IP Library Granted Patent US 8,119,681
Granted Patent B2
US 8,119,681 · App. 12/445,901 · Granted Feb 21, 2012

2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta [ƒ]indazole-5-YL]ethyl phenyl derivatives as glucocorticoid receptor ligands

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Quick Facts
Patent No.
US 8,119,681
App. No.
12/445,901
Granted
Feb 21, 2012
Kind
B2
Abstract

The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

Claims (214)

1. A compound of Formula I

or a pharmaceutically acceptable salt thereof, wherein

is an optional double bond;

A and B are independently selected from the group consisting of: H and F;

C, D and E are independently selected from the group consisting of: H, F, —CH 3 and —CF 3 ;

F is selected from the group consisting of: a bond, —C(R 1 )(R 2 )— and —C(R 1 )(R 2 )—C(R 3 )(R 4 )—;

G is selected from the group consisting of: —O—C(O)—N(R)(R), —O—C(O)—O—R, —C(O)—R, —C(O)—O—R, —C(O)—N(R)(R), —C(O)—N(R)—C(R a )(R b )—R, —C(O)—N(R)—C(R a )(R b )—C(O)—OR, —C(O)—N(R)—C(R a )(R b )—C(O)—NRR, —N(R)—C(O)—R, —N(R)—C(O)—OR, —N(R)—C(O)—N(R)(R), —N(R)—S(O) n —X, —S(O) n —N(R)(R), and —N(R)—S(O) n —N(R)(R), wherein n is 0, 1 or 2;

each R is independently selected from the group consisting of: H, haloC 1-8 alkyl, C 2-8 alkenyl, haloC 2-8 alkenyl, C 1-8 alkoxy and C 3-6 cycloalkyl-C 1-4 alkyl-, and

two R groups attached to the same nitrogen atom can be joined together with the nitrogen atom to which they are attached to form a 3- to 7-membered monocyclic ring, said ring optionally substituted with oxo and said ring further optionally substituted with 1 to 3 substituents independently selected from the group consisting of: halo, hydroxyl, C 1-4 alkyl and C 1-4 alkoxy;

X is selected from the group consisting of: H, C 1-8 alkyl, haloC 1-8 alkyl, C 2-8 alkenyl, haloC 2-8 alkenyl, C 1-8 alkoxy, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-4 alkyl-, —CH 2 —S(O) k —CH 3 , wherein k is 0, 1 or 2, aryl, substituted aryl, heteroaryl and substituted heteroaryl;

R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of: H, C 1-4 alkyl, C 1-4 haloalkyl and hydroxy, and R 1 and R 2 may be joined together with the carbon atom to which they are attached to form a 3- to 6-membered mono-cyclic ring;

R a and R b are independently selected from the group consisting of: H, C 1-4 alkyl, C 1-4 haloalkyl and hydroxy or R a and R b may be joined together with the carbon atom to which they are attached to form a 3- to 6-membered mono-cyclic ring; and

substituted aryl and substituted heteroaryl mean aryl and heteroaryl respectively, each substituted with one to three substituents independently selected from the group consisting of: halo, C 1-4 alkyl, C 1-4 haloalkyl and —CN.

2. The compound according to claim 1 wherein F is a bond and the optional double bond is not present.

3. The compound according to claim 2 wherein G is selected from the group consisting of: —C(O)—N(R)(R), —C(O)—N(R)—C(R a )(R b )—R, —C(O)—N(R)—C(R a )(R b )—C(O)—OR and —C(O)—N(R)—C(R a )(R b )—C(O)—NRR.

4. The compound according to claim 2 wherein G is —S(O) n —N(R)(R).

5. The compound according to claim 1 wherein F is —C(R 1 )(R 2 )— and the optional double bond is not present.

6. The compound according to claim 5 wherein R 1 and R 2 are H.

7. The compound according to claim 6 wherein G is —N(R)—S(O) n —X.

8. The compound according to claim 6 wherein G is —C(O)—N(R)(R).

9. The compound according to claim 1 wherein A is F.

10. A compound according to claim 1 selected from the following group:

(1) (4αS,5R)-5-(2-{2-[(3,3-diethoxyazetidin-1-yl)carbonyl]phenyl}ethyl)-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(2) N-(2,2-dimethylpropyl)-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(3) methyl 1-[(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoyl)amino]cyclopropanecarboxylate;

