ES363527A1 - Novel Benzazocine Derivatives, the Preparation thereof and Compositions Containing the same - Google Patents

Abstract

Novel benzazocine derivatives of the general formula wherein A is a hydrogen or halogen atom or an alkyl, acyl, haloalkyl or cyano radical, B is a hydrogen atom or an alkyl radical, X is a methylene radical or a sulphur atom R and R1 are each a hydrogen atom or an alkyl or alkenyl radical, or, together with the nitrogen atom to which they are attached, form a heterocyclic radical, containing at most 7 ring members, selected from alkyleneimino and oxa-, thiaaza-, N-alkyl-aza-, N-alkoxy-aza-, N-hydroxyalkyl-aza-, N-alkoxyalkyl-aza- and N-arylaza-alkyleneimino radicals, R11 is a C 1-5 alkylene radical and m is 0 or 1, and pharmaceutically acceptable acid addition salts thereof are prepared by reaction of a benzazocine of the general formula with a compound of the general formula YCO(R11) m Y, wherein Y is a halogen atom, and reaction of the resulting N-substituted benzazocine of the general formula with ammonia or an amine of the general formula HNRR1, followed optionally by salification of the product with a pharmaceutically acceptable acid. Pharmaceutical compositions having antiinflammatory, anti-depressant, anti-spasmodic, analgesic and anti-histaminic properties comprise, as active ingredient, a benzazocine derivative of the first general formula above or a pharmaceutically acceptable acid addition salt thereof, in admixture with a solid or liquid pharmaceutical excipient, and may be administered orally or parenterally.