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AssigneeACF Chemiefarma N.V.
InventorsAntony M. Akkerman, Hermanus C. C. K. van Bakel, Henriette G. Van Breevoort-Uurbanus
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The invention is concerned with certain new 6,7-benzomorphan derivatives having pharmacological, in particular analgesic and/or morphine-antagonistic properties, of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl or heteroaryl group; R.sup.2 is a hydrogen or halogen atom, or a hydroxy, alkoxy or acyloxy group; R.sup.3 is an alkyl or alkenyl group; R.sup.4 is a hydrogen atom or a hydroxy, alkoxy or acyloxy group; and R.sup.5 is an alkyl group or, when R.sup.2 is hydrogen in a trans-position to R.sup.3, R.sup.5 is a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, or a substituted or unsubstituted phenylalkyl, heteroarylalkyl or heterocycloalkylalkyl group; optical isomers and pharmaceutically acceptable salts thereof. The preferred compound is the .alpha.-isomer of 2,5-dimethyl-2'-hydroxy-9-phenyl-6,7-benzomorphan, in particular its (+)-enantiomer. These compounds are prepared by total synthesis and are not derived from opium alkaloids.
A benzomorphan compound of the formula ##STR80## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is unsubstituted phenyl or phenyl substituted by a substituent selected from the group consisting of halogen, lower alkyl, trifluoromethyl, hydroxy, lower alkoxy, di(lower) alkylamino, and piperidino;
A benzomorphan compound of the formula ##STR81## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is unsubstituted phenyl or phenyl substituted by a substituent selected from the group consisting of halogen, methyl, trifluoromethyl, hydroxy, methoxy, dimethylamino, and piperidino;
Dependencies are inferred from the claim text.