(4) N-ethyl-2-{2-[(4αS,5R)-5-hydroxy-4α-methyl-1-phenyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(5) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(1-methylcyclopropyl)benzamide;

(6) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-isobutylbenzamide;

(7) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-propylbenzamide;

(8) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(3,3,3-trifluoro-2-methylpropyl)benzamide;

(9) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(2-methylprop-2-en-1-yl)benzamide;

(10) N-allyl-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta indazol-5-yl]ethyl}benzamide;

(11) 2-{2-[(4αS,5R)-5-hydroxy-4α-methyl-1-phenyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(1-methylcyclopropyl)benzamide;

(12) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-isopropylbenzamide;

(13) N-ethyl-2-{2-[(4αS,5R)-1-(3-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(14) N-(cyclopropylmethyl)-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(15) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(3,3,3-trifluoro-2-methylpropyl)benzamide;

(16) 2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(1-methylcyclopropyl)benzamide;

(17) (4αS,5R)-5-{2-[2-(azetidin-1-ylcarbonyl)phenyl]ethyl}-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(18) methyl N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoyl)-2-methylalaninate;

(19) N-cyclopropyl-2-{2-[(4αS,5R)-5-hydroxy-4α-methyl-1-phenyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(20) N-ethyl-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(21) 2-{2-[(4αS,5R)-5-hydroxy-4α-methyl-1-phenyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(22) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(2-methylprop-2-en-1-yl)benzamide;

(23) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-[(2R)-3,3,3-trifluoro-2-methylpropyl]benzamide;

(24) (4αS,5R)-1-(4-fluorophenyl)-4α-methyl-5-{2-[2-(piperidin-1-ylcarbonyl)phenyl]ethyl}-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(25) (4αS,5R)-1-(4-fluorophenyl)-4α-methyl-5-{2-[2-(pyrrolidin-1-ylcarbonyl)phenyl]ethyl}-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(26) N-[(1R)-1,2-dimethylpropyl]-2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(27) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-propylbenzamide;

(28) N-allyl-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-methylbenzamide;

(29) 2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-ethylbenzamide;

(30) methyl N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoyl)-2-methylalaninate;

(31) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(2-fluoroprop-2-en-1-yl)benzamide;

(32) (4αS,5R)-1-(4-fluorophenyl)-5-[2-(2-{[(3S)-3-fluoropyrrolidin-1-yl]carbonyl}phenyl)ethyl]-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(33) N-(2,2-dimethylpropyl)-2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(34) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N-(2,2,2-trifluoroethyl)acetamide;

(35) N-allyl-2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(36) (4αS,5R)-1-(4-fluorophenyl)-5-[2-(2-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}phenyl)ethyl]-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(37) N-(tert-butyl)-2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(38) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(39) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-isobutylbenzamide;

(40) N-(tert-butyl)-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(41) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(1-methylcyclopropyl)benzamide;

(42) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-(2,2,2-trifluoroethyl)benzamide;

(43) (4αS,5R)-5-{2-[2-(azetidin-1-ylcarbonyl)-3-fluorophenyl]ethyl}-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(44) (4αS,5R)-5-(2-{2-[(3,3-difluoropiperidin-1-yl)carbonyl]phenyl}ethyl)-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(45) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-isopropylbenzamide;

(46) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(47) (4αS,5R)-5-[2-(3-fluoro-2-{[(3S)-3-fluoropyrrolidin-1-yl]carbonyl}phenyl)ethyl]-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(48) N-(2-amino-1,1-dimethyl-2-oxoethyl)-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(49) N-[2-(ethylamino)-1,1-dimethyl-2-oxoethyl]-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(50) methyl N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoyl)-D-alaninate;

(51) (4αS,5R)-1-(4-fluorophenyl)-4α-methyl-5-(2-{2-[(2-methylaziridin-1-yl)carbonyl]phenyl}ethyl)-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(52) (4αS,5R)-5-(2-{2-[(3,3-difluoropyrrolidin-1-yl)carbonyl]phenyl}ethyl)-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(53) N-[1,1-dimethyl-2-(methylamino)-2-oxoethyl]-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(54) (4αS,5R)-5-(2-{2-[(3,3-difluoropiperidin-1-yl)carbonyl]-3-fluorophenyl}ethyl)-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(55) (4αS,5R)-5-(2-{2-[(3,3-difluoropyrrolidin-1-yl)carbonyl]-3-fluorophenyl}ethyl)-1-(4-fluorophenyl)-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-ol;

