摘要 |
<p>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; 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 2aCOE - position; R3 is one of H, OH, OCON(CH3)2, COOCH3, or COOC2H5.</p> |