DISCLOSED ARE 3,6-DIAMINOPYRIDAZIN-3-YL DERIVATIVES CONTAINING PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS PRO-APOPTOTIC AGENTS Russian patent published in 2024 - IPC C07D417/12 C07D417/14 A61K31/501 A61K31/502 A61K31/5377 A61P35/00 A61P35/02 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I) or its enantiomers and diastereomers and addition salts thereof with a pharmaceutically acceptable acid or base, which have inhibitory activity on protein Bcl-xL and can be used to treat malignant neoplasms, autoimmune diseases or diseases of the immune system. In formula (I) R₁ and R₂ independently represent a group selected from hydrogen; linear or branched C₁-C₆ alkyl, optionally substituted with a hydroxyl or C₁-C₆ alkoxy group; C₃-C₆ cycloalkyl; trifluoromethyl, etc., R₃ is a group selected from hydrogen; C₃-C₆ cycloalkyl; linear or branched C₁-C₆ alkyl, etc., Het₁ is a group selected from the following, Het₂ is a group selected from the following, A₁ denotes S, A₂ denotes CH, G is selected from a group consisting of -C(O)OR_G3, -C(O)NR_G1R_G2, -C(O)R_G2, -NR_G1C(O)R_G2, etc., R_G1 and R_G2 in each case are independently selected from a group consisting of hydrogen, C₁-C₆ alkyl, optionally substituted with 1–3 halogen atoms, C₂-C₆ alkenyl, C₂-C₆ alkynyl, C₃-C₆ cycloalkyl, phenyl and -(CH₂)_1–4-phenyl; R_G3 is selected from a group consisting of C₁-C₆ alkyl optionally substituted with 1–3 halogen atoms, C₂-C₆ alkenyl, C₂-C₆ alkynyl, C₃-C₆ cycloalkyl, phenyl and -(CH₂)_1–4-phenyl, R₄ is a fluorine, chlorine or bromine atom, a methyl, hydroxyl or methoxy group, R₆ is a group selected from hydrogen, -C₂-C₆ alkenyl, etc., m=0, 1 or 2. Invention also relates to a pharmaceutical composition containing said compound and an intermediate synthesis compound.

EFFECT: disclosed are 3,6-diaminopyridazin-3-yl derivatives, pharmaceutical compositions containing them and use thereof as pro-apoptotic agents.

45 cl, 6 tbl, 290 ex