DERIVATIVES OF 1-[2-(SUBSTITUTED VINYL)]-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF PREPARING PHARMACEUTICAL COMPOSITION AND METHOD OF SUPPRESSION OF CONVULSIONS

organic chemistry, pharmacy. SUBSTANCE: invention describes the novel derivatives of 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine of the general formula (I) where R means hydrogen atom or C1-4-alkanoyl; R1 means phenyl that can has from 1 to 3 similar or different substituents taken a...

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Hauptverfasser: VAGO PAL, KHAMORI TAMASH, KHORVAT KATALIN, SHOMOD' D'ERD', BERZHEN'I PAL', BAKON'I ANNA, MATE D'ERD'NE, MORAVCHIK IMRE, BOTKA PETER, KHORVAT EHDIT, ZOL'OMI GABOR, REITER JOZHEF, D'ERT'JAN ISHTVAN, GIGLER GABOR, KERESHI ENE, SENTKUTI EHSTER, ANDRASHI FERENTS, BIRKASH FAIGL'NE EHRZHEBET
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Sprache:eng
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Zusammenfassung:organic chemistry, pharmacy. SUBSTANCE: invention describes the novel derivatives of 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine of the general formula (I) where R means hydrogen atom or C1-4-alkanoyl; R1 means phenyl that can has from 1 to 3 similar or different substituents taken among the group involving halogen atom, nitro-, amino-, di-(C1-4-alkyl)-amino-, C1-4-alkanoylamino-grpup, C1-4-alkyl, C1-4-alkoxy-group, methylenedioxyl and hydroxyl or naphthyl; R2 means hydrogen atom or C1-4-alkyl; R3 and R4 mean independently C1-4-alkyl; or R3 and R4 in common form methylene, and their pharmaceutically acceptable salts obtained by acid addition. New compounds form strong bonds with centers exhibiting specificity to homophthalzines and therefore can show significant activity in vivo with respect to the central nervous system. Invention describes also method of their synthesis, pharmaceutical composition and method of its preparing and method of suppression of convulsions. EFFECT: new compounds indicated above, valuable medicinal properties. 12 cl, 6 tbl, 42 ex