N-(PHENYLSULFONYL)BENZAMIDES AND RELATED COMPOUNDS AS BCL-2 INHIBITORS Russian patent published in 2020 - IPC C07D471/04 A61K31/437 A61P35/00 A61P35/02 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to compounds of formula IA, having properties of BCL-2 inhibitors, pharmaceutical compositions based thereon, use, a method of treating and a kit for treating diseases, disorders or conditions susceptible to BCL-2 protein inhibition, including hyperproliferative protein, such as cancer. In general formula IA: A is selected from a group consisting of:

E is a carbon atom and is a double bond; or E is -C(H)- and is a single bond; or E is a nitrogen atom and is a single bond; X¹, X², and X³ are each independently selected from a group consisting of -CR⁸ =; R^1a and R^1b, taken together with the carbon atom to which they are bonded, form 4-member cycloalkyl; or R^1a and R^1b, taken together with the carbon atom to which they are bonded, form 4-member heterocycle with 1 oxygen atom; R² is selected from a group consisting of -NO₂; R^2a is selected from a group consisting of hydrogen and halogen; R³ is selected from a group consisting of hydrogen and -N(R^4a)(R^4b); R^4a is selected from a group consisting of C_1-6 alkyl and 6-member (heterocycloalkyl) C_1-6 alkyl with 1 to 2 oxygen atoms; R^4b is selected from a group consisting of hydrogen and C_1-4 alkyl; R⁵ is selected from a group consisting of 6-member (heterocycloalkyl) C_1-6 alkyl with 1 oxygen atom; R^6a , R^6c, R^6e, R^6f, and R^6g are each independently selected from a group consisting of hydrogen, C_1-6 alkyl, 6-member heterocycloalkyl with 1 oxygen atom, C_1-6 heteroalkyl with 1–2 oxygen atoms, and 6-member (heterocycloalkyl) C_1-6 alkyl with 1 oxygen atom; R^6b and R^6d are each independently selected from a group consisting of hydrogen; and R⁸ is selected from a group consisting of hydrogen and halogen.

I-A.

EFFECT: treating diseases, disorders or conditions susceptible to BCL-2 protein inhibition, including hyperproliferative protein, such as cancer.

49 cl, 7 tbl, 20 ex, 4 dwg