NOVEL MONO- AND BISQUATERNARY AMMONIUM DERIVATIVES OF 2BETA, 16BETA-DIAMINO-5ALPHA-ANDROSTANE DERIVATIVES

摘要

This invention relates to novel mono- and bisquaternary ammonium derivatives of 5 alpha -androstanes having the formula: wherein: R1=H or alkyl (1-4 C); R2 and R3 each are alkyl (1-4 C) or form together with the N-atom a piperidino, pyrrolidino or morpholino group; R4=O or H( beta OR5) and R5=H or acyl derived from an organic carboxylic acid having 1-18, preferably 1-6 carbon atoms; the quaternarizing group being a saturated or unsaturated aliphatic hydrocarbon group having 1-4 carbon atoms the anion being halide; and acid addition salts of the monoquaternary compounds; and to pharmaceutical preparations containing one or more of said androstane compounds as active constituent. The compounds according to the invention are non-depolarizing neuromuscular blocking agents having very quick onset and recovery characteristics, a short duration of action and a favorable dissociation between muscle blocking and vagal blocking effects.