Imidazo-benzodiazepines 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, 2602393P, 2602393D, 2602393B, A61K 3155, C07D48704

Patent

active

043528155

ABSTRACT:
There is provided imidazodiazepines of the formula ##STR1## wherein R.sup.1 is methyl, ethyl or isopropyl, one of R.sup.4 and R.sup.5 is hydrogen and the other is nitro or cyano, and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are dimethylene, trimethylene or propenylene and the carbon atom denoted as .gamma. has the (S)-- or (R,S)-- configuration, and X is an oxygen or sulphur atom,
and their pharmaceutically acceptable acid addition salts. The compounds are useful in the antagonization of the central-depressant muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines. Also provided are methods for making the compounds.

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

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