DERIVATIVES OF 4-OXO-3,5-DIHYDRO-4H-PYRIDAZINO[4,5-B]-INDOL-1-ACETAMIDE, THEIR SYNTHESIS AND APPLICATION IN THERAPY

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of 4-oxo-3,5-dihydro-4H-pyridazino[4,5-b]indol-1- acetamide of the formula (I): where X means H, methyl-, methoxy-, phenylmethoxy-group; Y means H, one or two halogen atoms, OH, ; R1 means H, C1-C4-alkyl;...

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Hauptverfasser: EHVANNO JANNIK, DJUBUA LORAN, BARTSH REZHIN, SEVREN MIREJ, ZHIJ KATRIN, MARGEH FRANK, FRUASSAN ZHAK
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of 4-oxo-3,5-dihydro-4H-pyridazino[4,5-b]indol-1- acetamide of the formula (I): where X means H, methyl-, methoxy-, phenylmethoxy-group; Y means H, one or two halogen atoms, OH, ; R1 means H, C1-C4-alkyl; R2 and R3 each and independently each of other means H, C1-C4-alkyl, phenylmethyl group; or R2 and R3 with nitrogen atom that carries their form azethidinyl-, pyrrolidinyl-, 3-ethoxypyrrolidinyl-, piperidinal-, morpholinyl-, 4-methylpiperazinyl- or 1,3- thiazolidinyl-group. Compounds of the formula (I) are agonists of ω1- and ω2-benzodi-azepine receptors located in macromolecular gamma-aminobutyric acid (GABA) complex and therefore they can be used for treatment of diseases associated with disorder of GABA-ergic transmission. EFFECT: improved method of synthesis, valuable medicinal properties of compounds. 4 cl, 1 tbl