IMIDAZODIAZEPINES

摘要

RAN 4008/324 The novel imidazodiazepines of the general formula wherein A together with the two carbon atoms denoted at .alpha. and .beta. signifies the group (a) or (b) R1 signifies hydrogen, lower alkyl, lower alkoxymethyl, halogen or nitro, R4 signifies hydrogen, trifluoromethyl or halogen, R5 signifies hydrogen, trifluoromethyl, halogen or lower alkyl and X signifies an oxygen or sulphur atom, and either R2 signifies hydrogen and R3 signifies lower alkyl or R2 and R3 together signify trimethylene or propenylene and the carbon atom denoted as y has the (S)or (R,S)-configuration, and their pharmaceutically acceptable acid addition salts antagonize the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity, and can be used, for example, as antidotes in the case of intoxications with 1,4-benzodiazepines which have tranquillizing activity, for shortening anaesthesia induced by such 1,4-benzodiazepines etc; they can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines which are used in other fields of indication, for example of schistosomicidally -active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)- -1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one. The compounds of formula I above can be manufactured according to various methods starting from partly novel starting materials and can be used in galenical administration forms.