US2011190344A1PendingUtilityA1
Benzimidazole modulators of vr1
Est. expiryMay 3, 2026(expired)· nominal 20-yr term from priority
Inventors:Mark R. PlayerScott L. DaxWilliam H. ParsonsMichael BrandtRaul CalvoSharmila PatelJian LiuWing S. CheungMichele C. JetterYu-Kai LeeMark A. YoungmanWenxi PanKenneth M. WellsDerek Beauchamp
A61P 43/00A61P 9/12A61P 29/00A61P 25/22A61P 25/04A61P 25/00A61P 11/00A61P 13/10A61P 1/04C07D 403/06C07D 235/08A61K 31/4184C07D 401/06
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Claims
Abstract
The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
Claims
exact text as granted — not AI-modified1 . A compound of Formula (I):
and a salt, stereoisomer, tautomer or ester thereof, wherein:
the dashed lines between positions 1, 2 and 3 in Formula (I) indicate the positions of a tautomeric double bond,
wherein when a double bond is formed between positions 1 and 2, then R 3b is present, and
wherein, when a double bond is formed between positions 2 and 3, then R 3a is present;
p is 1 or 2;
q is 0 or 1;
r is 0, 1, 2 or 3;
L is C 1-3 alkyl;
A 1 is selected from the group consisting of phenyl, biphenyl, naphthyl, pyridinyl, quinolinyl and indole;
R 1 is each selected from the group consisting of hydroxy, cyano, halogen, formyl, carboxy, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylcarbonyl, C 1-6 alkoxycarbonyl, C 1-6 alkylthio, C 1-6 alkylsulfonyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-4 alkyl, C 3-8 cycloalkyl-C 1-4 alkoxy, C 3-8 cycloalkyl-oxy, amino, (C 1-6 alkyl) 1-2 amino, (C 3-8 cycloalkyl) 1-2 amino, (C 3-8 cycloalkyl-C 1-4 alkyl) 1-2 -amino, aminocarbonyl, (C 1-6 alkyl) 1-2 -aminocarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkoxycarbonylamino, aminocarbonylamino, (C 1-6 alkyl) 1-2 -aminocarbonylamino, C 1-6 alkylsulfonylamino, C 1-6 alkylsulfinylamino, aminosulfonyl, (C 1-4 alkyl) 1-2 -aminosulfonyl, aminosulfonylamino and (C 1-6 alkyl) 1-2 -aminosulfonylamino,
wherein alkyl is optionally substituted with C 1-8 alkoxy, amino, (C 1-4 alkyl) 1-2 amino, C 1-6 alkylcarbonylamino, C 1-6 alkoxycarbonylamino, aminocarbonylamino, (C 1-6 alkyl) 1-2 -aminocarbonylamino, C 1-6 alkylsulfonylamino, aminosulfonylamino, (C 1-6 alkyl) 1-2 aminosulfonylamino hydroxy and phenyl,
wherein phenyl is optionally substituted with one, two or three substituents independently selected from the group consisting of halogen, cyano, nitro, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio and C 1-6 alkylsulfonyl, and
wherein, each instance of alkyl and alkoxy is optionally perfluorinated;
R 2 is selected from the group consisting of halogen, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylsulfonyl, nitro, amino, (C 1-4 alkyl) 1-2 amino and cyano,
wherein each instance of alkyl and alkoxy is optionally perfluorinated;
R 3a and R 3b are each selected from the group consisting of hydrogen and optionally perfluorinated C 1-4 alkyl; and
R 4 is each selected from the group consisting of halogen, nitro, cyano, carboxy, C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy-C 1-6 alkyl, C 1-6 alkylcarbonyl, C 1-6 alkylthio, haloC 1-6 alkylthio, C 1-6 alkylsulfonyl, haloC 1-6 alkylsulfonyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-4 alkyl, C 3-8 cycloalkyl-C 1-4 alkoxy, C 3-8 cycloalkyl-oxy, amino, (C 1-6 alkyl) 1-2 amino, (C 3-8 cycloalkyl) 1-2 amino, (C 3-8 cycloalkyl-C 1-4 alkyl) 1-2 amino, aminocarbonyl, (C 1-6 alkyl) 1-2 aminocarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkoxycarbonylamino, aminocarbonylamino, (C 1-6 alkyl) 1-2 aminocarbonylamino, C 1-6 alkylsulfonylamino, haloC 1-6 alkylsulfonylamino, C 1-6 alkylsulfinylamino, aminosulfonyl and (C 1-4 alkyl) 1-2 aminosulfonyl,
wherein each instance of alkyl is optionally substituted with one, two or three substituents independently selected from the group consisting of C 1-8 alkoxy, amino, (C 1-4 alkyl) 1-2 amino, C 1-6 alkylcarbonylamino, C 1-6 alkoxycarbonylamino, aminocarbonylamino, (C 1-6 alkyl) 1-2 aminocarbonylamino, C 1-6 alkylsulfonylamino, oxo and hydroxy, and
wherein, each instance of alkyl and alkoxy is optionally perfluorinated.