(56) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)benzenesulfonamide;

(57) 2,4-difluoro-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)benzenesulfonamide;

(58) 2-fluoro-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)benzenesulfonamide;

(59) 3-cyano-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)benzenesulfonamide;

(60) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)pyridine-3-sulfonamide;

(61) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)propane-2-sulfonamide;

(62) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)ethanesulfonamide;

(63) 1,1-dichloro-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)methanesulfonamide;

(64) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)cyclopropanesulfonamide;

(65) 2,2,2-trifluoro-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)ethanesulfonamide;

(66) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)methanesulfonamide;

(67) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)cyclopropanesulfonamide;

(68) N′-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta indazol-5-yl]ethyl}benzyl)-N,N-dimethylsulfamide;

(69) 2,2,2-trifluoro-N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)ethanesulfonamide;

(70) N-[1-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)cyclopropyl]cyclopropane sulfonamide;

(71) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)furan-2-sulfonamide;

(72) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)-1-methyl-1H-imidazole-4-sulfonamide;

(73) 2-cyano-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)benzenesulfonamide;

(74) N-[(1S)-1-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethyl]cyclopropanesulfonamide;

(75) 2,2,2-trifluoro-N-[(1R)-1-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethyl]ethanesulfonamide;

(76) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)-1-(methylsulfonyl)methanesulfonamide;

(77) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)methanesulfonamide;

(78) 2,2,2-trifluoro-N-[(1S)-1-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethyl]ethanesulfonamide;

(79) N-[1-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)cyclopropyl]cyclopropanesulfonamide;

(80) 2,2,2-trifluoro-N-[(1R)-2,2,2-trifluoro-1-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethyl]ethanesulfonamide;

(81) 2,2,2-trifluoro-N-[1-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)cyclopropyl]ethanesulfonamide;

(84) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzyl)acetamide;

(85) N-ethyl-2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(86) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(87) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N-methylacetamide;

(88) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N,N-dimethylacetamide;

(89) N-cyclopropyl-2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(94) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N,N-dimethylsulfamide;

(95) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethanesulfonamide;

(96) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)cyclopropanesulfonamide;

(97) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)methanesulfonamide;

(98) 2,2,2-trifluoro-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethanesulfonamide;

(99) N-(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N,N-dimethylsulfamide;

(100) 2,2,2-trifluoro-N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethanesulfonamide;

(101) 2,2,2-trifluoro-N-(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethanesulfonamide;

(103) methyl(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)carbamate;

(104) ethyl(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)carbamate;

(105) ethyl(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)carbamate;

(106) methyl(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)carbamate;

(107) methyl(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)carbamate;

(108) ethyl(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)carbamate;

(109) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(110) 2,2,2-trifluoro-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(111) 2,2,2-trifluoro-N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(112) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(113) N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N-isopropylurea;

(114) N-ethyl-N-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)urea;

(115) N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N-isopropylurea;

(116) N-ethyl-N-(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)urea;

(117) N-ethyl-N-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)urea;

(118) N-(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N′-isopropylurea;

(119) N-(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-N-isopropylurea;

(120) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl methyl carbonate;

(121) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl ethylcarbamate;

(122) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl isopropylcarbamate;

(123) N-ethyl-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzenesulfonamide;

(124) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N,N-dimethylbenzenesulfonamide;

(125) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-N-methylbenzenesulfonamide;

(126) 2-{2-[(4αS,5R)-1-(3-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzenesulfonamide;

(127) 2-{2-[(4αS,5R)-5-hydroxy-4α-methyl-1-phenyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzenesulfonamide;

(128) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzenesulfonamide;

(129) 2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzenesulfonamide;

(133) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzonitrile;

(134) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzonitrile;

(135) 4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzonitrile;

(140) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-2-hydroxypropanamide;

(144) 2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzaldehyde;

(145) 2-{2-[(4αS,5R)-1-(4-Fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoic acid;

(146) N-Ethyl-n′-(2-(2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl)benzyl urea;

(147) N-(2-(2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta(f)indazol-5-yl]ethyl)benzyl cyclopropanecarboxamide;

(148) Ethyl(2-(2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl)benzyl carbamate;

