1-Substd. benzodiazepine derivs. - with cns depressant activity

摘要

Cpds. of formula (where R1 = H, halogen, NO2 or CF3, R2 = pyridyl, cyclohexenyl or R7, R8-substd. phenyl, where R7 and R8 are H, halogen, lower alkyl or CF3, R3 is H, lower alkyl, aryl or aralkyl, R4 = OH, lower alkoxy or acyloxy, R5 = H OH or acyloxy, or R4 + R5 is -O-CR9R10-O-, -O-CHR9-CHR10-O-, R11-substd. o-phenylenedioxy or -O-C(B)-O-, where R9 and R10 are H, lower alkyl, lower alkenyl, aryl, aralkyl, cycloalkyl or cycloalkylalkyl, R11 = H, halogen or lower alkyl, B is O or S, R6 = H, CN, acyloxy, alkoxycarbonyl, NR12R13, CONR12R13 or (A)p-R14 where R12 and R13 are H or lower alkyl, or NR12R13 is an opt. substd. 5- or 6-membered heterocycle opt. contg. other heteroatoms, R14 = H, acyl, lower alkyl, lower alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, polyhaloalkyl or cyanoalkyl, A is O, S, SO, or SO2, p = 0 or 1, 1 = 0 or 1, m = 0-3, n = 1-4) are transquillisers, sedatives, muscle relaxants, spasmolytics and hypnotics.