NEW IMIDAZO[4,5-c]QUINOLINE DERIVATIVES AS LRRK2 INHIBITORS Russian patent published in 2022 - IPC C07D471/04 C07D519/00 A61K31/437 A61P25/16 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I and their pharmaceutically acceptable salts having inhibitory activity against leucine-rich repeat kinase 2 (LRRK2). In formula I, R1 is selected from the group consisting of methyl, ethyl, cyclobutyl, cyclopentyl, etc., R2 is selected from the group consisting of 2,2-difluoropropyl, etc., R3 is selected from the group consisting of fluorine, chlorine, cyano, difluoromethyl and trifluoromethyl, wherein the compounds have one or more than one hydrogen atom which is replaced by a deuterium atom, provided that one or more hydrogen atoms are not replaced only by a deuterium atom in one or more of positions 2, 5, 7 or 8 of the quinoline ring. The invention also relates to specific compounds, in particular to [5-({8-chloro-1-[(2R,4R)-2-methyltetrahydro-2H-pyran-4-yl]-1H-imidazo[4,5-c ]quinolin-2-yl}methyl)pyrazin-2-yl]methanol and 8-chloro-2-{[5-(2H3)methylpyrazin-2-yl]methyl}-1-[(2R,4R)-2- methyltetrahydro-2H-pyran-4-yl]-1H-imidazo[4,5-c]quinoline, a pharmaceutical composition containing said compounds, and a method for treating a disease or disorder selected from the group consisting of Crohn's disease, Parkinson's disease, dementia with Lewy bodies, leprosy, Alzheimer's disease and tauopathy, with their use.

EFFECT: Crohn's disease, Parkinson's disease, dementia with Lewy bodies, leprosy, Alzheimer's disease and tauopathy treatment method improvement.

19 cl, 6 tbl, 96 ex