(149) N-[1-(2-{2-[(4αS,5R)-1-(4-Fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)cyclopropyl]cyclopropanesulfonamide;

(150) N-[(1R)-1-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)ethyl]cyclopropanesulfonamide;

(151) 2-(2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl)benzyl)ethylcarbamate;

(153) Ethyl-2-(2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl)phenylcarbonate;

(154) 2-(2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl)benzaldehyde;

(155) 1-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoyl)azetidin-3-one;

(156) 1-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzoyl)azetidin-3-one;

(157) 1-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetone;

(159) 5-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(160) 2-{(E)-2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]vinyl}benzenesulfonamide;

(161) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-4-(trifluoromethyl)benzonitrile;

(162) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-4-methylbenzonitrile;

(163) 5-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzonitrile; and

(164) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-5-(trifluoromethyl)benzonitrile;

or a pharmaceutically acceptable salt of any of the above compounds.

11. A pharmaceutical composition comprising a compound according to claim 1 in combination with a pharmaceutically acceptable carrier.

12. A method for treating a glucocorticoid receptor mediated disease or condition in a mammalian patient in need of such treatment comprising administering the patient a compound according to claim 1 in an amount that is effective for treating the glucocorticoid receptor mediated disease or condition; wherein the glucocorticoid receptor mediated disease or condition is rheumatoid arthritis.

13. A method of selectively modulating the activation, repression, agonism and antagonism effects of the glucocorticoid receptor in a mammal comprising administering to the mammal a compound according to claim 1 in an amount that is effective to modulate the glucocorticoid receptor.

14. A method of partially or fully antagonizing, repressing agonizing or modulating the glucocorticoid receptor in a mammal comprising administering to the mammal an effective amount of compound according to claim 1 .

15. A compound according to claim 1 selected from the following group:

(1) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-methoxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(2) 4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(3) 2-fluoro-6-{2-[(4αS,5R)-5-hydroxy-4α-methyl-1-phenyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(4) 2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-6-fluorobenzamide;

(5) 2-chloro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(6) 5-chloro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(7) 4-chloro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(8) 2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(9) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-4-(trifluoromethyl)benzamide;

(10) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-4-methylbenzamide;

(11) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-5-(trifluoromethyl)benzamide;

(12) 2-chloro-6-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(13) 4-chloro-2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(14) 4,5-difluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(15) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-methoxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-5-(trifluoromethyl)benzamide;

(16) 5-cyano-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(17) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-5-methylbenzamide;

(18) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-6-methylbenzamide;

(19) 2,3-difluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(20) 2-{2-[(4αS,5R)-1-(4-chlorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(21) 2-{2-[(4αS,5R)-1-(4-chlorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-6-fluorobenzamide;

(22) 2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-6-methylbenzamide;

(23) 2-{2-[(4αS,5R)-1-(3-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}benzamide;

(24) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-6-(trifluoromethyl)benzamide;

(25) 2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta indazol-5-yl]ethyl}-6-methoxybenzamide;

(26) 4-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}biphenyl-3-carboxamide;

(27) 2-{2-[(4αS,5R)-1-(3-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}-6-methylbenzamide;

(28) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-2-hydroxyacetamide;

(29) 2-(4-fluoro-2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(30) 2-(2-fluoro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(31) 2-(2-{2-[(4αS,5R)-1-(3,4-difluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(32) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)propanamide;

(33) 2-(2-chloro-6-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)acetamide;

(34) 2-fluoro-2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta indazol-5-yl]ethyl}phenyl)acetamide;

(35) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-2-hydroxybutanamide;

(36) 2-cyclopropyl-2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-2-hydroxyacetamide; and

(37) 2-(2-{2-[(4αS,5R)-1-(4-fluorophenyl)-5-hydroxy-4α-methyl-1,4,4α,5,6,7-hexahydrocyclopenta[f]indazol-5-yl]ethyl}phenyl)-2-hydroxy-3-methylbutanamide;

or a pharmaceutically acceptable salt of any of the above compounds.

16. A pharmaceutical composition comprising a compound according to claim 1 in combination with a pharmaceutically acceptable carrier.

17. A compound selected from the following group:

or a pharmaceutically acceptable salt of any of the foregoing compounds.

Assignments (3)
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →
CHANGE OF NAME Recorded Jan 27, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 023852/0595 →