Tricyclic benzodiazepines having anticonvulsant - muscle relaxant and sedative activity

摘要

Tricyclic benzodiazepines having anticonvulsant, muscle relaxant and sedative activity. M3A. Are new compounds of formula (I):- where R6 is H, alkyl, acyl; R1=H, halogen, NO2, CF3, alkyl, alkylthio, alkoxy; R2 = H, alkyl, cycloalkyl, hydroxyalkyl; R3=H, alkyl; Y=-CH2CH2- or -CH2CH2CH2- opt. substd. by R4 which is alkyl or CH2X, X being Cl, Br, alkoxyalkyl, dialkylamino; R5=H, alkyl, pyridyl, phenyl, opt. substd. by hal, NO2, CF3 or alkyl. Preferred Z=O; R'=7-Cl; R2=H, Me, -CH2CH2OH; R3=H; Y= -CH2CH2- opt. substd. by CH3, CH2Cl; R5= phenyl or 0-fluorophenyl. Used in unit dosage of 1-100 mg orally and 1-50 mg parenterally. The ED50 of 10-chloro-11n-(2-fluorophenyl)-2,3,5, 11b-tetrahydrooxazolo 3,2-d 1,4 benzodiazepin-6-(7H)-one in metrazol-induced convulsions in mice is 0.075 mg/kg. In the foot-shock test in mice 1 mg/kg gave 100% blocking of fighting response. Preparation by.