Imidazodiazepine derivatives

Details Imidazodiazepine derivatives Imidazodiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/239.4

C07D 487/00 (2006.01) C07D 243/14 (2006.01) C07D 265/26 (2006.01) C07D 333/42 (2006.01) C07D 487/04 (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 1143728

RAN 4008/306K Abstract Imidazodiazepine derivatives of the general formula Image I wherein A together with the two carbon atoms denoted as .alpha. and .beta. represents one of the groups Image and Image (a) (b) (c) and the dotted line represents the double bond present in groups (a) and (b), D represents ?C=0 or ?C=S, R1 represents cyano, lower alkanoyl or a group of the formula -COOR4, R4 represents methyl, ethyl, isopropyl or 2-hydroxyethyl, R5 represents hydrogen, trifluoromethyl or halogen and R6 represents hydrogen, trifluoro- methyl, halogen or lower alkyl and either R2 represents hydrogen and R3 represents hydro- gen or lower alkyl or R2 and R3 together represent trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are novel and are suitable for antagonising the central- -depressant, muscle relaxant, ataxic, blood pressure- -lowering and respiratory-depressant properties of 1,4- -benzodiazepines which have tranquillising activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzo- diazepines which have tranquillising activity par- ticipates, for shortening an 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 present imidazodiazepine derivatives can be manufactured according to various methods starting from partially novel starting materials and can be formulated into galenical administration forms.

360028

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