Imidazodiazepines

C - Chemistry – Metallurgy – 07 – D

Patent

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260/239.4

C07D 487/04 (2006.01) C07D 243/14 (2006.01) C07D 495/14 (2006.01)

Patent

CA 1184176

Abstract The novel imidazodiazepines of the general formula Image I wherein A together with the two carbon atoms denoted as .alpha. and .beta. signifies the group Image Image (a) or (b), X signifies an oxygen or sulphur atom and R1 signifies hydrogen or lower alkyl, and either R2 signifies hydrogen, trifluoromethyl, halogen, cyano or nitro and R3 signifies hydrogen or R2 signifies hydrogen and R3 signifies trifluoromethyl, halogen, cyano, nitro or lower alkyl, 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 field 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 and can be used in galenical administration forms.

393844

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