Patent ID: 7524874
Filing Date: 2009-04-28
Classification: A61P,C07D

Abstract:
1. A compound having the structure: or any pharmaceutically-acceptable salt thereof, wherein: n is independently, at each instance, 0, 1 or 2; R or R 1 is a naphthyl substituted by 0, 1, 2 or 3 substituents independently selected from R 5 ; or R 1 is R b substituted by 1, 2 or 3 substituents independently selected from R 5 ; R R R R 4 is a saturated or unsaturated 5- or 6-membered ring heterocycle containing 1, 2 or 3 atoms selected from O, N and S that is vicinally fused with a saturated or unsaturated 3- or 4-atom bridge containing 0, 1, 2 or 3 atoms selected from O, N and S with the remaining atoms being carbon, so long as the combination of O and S atoms is not greater than 2, wherein the carbon atoms of the heterocycle and bridge are substituted by 0, 1, 2 or 3 substituents independently selected from R e , C 1-4 haloalkyl, halo, nitro, cyano, oxo, —OR f , —S(═O) n R e , —OC 1-4 haloalkyl, —OC 2-6 alkylNR a R f , —OC 2-6 alkylOR f , —OC 1-6 alkylC(═O)OR e , —NR a R f , —NR a C 1-4 haloalkyl, —NR a C 2-6 alkylNR a R f , —NR a C 2-6 alkylOR f , —C(═O)R e , —C(═O)OR e , —OC(═O)R e , —C(═O)NR a R f and —NR a C(═O)R e ; and unsaturated carbon atoms may be additionally substituted by ═O; and any available nitrogen atoms in the heterocycle and bridge are substituted by H, —C 1-6 alkylOR f , R e , —C 1-6 alkylNR a R f , —C 1-3 alkylC(═O)OR e , —C 1-3 alkylC(═O)NR a R f , —C 1-3 alkylOC(═O)R e , —C 1-3 alkylNR a C(═O)R e , —C(═O)R c or —C 1-3 alkylR c ; or R 4 is naphthyl substituted by 1, 2 or 3 substituents independently selected from C 1-4 haloalkyl, halo, nitro, cyano, —S(═O) n R e , —OC 1-4 haloalkyl, —OC 2-6 alkylNR a R f , —OC 2-6 alkylOR f , —OC 1-6 alkylC(═O)OR e , —NR a C 1-4 haloalkyl, —NR a C 2-6 alkylNR a R f , —NR a C 2-6 alkylOR f , —C(═O)R e , —C(═O)OR e , —OC(═O)R e and —C(═O)NR a R f ; but in no instance is R 4 3,5-ditrifluoromethylphenyl, 3-trifluoromethyl-4-fluorophenyl, -phenyl-(C 1-8 alkyl), -phenyl-O—(C 1-6 alkyl), -phenyl-NR a R a or -phenyl-N(R a )C(═O)(C 1-8 alkyl); R R R R R A) R 10 is independently, at each instance, selected from H, C 1-8 alkyl, C 1-4 haloalkyl, halo, cyano, nitro, —C(═O)(C 1-8 alkyl), —C(═O)O(C 1-8 alkyl), —C(═O)NR a R a , —C(═NR a )NR a R a , —OR a , —OC(═O)(C 1-8 alkyl), —OC(═O)NR a R a , —OC(═O)N(R a )S(═O) 2 (C 1-8 alkyl), —OC 2-6 alkyNR a R a , —OC 2-6 alkylOR a , —SR a , —S(═O)(C 1-8 alkyl), —S(═O) 2 (C 1-8 alkyl), —S(═O) 2 NR a R a , —S(═O) 2 N(R a )C(═O)(C 1-8 alkyl), —S(═O) 2 N(R a )C(═O)O(C 1-8 alkyl), —S(═O) 2 N(R a )C(═O)NR a R a , —NR a R a , —N(R a )C(═O)(C 1-8 alkyl), —N(R a )C(═O)O(C 1-8 alkyl), —N(R a )C(═O)NR a R a , —N(R a )C(═NR a )NR a R a , —N(R a )S(═O) 2 (C 1-8 alkyl), —N(R a )S(═O) 2 NR a R a , —NR a C 2-6 alkylNR a R a