| 摘要 |
A class of epoxymorphinan derivatives is described having use as antitussive agents. Compounds of this class are character- ized in having antitussive potency but lacking narcotic side effects. Compounds of interest are those of the formula wherein R1 is selected from hydroxy, alkylcarboxyl, alkoxy and phenoxy; wherein R2 is selected from hydrido, alkyl, acyl and phenyl; wherein R3 is selected from <IMGS> wherein each of R5, R6, R7 and R8 is independently selected from hydrido, alkyl, phenyl and phenalkyl, wherein R4 is selected from hydrido, alkyl, cyano, cycloalkyl, cycloalkylalkyl, cycloalkyl- carbonyl, allyl, phenyl, benzyl, phenethyl and phenpropyl; and wherein any of the foregoing R1, R2, R3, R4, R5, R6, R7 and R8 substituents having a substitutable position may be substituted with one or more groups selected from hydroxy, halo, alkyl and cycloalkyl; or a pharmaceutically-acceptable salt thereof.
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