Patent · US Expired

Mono- and bisquaternary ammonium derivatives of 2.beta.,16.beta.-di-amino-5.alpha.-androstane derivatives and pharmaceutical preparations containing same

US4447425A · kind A · utility

8Cited by
3References
18Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJun 9, 1982
Grant dateMay 8, 1984
Priority date
Expiry dateJun 9, 2002

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07J71/001
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

This invention relates to novel mono- and bisquaternary ammonium derivatives of 5.alpha.-androstanes having the formula: ##STR1## wherein: R.sub.1 =H or alkyl (1-4 C); PA1 R.sub.2 and R.sub.3 each are alkyl (1-4 C) or form together with the N-atom a piperidino, pyrrolidino or morpholino group; PA1 R.sub.4 =O or H(.beta.OR.sub.5) and PA1 R.sub.5 =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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.