Benzodiazepine derivs. of formula (I) and their lower alkoxycarbonyl, lower alkanoyl, higher alkanoyl, adamantoyl, carbamoyl, mono- or di-lower alkyl carbamoyl, (3-7 C cycloalkyl)-carbonyl and H-Q-CO- derivs., 2-N-oxides, 2-lower alkyl or 2-HQ- lower alkyl quat. ammonium derivs. and their salts are new. (R1,R3 and R4 are H or lower alkyl; R2 is H, lower alkyl, higher alkyl, lower alkenyl, lower alkynyl, 3-7 C cycloalkyl or 3-7 C cycloalkenyl, or lower alkyl substd. by cycloalkyl, OH, NH2, mono- or di-lower alkylamino, COOH, lower alkoxycarbonyl, carabamoyl, mono or di-lower alkyl carbamoyl, HQ-, lower alkanoyl or HQCO; Q is 1,2-phenylene opt. substd. by 1 or 2 lower alkyl, lower alkoxy, lower alkylthio, halogen or CF3 gps.; CnH2n is lower alkylene separating the two N atoms by 2 or 3 C; R5 is H, lower alkyl, COOH, lower alkoxycarbonyl or lower alkyl substd. by OH, NH2 or mono- or di-lower alkylamino). (I) have analgesic, antihistamine, antiserotoninergic and esp. antidepressant activity. Daily dose is 0.01-100 (esp. 0:1-0.5) mg/kg, orally or parenterally, for treating depression, migraine, allergic states, etc. (I) are also intermediates for other cpds., esp. drugs.
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