Anxiolytic agents with reduced sedative and ataxic effects

Details Anxiolytic agents with reduced sedative and ataxic effects Anxiolytic agents with reduced sedative and ataxic effects

C - Chemistry, Metallurgy

07

D

C07D 243/14 (2006.01) A61K 31/5513 (2006.01) A61P 25/22 (2006.01) C07D 243/12 (2006.01) C07D 243/18 (2006.01) C07D 243/20 (2006.01) C07D 243/24 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 487/06 (2006.01) C07D 495/04 (2006.01) C07D 495/14 (2006.01) C07D 498/04 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2480869

Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects. Compounds of e.g. the following formula (I) are disclosed, wherein Y and Z are taken together with the two intervening carbon atoms to form a ring selected from phenyl and thienyl, which ring is substituted at the C(7) position with at least the substituent -C.ident.C-R where R is H, Si (CH3)3, t-butyl, isopropyl, methyl, or cyclopropyl; R1 is one of H, CH3, C2H4N (C2H5)2, CH2CF3, CH2CCH, or an alkyl cyclopropyl; R2is a substituted or unsubstituted at least partially unsaturated 5 or 6 membered cyclic or heterocyclic ring, wherein if substituted the substituent is one or more of F, Cl, Br, or NO2 at the 2~ - position; R3 is one of H, OH, OCON(CH3)2, COOCH3, or COOC2H5.

L'invention concerne des dérivés de benzodiazépine oralement actifs et leurs sels. Ces composés et leurs sels présentent une activité anxiolytique et anticonvulsive à effets sédatifs/hypnotiques/myorelaxants/ataxiques réduits.

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