Triazolobenzodiazepine derivs - with anticonvulsant, cns depressant and muscle-relaxant activity

摘要

Title cpds. of formula (I): (where R1 is H or 1-3C alkyl; R2 is 1-4C alkyl or R2--R2 is a satd. divalent 2-5C aliphatic hydrocarbon residue, and rings A and B can be substd. by F, Cl, Br, CF3, NO2 or 1-6C alkyl or alkoxy) and their 5-oxides and acid addn. salts, can be used as tranquillisers, sedatives, muscle relaxants and anti-epileptics; the 5-oxides are also of use as inters. for further pharmacologically active cpds. Cpds. (I) are e.g. prepd. by (a) reacting a 2-X-3-R1-5-phenyl-3H-1,4-benzodiazepine (where X is SH, lower alkoxy or alkylthio opt. activated by a substituent, or opt. mono- or disubstd. amino) with (R2O)2CHCONHNH2. The 5-oxides are obtd. by oxidn.