MONO- AND BISQUATERNARY AMMONIUM DERIVATIVES OF 2.beta., 16.beta.-DI-AMINO-5-.alpha.-ANDROSTANE DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING SAME

摘要

Title: NOVEL MONO- AND BISQUATAERNARY AMMONIUM DERIVATIVES OF 2.beta., 16.beta.-DI-AMINO-5.alpha.-ANDROSTANE DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING SAME. This invention relates to novel mono- and bisquaternary ammonium derivatives of 5.alpha.-androstanes having the formula: < IMG > 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 = 0 or H(.beta.OR5) and R5 = H or acyl derived from an organic carboxylic acid having 1-18, preferably 1-6 carbon atoms; the quaternarising 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-depolarising neuromuscular blocking agents having very quick onset and recovery characteristics, a short duration of action and a favourable dissociation between muscle blocking and vagal blocking effects.