| 摘要 |
There is presented imidazodiazepines of the formula <IMAGE> I wherein A together with the two carbon atoms denoted as alpha and beta is the group <IMAGE> R1 is hydrogen, lower alkyl, lower alkoxymethyl, halogen or nitro, R4 is hydrogen, trifluoromethyl or halogen, R5 is hydrogen, fluoromethyl, halogen or lower alkyl and X is an oxygen or sulphur atom, and either R2 is hydrogen and R3 is lower alkyl or R2 and R3 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. |
