2-AMINO-4-PHENYL-4-OXOBUTYRIC DERIVATIVES ACID AND PHARMACEUTICAL COMPOSITION

摘要

FIELD: medicine. SUBSTANCE: described are new 2-amino-4-phenyl-4-oxo-butyric acid of general formula IA: C1-C6 wherein each of groups X and Y is independently hydrogen, halogen, trifluoromethyl, hydroxy, alkyl, benzyl, phenyl, naphthyl, , SO2R, SOR or wherein C1-C6 is alkyl or benzyl; R is hydroxy, amino, hydroxy-amino, , , or wherein is as defined above, provided that R is not hydroxy when X and Y are simultaneously hydrogen; or X and Y are in position 3 or 4 of phenyl ring and are simultaneously hydroxy or group wherein is methyl, or one of groups X and Y is hydrogen and the other is in position 4 of phenyl ring and is hydroxy fluorine, chlorine, methyl, n-propyl or methoxy; or as individual isomers or mixtures thereof, or pharmaceutically acceptable salts thereof. 2-amino-4- phenyl-4-oxobutyric acid derivatives act as kinureninase and/or kinurenin-3-hydroxylase and are useful for prevention and/or treatment of diseases associated with neurodegeneration of tissues. Also described is pharmaceutical composition based on compounds of formula I. EFFECT: improved properties of the composition. 5 cl, 16 ex, 2 tbl