| 摘要 |
This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opioids, wherein the compounds have the general formula: <IMAGE> including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein: R is a substituted or unsubstituted unsaturated heterocyclic ring system having 5 to 6 cyclic member atoms containing at least one nitrogen atom, and is preferably selected from the group consisting of pyridinyl, pyrimidinyl, and pyrazinyl; R1 is selected from the group consisting of unsubstituted or substituted heterocyclic ring systems having 5 cyclic member atoms, lower cyclic alkyl ring systems, lower-alkyl and lower-alkoxy lower-alkyl, and is preferably selected from the group consisting of furanyl lower-alkyl, thienyl lower-alkyl, pyrrolyl lower-alkyl, lower-alkyl, lower-cycloalkyl, and lower-alkoxy lower-alkyl of 2 to 6 carbons; R2 is a cyclic ring system lower-alkyl having 5 to 6 cyclic member atoms, and is preferably selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, thienyl hydroxy lower-alkyl, pyrazoyl lower-alkyl, and (4,5-dihydro-5-oxo-1H-tetrazol-1-yl) lower-alkyl which may be substituted in the 4-position with a group selected from lower-alkyl; and R3 is selected from the group consisting of hydrogen and methyl.
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