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, C1-6-alkyl, halo-C1-6-alkyl, cyano, 3–6-member cycloalkyl, 5–6 membered saturated or partially unsaturated monocyclic hydrocarbon group having one N atom and -(CH2)xRa, where 5–6 membered saturated or partially unsaturated monocyclic hydrocarbon group is optionally substituted with one or more groups selected from group, consisting of C1-6-alkyl; Ra 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 C1-6-alkyl, a halogen atom and hydroxy-C1-6-alkyl; R2 is C1-6-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 C1-6-alkyl, a halogen atom and halo-C1-6-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, C1-6-alkyl and C1-6-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-C1-6-alkyl, -C(O)R6, -S(O)mR6 and -NR7R8; R6 is selected from C1-6-alkyl; R7 and R8 are identical or different from each other, and each is independently selected from a group consisting of C1-6-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
Authors
Dates
2020-07-21—Published
2016-11-02—Filed