C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/239.4
C07D 487/04 (2006.01) A61K 31/55 (2006.01) C07D 243/14 (2006.01) C07D 487/14 (2006.01) C07D 495/04 (2006.01) C07D 495/14 (2006.01) C07D 495/22 (2006.01) C07D 498/04 (2006.01)
Patent
CA 1174673
RAN 4008/324 Abstract The novel imidazodiazepines of the general formula Image wherein A together with the two carbon atoms denoted at .alpha. and .beta. signifies the group Image Image (a) or (b) R1 signifies hydrogen, lower alkyl, lower alkoxymethyl, halogen or nitro, R4 signifies hydrogen, trifluoromethyl or halogen, R5 signifies hydrogen, trifluoromethyl, halogen or lower alkyl and X signifies an oxygen or sulphur atom, and either R2 signifies hydrogen and R3 signifies lower alkyl or R2 and R3 together signify trimethylene or propenylene and the carbon atom denoted as y has the (S)- or (R,S)-configuration, and their pharmaceutically acceptable acid addition salts antagonize the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity, and can be used, 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 which are 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.
392373
Hunkeler Walter
Kyburz Emilio
Gowling Lafleur Henderson Llp
Hoffmann-La Roche Limited
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