 1 2 0 R H 2184 2 2 1 - H 2185 2 2 1 - H 2186 2 2 1 - H 2187 1 2 0 R H 2188 2 2 1 - H 2189 1 2 0 R H Compd. No. k m n chirality R³ 2190 2 2 1 - H 2191 2 2 1 - H 2192 2 2 1 - H 2193 2 2 1 - H 2194 2 2 1 - H 2195 2 2 1 - H 2196 1 2 0 R H 2197 1 2 0 R H 2198 1 2 0 R H 2199 2 2 1 - H 2200 2 2 1 - H Compd. No. k m n chirality R³ 2201 2 2 1 - H 2202 1 2 0 R H 2203 2 2 1 - H 2204 2 2 1 - H 2205 2 2 1 - H 2206 2 2 1 - H 2207 2 2 1 - H 2208 2 2 1 - H 2209 2 2 1 - H 2210 1 2 0 R H 2211 2 2 1 - H Compd. No. k m n chirality R³ 2212 2 2 1 - H 2213 2 2 1 - H 2214 2 2 1 - H 2215 1 2 0 R H 2216 1 2 0 R H 2217 1 2 0 R H 2218 1 2 0 R H 2219 1 2 0 R H 2220 1 2 0 R H 2221 1 2 0 R H 2222 1 2 0 R H Compd. No. k m n chirality R³ 2223 1 2 0 R H 2224 1 2 0 R H 2225 1 2 0 R H 2226 1 2 0 R H 2227 1 2 0 R H 2228 1 2 0 R H 2229 1 2 0 R H 2230 1 2 0 R H 2231 1 2 0 R H 2232 1 2 0 R H 2233 1 2 0 R H Compd. No. k m n chirality R³ 2234 1 2 0 R H 2235 1 2 0 R H 2236 1 2 0 R H 2237 1 2 0 R H 2238 1 2 0 R H 2239 1 2 0 R H 2240 1 2 0 R H 2241 1 2 0 R H 2242 1 2 0 R H 2243 1 2 0 R H 2244 1 2 0 R H Compd. No. k m n chirality R³ 2245 1 2 0 R H 2246 1 2 0 R H 2247 1 2 0 R H 2248 1 2 0 R H 2249 1 2 0 R H 2250 1 2 0 R H 2251 1 2 0 R H 2252 2 2 1 - H 2253 2 2 1 - H 2254 2 2 1 - H 2255 2 2 1 - H Compd. No. k m n chirality R³ 2256 2 2 1 - H 2257 2 2 1 - H 2258 1 2 0 R H 2259 1 2 0 R H 2260 1 2 0 R H 2261 1 2 0 R H 2262 1 2 0 R H 2263 1 2 0 S R 2264 1 2 0 S H 2265 1 2 0 S H 2266 1 2 0 S H Compd. No. k m n chirality R³ 2267 2 2 1 - H 2268 2 2 1 - H 2269 2 2 1 - H 2270 2 2 1 - H 2271 2 2 1 - H 2272 2 2 1 - H 2273 2 2 1 - H 2274 2 2 1 - H 2275 2 2 1 - H 2276 2 2 1 - H 2277 2 2 1 - H Compd. No. k m n chirality R³ 2278 1 2 0 R H 2279 1 2 0 R H 2280 1 2 0 S H 2281 1 2 0 S H 2282 2 2 1 - H 2283 2 2 1 - H 2284 2 2 1 - H 2285 2 2 1 - H 2286 2 2 1 - H 2287 2 2 1 - H 2288 2 2 1 - H Compd. No. k m n chirality R³ 2289 2 2 1 - H 2290 2 2 1 - H 2291 2 2 1 - H 2292 2 2 1 - H 2293 2 2 1 - H 2294 2 2 1 - H 2295 2 2 1 - H 2296 1 2 0 R H 2297 1 2 0 R H 2298 1 2 0 R H 2299 1 2 0 R H Compd. No. k m n chirality R³ 2300 1 2 0 S H 2301 1 2 0 S H 2302 1 2 0 R H 2303 1 2 0 R H 2304 1 2 0 R H 2305 1 2 0 S H 