DERIVATIVES OF 1-[2-(SUBSTITUTED VINYL)]-5H-2,3-BENZODIAZEPINE, METHOD OF THEIR SYNTHESIS, INTERMEDIATE COMPOUND, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING, METHOD OF TREATMENT OF PATIENTS WITH CENTRAL NERVOUS SYSTEM DISEASE

organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of 1-[2-(substituted vinyl)]-5H-2,3-benzodiazepine, method of their synthesis, pharmaceutical composition, method of its preparing and method of treatment of patients with diseases of the central nervous system. Compounds have the general formula (I) where A and B in common form the group of the formula =C=N or =CH-NH-; R1 means phenyl that can has from 2 to 3 hydroxyl groups or from 1 to 3 similar or different substituents taken among the group including halogen atom, trifluoromethyl-, nitro-, cyano-, amino-group, (C1-3alkyl)amino-, C1-4alkanoylamino-, C1-4alkyl, C1-4-alkoxy-group, carboxyl, (C1-4-alkoxy)-carbonyl, methylenedioxyl-group, naphthyl that can has substituent as hydroxyl, furyl, thienyl or indolyl; R2 means hydrogen atom or C1-4alkyl; R3 and R4 each means C1-4alkoxy-group bound at position 7 or 8 of benzodiazepine ring, or R3 and R4 in common form 7,8- or 8,9-methylenedioxyl group, and their pharmaceutically acceptable acid addition salts. Compounds show significant activity with respect to the central nervous system. EFFECT: new compounds indicated above, improved method of synthesis, valuable medicinal properties. 9 cl, 10 tbl, 98 ex