| 摘要 |
<p>The novel imidazodiazepines of the general formula < IMG > wherein R1 signifies methyl, ethyl or isopropyl, one of R4 and R5 signifies hydrogen and the other signifies nitro or cyano, and either R2 signifies hydrogen and R3 signifies hydrogen or lower alkyl or R2 and R3 together signify dimethylene, trimethylene or propenylene and the carbon atom denoted as .gamma. has the (S)- or (R,S)configuration, and X signifies an oxygen or sulphur atom, and their pharmaceutically acceptable acid addition salts 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, for example as antidotes in the case of intoxications with 1,4-benzo-diazepines 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 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.</p> |
