6-aryl-s-triazolo-(4,3-a)-pyrido-(2,3-f)-1,4-diazepines

Details 6-aryl-s-triazolo-(4,3-a)-pyrido-(2,3-f)-1,4-diazepines 6-aryl-s-triazolo-(4,3-a)-pyrido-(2,3-f)-1,4-diazepines

C - Chemistry, Metallurgy

07

D

260/239.1

C07D 471/14 (2006.01) C07D 213/61 (2006.01) C07D 213/64 (2006.01) C07D 213/70 (2006.01) C07D 471/04 (2006.01)

Patent

CA 1076111

ABSTRACT OF THE DISCLOSURE The present invention provides 6-aryl-s-triazolo- (4,3-a)-pyrido-(2,3-f)-(1,4)-diazepines of the formula Image I where R1 is a hydrogen atom, a halogen atom, an alkyl group with 1-6 C atoms, a mercapto group, an alkylmercapto group with 1-6 C atoms, an amino group, a monoalkylamino group with 1-6 C atoms or a dialkylamino group with alkyl residues from 1-6 C atoms, which alkyl residues together with the N atom to whiah they are attached may also form a pyrollidine ring, R2 is a hydrogen atom, an alkyl group with 1-6 C atoms, a hydroxy group, an acyloxy group with 2-6 C atoms, or an alkoxy group with 1-6 C atoms, R3 is hydrogen, an alkyl group with 1-6 C atoms, an alkoxy group with 1-6 C atoms or a halogen atom, the grouping A-B-represents the group -N=N-, -CO-NR4, C(SR5)=N-, -C(OR5)=N-, or -CR6=N-, R4 is hydrogen, an alkenyl group with 2 to 6 C atoms, an alkinyl group with 2-6 C atoms, a hydroxyalkyl group with 1-6 C atoms, a keto- alkyl group with 1-6 C atoms, a cyanoalky group with 1-6 C atoms or an alkyl group with 1-6 C atoms which may also contain an alkoxy group with 1-6 C atoms or a dialkylamino group with alkyl residues from 1-6 C atoms, R5 is hydrogen or an alkyl group with 1-6 C atoms, R6 is hydrogen or an alkyl group with 1-6 C atoms or a haloalkyl group with 1-6 C atoms and -Y-Z-stands for the groupings ?C=N-, ?C=N(?O)-, ?CH-NH- or ?CH-N(OH)-, and where R6 is other than an alkyl group when R1 is chlorine, R2 is hydrogen, R3 is hydrogen or a halogen and Y-Z is the grouping ?C=N- its optical isomers and its pharmaceutically acceptable salts. The compounds of formula I are pharmacodynamically active. In particular, they possess anxiolytic, spasmolytic and sedative properties. Some are also antiphlogistic and protect against ulcers.

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