HETEROCYCLIC DERIVATIVES AND USE THEREOF Russian patent published in 2019 - IPC C07D209/42 C07D231/56 C07D233/54 C07D277/68 C07D307/87 C07D333/72 C07D401/12 C07D403/12 C07D409/12 C07D413/12 C07D417/04 C07D471/04 C07D495/04 A61K31/34 A61K31/381 A61K31/404 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula:

n which A represents a saturated or unsaturated C_5-6 carbocycle or a 5-10-membered heterocycle; B is a benzene or a 5-12-membered heterocycle containing 1-3 nitrogen atoms; C is a benzene, a 5-12-membered heterocycle or a C_3-6 carbocycle; Y represents -C(= O)- associated with X₂ or X₅; X₁ is -O-, -S-, -S(=O)-, -S(=O)₂- or -N(W₁)-; X₂ is a carbon atom bound to Y, or -N =, -NH-, -C(W₂)= or -CH(W₂)-, which is not associated with Y; X₃ and X₄ independently represent a carbon or nitrogen atom; X₅ is a carbon atom bound to Y, or -CH=, which is not bound to Y; wherein the 5-membered ring including X₁-X₅ is aromatic or non-aromatic; W is a hydrogen, halogen or C_1-6 alkyl; W₁ is a hydrogen, C_1-6 alkyl, C_1-6 alkoxycarbonyl or 5-8-membered heterocyclyl-C_1-4 alkyl; W₂ is a hydrogen, halogen, C_1-6 alkyl or 5-8-membered heterocyclyl-C_1-4 alkyl; L is -(CR₉R₁₀)_m-, -(CR₉R₁₀)_m-O-, -NH-, -N(C_1-6 alkyl)-, -S(=O)₂-, -C(=O)-, -C(=CH₂)- or C_3-7 cycloalkylene, wherein m is an integer from 0 to 3 and R₉ and R₁₀ independently represent a hydrogen, halogen or C_1-6 alkyl; R₁ is nitro, amino, C_1-6 alkylsulfonyl, halogenC_1-6 alkoxy or any of the following structural formulas i) to iv): i) , ii) , iii) and iv) ; R₂ is a hydrogen, halogen, nitro, amino, C_1-6alkoxy, halogenC_1-6alkoxy, C_1-6 alkylsulfonyl or 5- or 6-membered heterocycloalkyl; R₃ is a hydrogen, halogen, cyano, C_1-6 alkyl, halogen_1-6 alkyl, cyanoC_1-6 alkyl, C_1-6 alkylcarbonyl, C_1-6 alkoxy, halogen C_1-6 alkoxy, cyanoC_1-6 alkoxy, C_1-6 alkylamino, diC_1-6 alkylamino, C_1-6 alkylthio, C_1-6 alkylaminocarbonyl, diC_1-6 alkylaminocarbonyl, C_2-8 alkynyl, C_6-10 aryl, halogenC_6-10 aryl, 5-10-membered heterocyclyl or 5-10-membered heterocyclylcarbonyl, wherein the heterocyclyl part may be substituted by one to three substituents; R₄ is a hydrogen, halogen, hydroxy, cyano, nitro, amino, oxo, aminosulfonyl, sulfonylamido, C_1-6 alkylamino, C_1-6 alkyl, halogenC_1-6 alkyl, cyanoC_1-6 alkyl, C_1-6 alkoxy, halogen C_1-6 alkoxy, cyanoC_1-6 alkoxy, C_3-8 cycloalkyloxy, C_2-8 alkynyl, C_1-6 alkylamino-C_1-6 alkoxy, C_1-6 alkylamino-C_1-6 alkoxy, C_1-6 alkoxycarbonyl, carbamoyl, carbamoyl-C_1-6 alkoxy, C_1-6 alkylthio, C_1-6 alkylsulfinyl, C_1-6 alkylsulfonyl, 5-10 membered heterocyclyl, 5-10 membered heterocyclyl-C_1-6 alkyl, 5-10-membered heterocyclyl-C_1-6 alkoxy or 5-10-membered heterocyclyloxy, with the heterocyclyl part being substituted with one or two substituents; R₆ is C_1-6 alkyl, halogen_1-6 alkyl, C_1-6 alkoxyC_1-6 alkyl, C_1-6 alkylcarbonylC_1-6 alkyl, C_2-7 alkenyl, amino, aminoC_1-6 alkyl, C_3-7 cycloalkyl, 5-10 membered heterocyclyl or 5-10 membered heterocyclyl-C_1-6 alkyl, or condensed with R₅, forming C_3-4 alkylene, and the amino group may be substituted by one or two substituents, R₇ and R₈ independently represent a hydrogen or C_1-6 alkyl; p is 1 and q is 0 or 1; r is an integer from 0 to 3, and when r = 2 or more, the R₃ groups are the same or different; and s is an integer from 0 to 3, and when s = 2 or more, the R₄ groups are the same or different, which has an inhibitory effect on the activation of STAT3 protein.

EFFECT: invention can be used for the prevention or treatment of diseases associated with the activation of STAT3 protein.

17 cl, 46 tbl, 497 ex