5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them

摘要

The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) <IMAGE> (I) wherein R1 stands for hydrogen, halogen, trifluoromethyl or a nitro group; R2 stands for hydrogen or alkyl having 1 to 6 carbon atoms; R3 represents a group conventionally attached to the -CH(NH2)-COOH group of the known optically active or racemic alpha -amino-acids, preferably an optionally substituted lower alkyl group; R4 is hydrogen, chlorocarbonyl or carbamoyl; and X is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R4 stands for hydrogen R3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation. The new compounds show valuable enzyme inducing activity and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.