2 . The compound of claim 1 , wherein q is 0.
3 . The compound of claim 1 , wherein A 1 is selected from the group consisting of phenyl, biphenyl, naphthyl, quinolinyl and indole.
4 . The compound of claim 1 , wherein
R 1 is each selected from the group consisting of hydroxy, halogen, formyl, C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkylcarbonyl, C 1-6 alkoxycarbonyl, C 1-6 alkylthio, C 1-6 alkylsulfonyl, amino, aminocarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkoxycarbonylamino, C 1-6 alkylsulfonylamino, aminosulfonyl, (C 1-4 alkyl) 1-2 aminosulfonyl and aminosulfonylamino, wherein alkyl is optionally substituted with amino, (C 1-4 alkyl) 1-2 amino, aminosulfonylamino or hydroxy, and wherein, alkyl is optionally perfluorinated.
5 . The compound of claim 1 , wherein R 2 is selected from the group consisting of halogen and C 1-4 alkyl, wherein alkyl is optionally perfluorinated.
6 . The compound of claim 1 , wherein R 3a and R 3b are each selected from the group consisting of hydrogen and C 1-4 alkyl.
7 . The compound of claim 1 , wherein R 4 is each selected from the group consisting of halogen, carboxy, C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkylcarbonyl, haloC 1-6 alkylthio, C 1-6 alkylsulfonyl, haloC 1-6 alkylsulfonyl, (C 1-6 alkyl) 1-2 amino, (C 1-6 alkyl) 1-2 aminocarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkylsulfonylamino and haloC 1-6 alkylsulfonylamino, wherein alkyl and alkoxy are optionally perfluorinated.
8 . The compound of claim 1 , wherein
p is 1 or 2; q is 0; r is 0, 1, 2 or 3; L is C 1-3 alkyl; A 1 is selected from the group consisting of phenyl, biphenyl, naphthyl, quinolinyl and indole; R 1 is each selected from the group consisting of hydroxy, halogen, formyl, C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkylcarbonyl, C 1-6 alkoxycarbonyl, C 1-6 alkylthio, C 1-6 alkylsulfonyl, amino, aminocarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkoxycarbonylamino, C 1-6 alkylsulfonylamino, aminosulfonyl, (C 1-4 alkyl) 1-2 aminosulfonyl and aminosulfonylamino, wherein alkyl is optionally substituted with amino, (C 1-4 alkyl) 1-2 amino, aminosulfonylamino or hydroxy, and wherein, alkyl is optionally perfluorinated; R 2 is selected from the group consisting of halogen and C 1-4 alkyl, wherein alkyl is optionally perfluorinated; R 3a and R 3b are each selected from the group consisting of hydrogen and C 1-4 alkyl; and R 4 is each selected from the group consisting of halogen, carboxy, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylcarbonyl, haloC 1-6 alkylthio, C 1-6 alkylsulfonyl, haloC 1-6 alkylsulfonyl, (C 1-6 alkyl) 1-2 amino, (C 1-6 alkyl) 1-2 aminocarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkylsulfonylamino and haloC 1-6 alkylsulfonylamino, wherein alkyl and alkoxy are optionally perfluorinated.
