Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...
Patent
1980-04-25
1981-09-08
Schwartz, Richard A.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Parasitic organism or component thereof or substance...
546 97, A61K 31445, C07D40506
Patent
active
042884446
ABSTRACT:
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.
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Akkerman Antony M.
van Bakel Hermanus C. C. K.
van Breevoort-Uurbanus Henriette G.
ACF Chemiefarma N.V.
Schwartz Richard A.
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