| abstract |
The invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain, of the formulan wherein:n R 1 is hydrogen or C 1 -C 4 alkanoyl; R 2 is hydrogen, C 1 -C 4 alkyl or C 2 -C 6 alkenyl; R 3 is C 4 -C 8 cycloalkyl, C 4 -C 8 cycloalkenyl, C 1 -C 6 alkyl, C 2 -Cs alkenyl, C 1 -C 4 alkyl substituted C 4 -C 8 cycloalkyl, C 1 -C 4 alkyl substituted C 4 -C 8 cycloalkenyl or thiophene; Z isn n R 4 is hydrogen, C 1 -C 6 alkyl,n n R 5 is C 1 -C 4 alkyl orn n is 1, 2 or 3; or na pharmaceutically acceptable salt thereof. |