ACTIVE COMPOUNDS WITH RESPECT TO BROMO-DOMAINS Russian patent published in 2021 - IPC C07D215/16 C07D401/12 C07D401/14 C07D405/14 C07D413/12 C07D413/14 C07D471/04 C07D487/04 C07D491/04 C07D498/04 A61K31/4704 A61K31/4709 A61K31/496 A61K31/517 A61K31/5377 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of general formula (XI), in which R_2a is hydrogen; R_3a is methyl; R₇ is hydrogen; R₄, R₅, R₆ and R_8b are independently selected from a group consisting of hydrogen, C_1-4 alkyl and C_1-4 alkoxy; X₃ and X₄ are independently selected from a group consisting of N and C; provided that if X₄ is N, then R_9b is absent, and if X₄ is C, then R_9b is hydrogen; if X₃ is N, then R_10b is absent, and if X₃ is C, then R_10b is hydrogen; R_11b is selected from the group consisting of hydrogen, halogen, substituted C_1-6alkyl, substituted C_1-6alkoxy, -CN, -NO₂, substituted C_3-8cycloalkyl, unsubstituted or substituted 4–6-membered C_3-4heteroalicyclyl, unsubstituted or substituted heteroaryl, -NR₁₂R₁₃, -NR₁₄C(=O)R₁₅, -NR₁₄SO₂R₁₅, -C(=O)R₂₀, -C(=O)NR₂₂R₂₃, -SO₂NR₂₆R₂₇ and -OR₃₁; A is N; R_x and R y are independently selected from hydrogen, unsubstituted or substituted C_1-6alkyl, unsubstituted or substituted C_3-8cycloalkyl, unsubstituted or substituted 5-member C₄heteroalicyclyl and unsubstituted heteroaryl; or both of R_x and R y are taken together with A to form a ring system selected from a group consisting of unsubstituted or substituted 4–6 membered C_3-4heteroalicyclyl, unsubstituted or substituted 8–10-membered bicyclic C_6-8heteroalicylic, unsubstituted 7–10-membered spirocyclic C_5-8heteroalicyclyl and unsubstituted 5-member heteroaryl; and in cases where R_x and R_y are independently selected from hydrogen, unsubstituted or substituted C_1-6alkyl, unsubstituted or substituted C_3-8cycloalkyl, unsubstituted or substituted 5-member C₄heteroalicyclyl and unsubstituted heteroaryl, then R_11b cannot be hydrogen; values of other radicals are given in the patent claim. Invention also relates to individual compounds.

EFFECT: obtaining novel compounds of general formula (XI) which inhibit activity of at least one bromodomain selected from BRD4 (1) and BRD4 (2).

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