FIELD: chemistry.
SUBSTANCE: invention relates to a resorcinol derivative of formula (I) as an inhibitor of HSP90 and to its pharmaceutically acceptable salts, a method for preparing it, a pharmaceutical composition based thereon. In general formula (I), each of X and Y is independently selected from N, O or S; X1, X2, Y1, Y2 and a carbon atom linking X1 and X2, together form 5–7-member aromatic ring, an aliphatic saturated ring or an aliphatic unsaturated ring; each of X1 and X2 is independently selected from C, O, S, N, -C=C-, -C=N-; C to X1 or X2 can be unsubstituted or can be substituted with R01 or R02; each of R01 and R02 is independently selected from C1-10alkyl; each of Y1 and Y2 is independently selected from C or N; two substitutes at Y1 and Y2 are joined together to form a five-, six- or seven-member nitrogen-containing saturated ring containing substituents R1, R2 and R3; R1 is selected from hydrogen, C1-6alkyl, hydroxy-C1-6alkyl, C1-4alkoxy-C1-4alkyl, halogen-C1-4alkyl, C1-4alkylsulphonyl-C1-4alkyl, C1-4alkylamido-C1-4alkyl, N, N-di(C1-4alkyl)aminoacyl-C1-4alkyl, N, N-di(C1-4alkyl)amino-C1-4alkanoyl, morpholinyl-C1-4alkanoyl; R2 and R3 are selected from hydrogen or methyl, or substitutes R2 and R3 are linked to each other by a covalent bond to form a five-, six- or seven-membered saturated ring without substitutes; R4 is selected from halogen, C1-6alkyl, C3-6cycloalkyl; R5 is selected from C1-6alkoxyacyl, C1-7alkylaminocarbonyl, halogen-C1-6alkylaminocarbonyl, C1-6alkoxy-C1-6alkylaminocarbonyl, N, N-di (C1-6alkyl) amino-C1-6alkylaminocarbonyl, aminocarbonyl, hydroxy-C1-6alkylaminocarbonyl substituted with a hydroxyl group of halogen-C1-6alkyl substituted with a nitrile group of amidino or selected from 5–6 membered aromatic ring, optionally substituted with one or more R05; R05 is selected from C1-6alkyl.
(I)
EFFECT: invention relates to use in the preparation of a medicinal agent for treating proliferative diseases, such as cancer, and neurodegenerative diseases mediated by HSP90 heat shock protein activity.
23 cl, 4 tbl, 77 ex
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