1-[2-(SUBSTITUTED VINYL)]-5H-2,3-BENZODIAZEPINE DERIVATIVES

摘要

This invention relates to new 1-¢2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said benzodiazepine derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The compounds according to the invention correspond to the general formula (I), (I) <IMG> wherein A and B together form a =C=N- or =CH-NH- group; R1 represents phenyl optionally carrying 2 or 3 hydroxy groups or 1 to 3 identical or different substituent(s) selected from the group consisting of halogen, trifluoromethyl, nitro, cyano, amino C1-3 alkylamino, di-(C1-3 alkyl)-amino, C1-4 alkanoylamino, C1-4 alkyl, C1-4 alkoxy, carboxy, (C1-4 alkoxy)carbonyl, C1-C4 alkoxycarbonyloxy and methylenedioxy; naphthyl optionally carrying a substituent selected from the group consisting of hydroxy, C1-4 alkoxy and C1-4 acyloxy; furyl, thienyl or indolyl; R2 stands for hydrogen or C1-4 alkyl; R3 and R4 are independently C1-4 alkoxy attached to positions 7 and 8 of the benzodiazepine ring, or R3 and R4 together form a 7,8- or 8,9-methylenedioxy group, and possess valuable central nervous activities.