9 . A compound selected from the group consisting of:
2-{2-[3-(4-tert-butyl-phenyl)-propyl]-1H-benzimidazol-5-yl}-phenol, 2-[3-(4-tert-butyl-phenyl)-propyl]-5-m-tolyl-1H-benzimidazole, N-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-{2-[2-(4-tert-butyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenol, 3-{2-[2-(4-tert-butyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenol, 4-{2-[2-(4-tert-butyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenol, 1-(2-{2-[2-(4-trifluoromethanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, 2-{2-[2-(4-trifluoromethoxy-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-trifluoromethanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethoxy-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 1-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, N-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, 2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, N-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-C,C,C-trifluoro-methanesulfonamide, 1-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, N-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, 2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 1-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanone, 1-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanol, N-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 2-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-benzenesulfonamide, C,C,C-trifluoro-N-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 1-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanone, 1-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanol, N-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 2-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-benzenesulfonamide, C,C,C-trifluoro-N-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 1-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanone, 1-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanol, N-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 2-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-benzenesulfonamide, C,C,C-trifluoro-N-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 1-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)ethanol, N-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, 2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, N-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-C,C,C-trifluoro-methanesulfonamide, 1-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, N-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, 2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, N-(4-{2-[5-(2-acetyl-phenyl)-1H-benzimidazol-2-yl]-ethyl}-phenyl)-methanesulfonamide, N-[4-(2-{5-[2-(1-hydroxy-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, N-(2-{2-[2-(4-methanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, N-[4-(2-{5-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, 2-{2-[2-(4-methanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-methanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, N-(4-{2-[5-(2-acetyl-phenyl)-1H-benzimidazol-2-yl]-ethyl}-phenyl)-C,C,C-trifluoro-methanesulfonamide, C,C,C-trifluoro-N-[4-(2-{5-[2-(1-hydroxy-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, C,C,C-trifluoro-N-(4-{2-[5-(2-methanesulfonylamino-phenyl)-1H-benzimidazol-2-yl]-ethyl}-phenyl)-methanesulfonamide, C,C,C-trifluoro-N-[4-(2-{5-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, 2-{2-[2-(4-trifluoromethanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-{2-[2-(4-fluoro-3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,3,4-trifluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,4,5-trifluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,6-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,5-bis-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-chloro-2-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-chloro-3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3-trifluoromethoxy-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,4-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3,4-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,3-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,5-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3,5-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-(2-phenethyl-1H-benzimidazol-5-yl)-benzenesulfonamide, N,N-dimethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, N-methyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-fluoro-2-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2-fluoro-3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2-fluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-fluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3-fluoro-5-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-isopropyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 4-trifluoromethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, (E)-5-trifluoromethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 5-trifluoromethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, (E)-1-[4-(2-{5-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-1H-benzimidazol-2-yl}-vinyl)-phenyl]-ethanone, N-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-acetamide, 2-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, 2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzylamine.
