BENZIMIDAZOLE DERIVATIVES, METHODS FOR THEIR PRODUCTION AND USE Russian patent published in 2022 - IPC C07D471/04 C07D487/04 C07D498/04 A61K31/506 A61K31/5365 A61P35/00 A61P35/02 

FIELD: pharmaceutical chemistry.

SUBSTANCE: group of inventions relates to pharmaceutical chemistry and includes a compound of the formula (I), its enantiomers or pharmaceutically acceptable salts, 4-(6-fluor-1-methyl-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-8-yl)-N-(5-(4-methylpiperazine-1-yl)pyridine-2-yl)pyrimidine-2-amine, N-(5-((4-ethylpiperazine-1-yl)methyl)pyridine-2-yl)-5-fluor-4-(6-fluor-1-methyl-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-8-yl)pyrimidine-2-amine, a pharmaceutical composition based on them, and its use, as well as a method for the treatment of a disease mediated with CDK4 and/or CDK6 in a subject. In the formula (I), A is selected from pyridyl, pyrimidinyl, and pyridazinyl; Z is NH or O; R₁ is independently selected from a group consisting of heterocyclyl, a group of heterocyclyl-(CH₂)m-, NR₁₂R₁₃, -NR₁₂-C_1-6alkylene-NR₁₂R₁₃, and heterocyclyl-C(O)-, where each heterocyclyl is 5-6-element and is selected from pyrrolidinyl, piperidinyl, and piperazinyl, and it can be substituted with 1-2 substitutes selected from hydroxyl, C_1-8alkyl, C_3-8cycloalkyl, oxetanyl, -NR₁₂R₁₃, or -(CH₂)_t-OH; each R₂ and R₃ is independently selected from H, halogen, C_1-8alkyl, where C_1-8alkyl can be substituted with 1-3 halogen atoms; each R₁₂ and R₁₃ is independently selected from C_1-8alkyl, which can be substituted with one hydroxyl; m is equal to 0 or 1; n and t are equal to 1.

EFFECT: benzimidazole derivatives showing properties of CDK4 and/or CDK6 inhibitors.

30 cl, 19 tbl, 7 ex