C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
260/20
C07J 43/00 (2006.01) C07J 1/00 (2006.01) C07J 13/00 (2006.01) C07J 21/00 (2006.01) C07J 71/00 (2006.01)
Patent
CA 1186681
Title: NOVEL MONO- AND BISQUATAERNARY AMMONIUM DERIVATIVES OF 2.beta., 16.beta.-DI-AMINO-5.alpha.-ANDROSTANE DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING SAME. ABSTRACT This invention relates to novel mono- and bisquaternary ammonium derivatives of 5.alpha.-androstanes having the formula: Image 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.
405039
Carlyle Ian C.
Savage David S.
Sleigh Thomas
Akzo N.v.
Fetherstonhaugh & Co.
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