2306 1 2 0 S H 2307 1 2 0 R H 2308 1 2 0 R H 2309 1 2 0 S H 2310 1 2 0 S H Compd. No. k m n chirality R³ 2311 1 2 0 S H 2312 1 2 0 R H 2313 1 2 0 R H 2314 1 2 0 S H 2315 2 2 1 - H 2316 1 2 0 S H 2317 2 2 1 - H 2318 1 2 0 R H 2319 2 2 1 - H 2320 2 2 1 - H 2321 2 2 1 - H Compd. No. k m n chirality R³ 2322 2 2 1 - H 2323 2 2 1 - H 2324 2 2 1 - H 2325 1 2 0 R H 2326 1 2 0 R H 2327 1 2 0 R H 2328 1 2 0 S H 2329 1 2 0 S H 2330 1 2 0 S H 2331 1 2 0 S H 2332 1 2 0 R H Compd. No. k m n chirality R³ 2333 1 2 0 R H 2334 1 2 0 S H 2335 1 2 0 S H 2336 1 2 0 S H 2337 1 2 0 S H 2338 2 2 1 - H 2339 2 2 1 - H 2340 2 2 1 - H 2341 2 2 1 - H 2342 2 2 1 - H 2343 2 2 1 - H Compd. No. k m n chirality R³ 2344 2 2 1 - H 2345 2 2 1 - H 2346 2 2 1 - H 2347 1 2 0 S H 2348 1 2 0 R H 2349 1 2 0 R H 2350 1 2 0 R H 2351 1 2 0 R H 2352 2 2 1 - H 2353 2 2 1 - H 2354 1 2 0 R H Compd. No. k m n chirality R³ 2355 1 2 0 R H 2356 1 2 0 R H 2357 1 2 0 R H 2358 1 2 0 R H 2359 1 2 0 R H 2360 1 2 0 R H 2361 1 2 0 R H 2362 1 2 0 R H 2363 2 2 1 - H 2364 2 2 1 - H 2365 2 2 1 - H Compd. No. k m n chirality R³ 2366 2 2 1 - H 2367 2 2 1 - H 2368 2 2 1 - H 2369 2 2 1 - H 2370 2 2 1 - H 2371 2 2 1 - H 2372 2 2 1 - H 2373 2 2 1 - H 2374 2 2 1 - H 2375 2 2 1 - H 2376 2 2 1 - H Compd. No. k m n chirality R³ 2377 2 2 1 - H 2378 2 2 1 - H 2379 2 2 1 - H 2380 2 2 1 - H 2381 2 2 1 - H 2382 2 2 1 - H 2383 2 2 1 - H 2384 1 2 0 R H 2385 1 2 0 R H 2386 1 2 0 R H 2387 1 2 0 R H Compd. No. k m n chirality R³ 2388 1 2 0 R H 2389 1 2 0 R H 2390 1 2 0 R H 2391 1 2 0 R H 2392 1 2 0 R H 2393 1 2 0 R H 2394 2 2 1 - H 2395 2 2 1 - H 2396 2 2 1 - H 2397 2 2 1 - H 2398 2 2 1 - H Compd. No. k m n chirality R³ 2399 2 2 1 - H 2400 2 2 1 - H 2401 2 2 1 - H 2402 2 2 1 - H 2403 2 2 1 - H 2404 2 2 1 - H 2405 2 2 1 - H 2406 2 2 1 - H 2407 2 2 1 - H 2408 2 2 1 - H 2409 2 2 1 - H Compd. No. k m n chirality R³ 2410 2 2 1 - H 2411 2 2 1 - H 2412 2 2 1 - H 2413 2 2 1 - H 2414 2 2 1 - H 2415 2 2 1 - H 2416 2 2 1 - H 2417 2 2 I - H 2418 2 2 1 - H 2419 2 2 1 - H 2420 2 2 1 - H Compd. No. k m n chirality R³ 2421 2 2 1 - H 2422 1 2 0 R H 2423 1 2 0 R H 2424 1 2 0 R H 2425 1 2 0 R H 2426 1 2 0 R H 2427 1 2 0 R H 2428 1 2 0 R H