1-(Substd. methyl)triazolo(4,3-a)(1,4)benzodiazepines - CNS depressants prepd. by reacting a hydrazide with 2-aminobenzodiazepines

摘要

Triazolo (4,3-a)benzodiazepines of formula (I) are new and are prepd by reacting cpds. (II) and (III) R2.A.CONH-NH2 opt. followed by conversion to 5-oxide or by acylation (when R2=OH); (R1=H or 1-3C alkyl; R2=OH, 1-6C alkoxy, mono- or diaryl-methoxy, 5-7 membered 2-oxacycloalkoxy or F; A=1-3C alkylene; rings B and C may be substd by F, Cl, Br, CF3 or 1-6C alkyl or alkoxy; X=NH2 opt. mono or di-substd). (I) are CNS depressants e.g. anticonvulsants and antiaggressive agents, and also inhibit the somatic reflux. They are useful e.g. in treatment of epilepsy, the daily dose being 0.01-2 mg/kg pref orally or rectally.