10 . The compound of claim 9 , wherein the compound is selected from the group consisting of:
2-{2-[3-(4-tert-butyl-phenyl)-propyl]-1H-benzimidazol-5-yl}-phenol, 2-[3-(4-tert-butyl-phenyl)-propyl]-5-m-tolyl-1H-benzimidazole, N-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-{2-[2-(4-tert-butyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenol, 3-{2-[2-(4-tert-butyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenol, 4-{2-[2-(4-tert-butyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenol, 1-(2-{2-[2-(4-trifluoromethanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, 2-{2-[2-(4-trifluoromethoxy-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-trifluoromethanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, N-methyl-2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-fluoro-3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,3,4-trifluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,4,5-trifluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,6-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,5-bis-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-chloro-2-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-chloro-3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3-trifluoromethoxy-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,4-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3,4-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,3-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2,5-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3,5-difluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-(2-phenethyl-1H-benzimidazol-5-yl)-benzenesulfonamide, N,N-dimethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, N-methyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-fluoro-2-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2-fluoro-3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(2-fluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-fluoro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(3-fluoro-5-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 2-{2-[2-(4-isopropyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 4-trifluoromethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, 5-trifluoromethyl-2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, (E)-1-[4-(2-{5-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-1H-benzimidazol-2-yl}-vinyl)-phenyl]-ethanone, (E)-N-isopropyl-4-{2-[5-(2-methylsulfamoyl-phenyl)-1H-benzimidazol-2-yl]-vinyl}-benzamide, N-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-acetamide, 2-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, (E)-2-[2-(2-styryl-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzylamine, 2-[2-(2-phenylethynyl-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-phenylethynyl-1H-benzimidazol-5-yl)-benzenesulfonamide,
11 . The compound of claim 9 , wherein the compound is selected from the group consisting of:
C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethoxy-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 1-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, N-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, N-(2-{2-[2-(4-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-C,C,C-trifluoro-methanesulfonamide, 1-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, N-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, C,C,C-trifluoro-N-(2-{2-[2-(4-methanesulfonyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 1-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanone, 1-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanol, N-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 2-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-benzenesulfonamide, C,C,C-trifluoro-N-[2-(2-{2-[4-(2,2,2-trifluoro-1-trifluoromethyl-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 1-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanone, 1-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanol, N-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 2-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)phenyl]-ethyl}-1H-benzimidazol-5-yl)-benzenesulfonamide, C,C,C-trifluoro-N-[2-(2-{2-[4-(2,2,2-trifluoro-ethoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 1-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanone, 1-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-ethanol, N-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 2-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-propan-2-ol, 2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-benzenesulfonamide, C,C,C-trifluoro-N-[2-(2-{2-[4-(2,2,3,3,3-pentafluoro-propoxy)-phenyl]-ethyl}-1H-benzimidazol-5-yl)-phenyl]-methanesulfonamide, 1-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)ethanol, N-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, 2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, N-(2-{2-[2-(3-chloro-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-C,C,C-trifluoro-methanesulfonamide, 1-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanone, 1-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-ethanol, N-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, 2-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol, C,C,C-trifluoro-N-(2-{2-[2-(3-trifluoromethyl-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, N-(4-{2-[5-(2-acetyl-phenyl)-1H-benzimidazol-2-yl]-ethyl}-phenyl)-methanesulfonamide, N-[4-(2-{5-[2-(1-hydroxy-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, N-(2-{2-[2-(4-methanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, N-[4-(2-{5-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, 2-{2-[2-(4-methanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-methanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide, N-(4-{2-[5-(2-acetyl-phenyl)-1H-benzimidazol-2-yl]-ethyl}-phenyl)-C,C,C-trifluoro-methanesulfonamide, C,C,C-trifluoro-N-[4-(2-{5-[2-(1-hydroxy-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, C,C,C-trifluoro-N-(4-{2-[5-(2-methanesulfonylamino-phenyl)-1H-benzimidazol-2-yl]-ethyl}-phenyl)-methanesulfonamide, C,C,C-trifluoro-N-[4-(2-{5-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-1H-benzimidazol-2-yl}-ethyl)-phenyl]-methanesulfonamide, 2-{2-[2-(4-trifluoromethanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-benzenesulfonamide, C,C,C-trifluoro-N-(2-{2-[2-(4-trifluoromethanesulfonylamino-phenyl)-ethyl]-1H-benzimidazol-5-yl}-phenyl)-methanesulfonamide.
12 . A salt of the compound of claim 1 selected from the group consisting of acetate, adipate, benzenesulfonate, benzoate, bicarbonate, bisulfate, bitartrate, borate, bromide, calcium, camsylate (or camphorsulphonate), carbonate, chloride, choline, clavulanate, citrate, dihydrochloride, disodium, edetate, fumarate, gluconate, glutamate, hydrabamine, hydrobromine, hydrochloride, iodide, isothionate, lactate, malate, maleate, mandelate, mesylate, nitrate, oleate, pamoate, palmitate, phosphate/diphosphate, salicylate, sodium, stearate, sulfate, succinate, tartrate, tromethane, tosylate, trichloroacetate and trifluoroacetate.
13 . The salt of claim 12 , wherein the salt is selected from the group consisting of disodium, hydrochloride and sodium.
14 . A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutically acceptable carriers, excipients or diluents.
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