| 摘要 |
organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of indole-2,3-dione-3-oxime of the formula (I): where R1 means hydrogen atom, C1-C6-alkyl; R3 means Het or group of the formula: where Het means tetrahydrofuryl that can be substituted once or more times with substitutes taken among the group comprising of halogen atom, C1-C6-alkyl, C1-C6-alkoxy-group and oxo-group; at least one of R31, R32, R33 means independently hydrogen atom, C1-C6-alkyl or hydroxy-C1-C6-alkyl and at least one of R31, R32, R33 means independently (CH2)nR34 where R34 means hydroxyl, carboxyl, C1-C6-alkoxycarbonyl, C3-C7-cycloalkyl-C1-C6-alkoxycarbonyl, isoxazolyl ring that can be substituted once or more times with substitutes taken among the group comprising of halogen atom, C1-C6-alkyl, C1-C6-alkoxy-group, oxo-group or CONR35R36 where R35 and R36 mean hydrogen atom, C1-C6-alkyl, hydroxy-C1-C6-alkyl or (CH2)nR37 where R37 means hydroxyl, C1-C6-alkoxycarbonyl, C3-C7-cycloalkyl-C1-C6- -alkoxycarbonyl; or and R36 in common with N-atom to which they are bound form unsaturated 6-membered heterocyclic ring containing possibly one additional O-atom; n = 0, 1, 2 or 3; R5 means phenyl that can be substituted with phenyl or SO2NR51R52 where R51 and R52 each means independently C1-C6-alkyl; or R51 and R52 in common with N-atom to which they are bound form unsaturated 6-membered monocyclic heterocyclic ring; "A" is a ring condensed with benzyl ring in positions "a" and "b" and formed by the following bivalent radicals: a-CH2-NR6-CH2-CH2-b where R6 means C1-C6-alkyl, or its pharmaceutically acceptable salt. Compounds of the formula (I) are antagonists of exciting amino acids and can be used in pharmaceutical composition showing affinity to AMPA-receptor and useful for treatment of disorders and diseases responding to an antagonist of AMPA-receptor in mammals including humans. Invention describes a method of synthesis of compound of the formula (I). EFFECT: valuable medicinal properties. 12 cl, 24 ex
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