BENZOFURAN DERIVATIVE, A METHOD FOR PRODUCTION THEREOF AND USE THEREOF IN MEDICINE Russian patent published in 2020 - IPC C07D405/14 C07D405/12 A61K31/4545 A61K31/5377 A61K31/496 A61K31/4433 A61P35/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a benzofuran derivative of general formula (I), or a pharmaceutically acceptable salt thereof, in which ring A is selected from a group consisting of heterocyclyl, which is 5–6 membered saturated monocyclic hydrocarbon group having one heteroatom selected from N, O and S, and 3–6-member cycloalkyl; each R¹ is identical to or different from the other, and each is independently selected from a group consisting of a hydrogen atom, a halogen atom, C_1-6-alkyl, halo-C_1-6-alkyl, cyano, 3–6-member cycloalkyl, 5–6 membered saturated or partially unsaturated monocyclic hydrocarbon group having one N atom and -(CH₂)_xR^a, where 5–6 membered saturated or partially unsaturated monocyclic hydrocarbon group is optionally substituted with one or more groups selected from group, consisting of C_1-6-alkyl; R^a is selected from a group consisting of heterocyclyl which is 5–6 membered saturated monocyclic hydrocarbon group having one or two heteroatoms selected from N and O, and -NR⁷R⁸, where each heterocyclyl is independently and optionally substituted with one or more groups selected from a group consisting of C_1-6-alkyl, a halogen atom and hydroxy-C_1-6-alkyl; R² is C_1-6-alkyl, where alkyl is optionally substituted with one or more groups selected from a group consisting of 3–6-member cycloalkyl; R³ is selected from a group consisting of C_1-6-alkyl, a halogen atom and halo-C_1-6-alkyl; each R⁴ is identical to the other or different from it, and each is independently selected from a group consisting of a hydrogen atom, C_1-6-alkyl and C_1-6-alkoxy; each R⁵ is identical to the other or different from it, and each is independently selected from a group, consisting of a hydrogen atom, oxo, a halogen atom, halo-C_1-6-alkyl, -C(O)R⁶, -S(O)_mR⁶ and -NR⁷R⁸; R⁶ is selected from C_1-6-alkyl; R⁷ and R⁸ are identical or different from each other, and each is independently selected from a group consisting of C_1-6-alkyl; m equals 2; n equals 2; p is 0, 1 or 2; q equals 0 or 1; and x is equal to 1, 2 or 3. Invention also relates to a method of producing a compound of formula (I) and a pharmaceutical composition having inhibitory activity on EZH2 based thereon.

EFFECT: technical result is obtaining a novel compound and a pharmaceutical composition based thereon, which can be used in medicine for preventing and/or treating diseases, such as tumors and cancer.

13 cl, 4 tbl, 34 ex