| 摘要 |
<p>RAN 4008/322 The novel imidazodiazepines of the general formula I wherein A together with the two carbon atoms denoted as a and signifies the group (a) or (b) R1 signifies hydrogen, lower alkyl, lower alkoxymethyl, halogen, nitro or a group of the formula -COOR4, R2 signifies hydrogen, trifluoromethyl or halogen, R3 signifies hydrogen, trifluoromethyl, halogen or lower alkyl, R4 signifies methyl, ethyl or isopropyl and X signifies an oxygen or sulphur atom and the carbon atom denoted as .gamma. has the (S)- or (R,S) -configuration, 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-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 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> |
