| 摘要 |
X-6864 This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines of the formula (I): (I) wherein: R1 is hydrogen or C1-C4 alkanoyl; R2 is hydrogen, C1-C4 alkyl or C2-C6 alkenyl; R3 is C4-C8 cycloalkyl, C4-C8 cycloalkenyl, C1-C6 alkyl, C2-C6 alkenyl, C1-C4 alkyl substituted C4-C8 cycloalkyl, C1-C4 alkyl substituted C4-C8 cycloalkenyl or thiophene; Z is , -?- or a bond; R4 is hydrogen, C1-C6 alkyl, or ; R5 is C1-C4 alkyl or ; n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof. These compounds are opioid antagonists which are capable of blocking the m.mu. or kappa receptors in the brain. |
