1-[2'-(Substituted)vinyl]-5H-2,3-benzodiazepine derivatives, process and intermediates for their preparation, medicaments containing them and use

Disclosed are 1-[2'-(substituted)vinyl]-5H-2,3- benzodiazepine derivatives of general formula (I), wherein A and B together are the group of formula =C=N- or =CH-NH-, R1 is phenyl with 1 to 3 identical or different substituents selected from the group consisting of halogen, trifluoromethyl or cyano, R2 is H and R3 and R4 together are 7,8- or 8,9-methylenedioxy group, as well as their addition salts with acids and stereoisomers and their mixtures. Disclosed are also process for their preparation, benzopyrilium percholate derivatives, which are intermediates for their preparation, the medicaments containing 1-[2'-(substituted) vinyl]-5H-2,3-benzodiazepine derivatives, their use for the preparation of medicaments, particularly for treatment of CNS disorders. 1-[4'-(fluoro)styryl]-4-[methyl]-7,8-[methylenedioxy]-5H-2,3- benzodiazepine is particularly effective compound as well as its addition salts with acids and stereoisomers and their mixtures. Opísané sú 1-[2'-(substituovaný)vinyl]-5H-2,3- benzodiazepínové deriváty všeobecného vzorca (I), kde A a B spolu tvoria skupinu vzorca =C=N- alebo =CH-NH-, R1 predstavuje fenyl nesúci 1 až 3 zhodné alebo rozdielne substituenty vybrané zo skupiny pozostávajúcej z halogénu, trifluórmetylu alebo kyano, R2 predstavuje vodík a R3 a R4 spolu tvoria 7,8- alebo 8,9-metyléndioxyskupinu, ako aj ich adičné soli s kyselinami a stereoizoméry a ich zmesi. Opísaný je tiež spôsob ich prípravy, 2-benzopyrílium perchlorátové deriváty, ktoré sú medziproduktmi na ich prípravu, liečivá obsahujúce 1-[2'-(substituovaný)vinyl]- 5H-2,3-benzodiazepínové deriváty, ich použitie na prípravu liečiv, najmä na ošetrenie porúch centrálneho nervového systému. Obzvlášť účinnou zlúčeninou je 1-[4'-(fluór)styryl]-4-[metyl]- 7,8-[metyléndioxy]-5H-2,3-benzodiazepín, ako aj jeho adičné soli s kyselinami a stereoizoméry a ich zmesi.ŕ