TRIFLUOROMETHYL-SUBSTITUTED SULPHONAMIDE AS SELECTIVE INHIBITOR OF BCL-2 Russian patent published in 2024 - IPC C07D211/96 C07D471/04 C07D215/20 A61K31/404 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I

where R¹ is selected from Cl or F; R² is selected from -C_0-3alkylene-R³; R³ is selected from 5-6-membered heterocycloalkyl, wherein heteroatom in 5-6-membered heterocycloalkyl is selected from the group consisting of N and O, and the number of heteroatoms is selected from 1–2, where 5-6-membered heterocycloalkyl is optionally substituted with one or two groups selected from the group consisting of 4-6 membered heterocycloalkyl, -COR^a, -SO₂R^b, -COOC_1-6alkyl and C_1-6alkyl, optionally substituted with a halogen atom, where heteroatom in 4-6 membered heterocycloalkyl is selected from O, and the number of heteroatoms is selected from 1; and each of R^a or R^b is independently selected from the group consisting of H, 4-member heterocycloalkyl, C_3-4cycloalkyl and C_1-6alkyl, where C_1-6alkyl is optionally substituted with a halogen atom, -CN, -N(C_1-6alkyl)₂, -NHC_1-6alkyl or -OC_1-6alkyl, wherein the structural fragment is selected from the group, consisting of and , which are selective inhibitors of BCL-2, a pharmaceutical composition and use for treating diseases associated with anti-apoptotic BCL-2, such as cancer.

EFFECT: novel compounds are obtained, which are selective inhibitors of BCL-2.

22 cl, 88 ex, 8 tbl