| 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, nitro or a group of the formula -COOR4,R2 is hydrogen, trifluoromethyl or halogen, R3 is hydrogen, trifluoromethyl, halogen or lower alkyl, R4 is methyl, ethyl or isopropyl and X is 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. 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 therapy, for example, of schistosomicidally-active 1,4-benzodiazepines. Also provided are methods to produce the above compounds. |
