ISOXAZOLE DERIVATIVES AS NUCLEAR RECEPTOR AGONISTS AND USE THEREOF Russian patent published in 2021 - IPC C07D261/08 C07D413/12 A61K31/42 A61P3/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof, which can be used as farnesoid-X receptor agonists. In formula IY is carbon; each of R¹ and R² independently represents hydrogen, halogen or trifluoromethyl; Z is n equals 0, 1 or 2; each of X¹, X² and X³ independently represents carbon or nitrogen; each of R³ and R⁴ independently represents hydrogen, halogen, cyano, C_1-6alkyl, C_3-6cycloalkyl, halo-C_1-6 alkyl, CONR^a1R^a2, NR^a1R^a2, CH₂NR^a1R^a2, CH₂R^c3, COR^a3, OR^a3, NR^a4COR^a3, NR^a4CO₂R^a3, NHCONHR^a3 or 3- or 8-member heterocycles, which in their structure contain one or two oxygen or nitrogen atoms, where m equals 1 or 2; each of R^a1 and R^a2 independently represents hydrogen, C_1-6alkyl, C_3-6cycloalkyl, halo-C_1-6alkyl or 3- or 8-member heterocycles, which in their structure contain one or two oxygen atoms or nitrogen; R^a3 is hydrogen, C_1-6alkyl, C_3-6cycloalkyl, halo-C_1-6alkyl, or 3- or 8-member heterocycles, which in their structure contain one or two oxygen or nitrogen atoms; R^a4 is hydrogen or C_1-6alkyl; R⁵ is hydrogen, each of R⁶ and R⁷ independently represents hydrogen, halogen, trifluoromethyl or trifluoromethoxy; R^c3 represents hydrogen or C_1-6alkyl; each of W¹, W² and W³ independently represents oxygen, nitrogen, CR^w1 or NR^w1, where R^w1 is hydrogen, C_1-6alkyl, C_3-6cycloalkyl, C_1-6alkylamine, C_1-6alkyl alcohol, or (CH₂)_pheteroaryl, where heteroaryl is 6-member monocyclic ring with one nitrogen atom, and p is equal to 1, 2 or 3. Invention also relates to a pharmaceutical composition for affecting a farnesoid-X receptor containing said compound of formula I or a pharmaceutically acceptable salt thereof.

EFFECT: disclosed are isoxazole derivatives as nuclear receptor agonists and use thereof.

7 cl, 2 tbl, 115 ex