Diazepine derivatives and their use

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...

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Details

2602393T, 2602393B, 2602393P, A61K 3155, C07D48704, C07D51314

Patent

active

043528180

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.

REFERENCES:
patent: 4316832 (1982-02-01), Gerecke et al.

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