Patent · US Expired

Diazepine derivatives and their use

US4352818A · kind A · utility

14Cited by
1References
12Claims
0Family size

Assignee

Inventors

Key dates

Filing dateFeb 18, 1982
Grant dateOct 5, 1982
Priority date
Expiry dateFeb 18, 2002

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY02A50/30
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

There is presented imidazodiazepines of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is the group ##STR2## R.sup.1 is hydrogen, lower alkyl, lower alkoxymethyl, halogen or nitro, R.sup.4 is hydrogen, trifluoromethyl or halogen, R.sup.5 is hydrogen, fluoromethyl, halogen or lower alkyl and X is an oxygen or sulphur atom, and either R.sup.2 is hydrogen and R.sup.3 is lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the (S)-- or (R,S)-- configuration, and their pharmaceutically acceptable acid addition salts. The compounds antagonize the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. Thus they can be used, for example, as antidotes in the case of intoxications with 1,4-benzodiazepines which have tranquillizing activity. Also presented are various methods to produce the imidazodiazepine derivatives.

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