COMPOUNDS Russian patent published in 2025 - IPC C07D413/04 C07D413/12 C07D417/12 C07D261/20 A61K31/423 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I)

or a pharmaceutically acceptable salt thereof, where: R¹, R², R³ and R⁴ are independently selected from: (i) H; (ii) C_1-3 alkyl, optionally substituted with: hydroxy, C_1-2 alkoxy, NH₂, phenyl, C_5-6 heteroaryl, C_1-4 alkylcarbamoyl, or acylamido; (iii) C_1-3 alkoxy optionally substituted with C_3-6 cycloalkyl or one or more fluoro groups; (iv) C_3-6 cycloalkyl; (v) halogen; (vi) COR^C, where R^C is selected from NR^N1R^N2, where R^N1 and R^N2 are independently selected from H and methyl; (vii) cyano, NH₂ or NO₂; and (viii) phenyl or C_5-6 heteroaryl, optionally substituted with methyl, cyano, hydroxy or methoxy; Ar is phenyl optionally substituted with one or more groups selected from: (i) C_1-4 alkyl optionally substituted with hydroxy, C_1-2 alkoxy, NH₂, C_1-4 alkylcarbamoyl or one or more fluoro groups; (ii) C_3-6 cycloalkyl; (iii) hydroxy; cyano; NR^N3R^N4, where R^N3 and R^N4 are independently selected from H and methyl; or acylamido; (iv) halogen; (v) C_1-3 alkoxy, optionally substituted with hydroxy, C(O)NH₂, C_3-6 cycloalkyl, phenyl, C_5-6 heteroaryl or one or more fluoro groups; (vi) phenoxy, optionally substituted with fluorine; (vii) phenyl or C_5-6 heteroaryl; or (viii) SF₅ or SO₂CH₃; and, where at least one of R¹, R², R³ and R⁴ is not H and where C_5-6 heteroaryl has 5 to 6 ring atoms, of which 1 to 3 ring atoms are heteroatoms selected from a nitrogen atom, oxygen or sulphur, as well as a pharmaceutical composition which inhibits lysine acetyltransferase (KAT).

EFFECT: novel compounds which inhibit the activity of one or more KATs from the MYST family are obtained, and can be used for treating cancer.

14 cl, 17 tbl, 252 ex