and —NR a C 2-6 alkylOR a ; or R 10 is a saturated or unsaturated 5-, 6- or 7-membered monocyclic or 6-, 7-, 8-, 9-, 10- or 11-membered bicyclic ring containing 1, 2 or 3 atoms selected from N, O and S, wherein the ring is fused with 0 or 1 benzo groups and 0 or 1 saturated or unsaturated 5-, 6- or 7-membered heterocyclic ring containing 1, 2 or 3 atoms selected from N, O and S; wherein the carbon atoms of the ring are substituted by 0, 1 or 2 oxo groups, wherein the ring is substituted by 0, 1, 2 or 3 groups selected from C 1-8 alkyl, C 1-4 haloalkyl, halo, cyano, nitro, —C(═O)(C 1-8 alkyl), —C(═O)O(C 1-8 alkyl), —C(═O)NR a R a , —C(═NR a )NR a R a , —OR a , —OC(═O)(C 1-8 alkyl), —OC(═O)NR a R a , —OC(═O)N(R a )S(═O) 2 (C 1-8 alkyl), —OC 2-6 alkylNR a R a , —OC 2-6 alkylOR a , —SR a , —S(═O)(C 1-8 alkyl), —S(═O) 2 (C 1-8 alkyl), —S(═O) 2 NR a R a , —S(═O) 2 N(R a )C(═O)(C 1-8 alkyl), —S(═O) 2 N(R a )C(═O)O(C 1-8 alkyl), —S(═O) 2 N(R a )C(═O)NR a R a , —NR a R a , —N(R a )C(═O)(C 1-8 alkyl), —N(R a )C(═O)O(C 1-8 alkyl), —N(R a )C(═O)NR a R a , —N(R a )C(═NR a )NR a R a , —N(R a )S(═O) 2 (C 1-8 alkyl), —N(R a )S(═O) 2 NR a R a , —NR a C 2-6 alkylNR a R a and —NR a C 2-6 alkylOR a ; or R 10 is C 1-4 alkyl substituted by 0, 1, 2 or 3 groups selected from C 1-4 haloalkyl, halo, cyano, nitro, —C(═O)(C 1-8 alkyl), —C(═O)O(C 1-8 alkyl), —C(═O)NR a R a , —C(═NR a )NR a R a , —OR a , —OC(═O)(C 1-8 alkyl), —OC(═O)NR a R a , —OC(═O)N(R a )S(═O) 2 (C 1-8 alkyl), —OC 2-6 alkylNR a R a , —OC 2-6 alkylOR a , —SR a , —S(═O)(C 1-8 alkyl), —S(═O) 2 (C 1-8 alkyl), —S(═O) 2 NR a R a , —S(═O) 2 N(R a )C(═O)(C 1-8 alkyl), —S(═O) 2 N(R a )C(═O)O(C 1-8 alkyl), —S(═O) 2 N(R a )C(═O)NR a R a , —NR a R a , —N(R a )C(═O)(C 1-8 alkyl), —N(R a )C(═O)O(C 1-8 alkyl), —N(R a )C(═O)NR a R a , —N(R a )C(═NR a )NR a R a , —N(R a )S(═O) 2 (C 1-8 alkyl), —N(R a )S(═O) 2 NR a R a , —NR a C 2-6 alkylNR a R a and —NR a C 2-6 alkylOR a ; and R B) R 10 and R 11 together are a saturated or unsaturated 3- or 4-atom bridge containing 1, 2 or 3 atoms selected from O, N and S with the remaining atoms being carbon, so long as the combination of O and S atoms is not greater than 2, wherein the bridge is substituted by 0, 1 or 2 substituents selected from ═O, R e , halo, cyano, nitro, —C(═O)R e , —C(═O)OR e , —C(═O)NR a R f ,—C(═NR a )NR a R f , —OR f , —OC(═O)R e , —OC(═O)NR a R f , —OC(═O)N(R f )S(═O) 2 R e , —OC 2-6 alkylNR a R f , —OC 2-6 alkylOR f , —SR f , —S(═O)R e , —S(═O) 2 R e , —S(═O) 2 NR a R f , —S(═O) 2 N(R f )C(═O)R e , —S(═O) 2 N(R f )C(═O)OR e , —S(═O) 2 N(R f )C(═O)NR a R f , —NR a R f , —N(R f )C(═O)R e , —N(R f )C(═O)OR e , —N(R f )C(═O)NR a R f , —N(R f )C(═NR a )NR a R f , —N(R f )S(═O) 2 R e , —N(R f )S(═O) 2 NR a R f , —NR f C 2-6 alkylNR a R f and —NR f C 2-6 alkylOR f ; and R R R R R R R R R R