C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/239.4
C07D 487/14 (2006.01) A61K 31/55 (2006.01) C07D 487/04 (2006.01) C07D 487/22 (2006.01) C07D 495/04 (2006.01) C07D 495/14 (2006.01) C07D 495/22 (2006.01)
Patent
CA 1173441
RAN 4008/322 Abstract The novel imidazodiazepines of the general formula Image I wherein A together with the two carbon atoms denoted as a and signifies the group Image Image (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 iso- propyl 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.
392415
Hunkeler Walter
Kyburz Emilio
Gowling Lafleur Henderson Llp
Hoffmann-La Roche Limited
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