ANXIOLYTIC AGENTS WITH REDUCED SEDATIVE AND ATAXIC EFFECTS

摘要

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≡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; R2 is 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.