ISOXAZOL AS FXR RECEPTOR AGONISTS Russian patent published in 2023 - IPC C07D261/08 A61K31/42 A61P1/00 A61P3/00 

Abstract RU 2793266 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to new isoxazoles of formula (I) or pharmaceutically acceptable salts thereof, having agonistic activity against the farnesoid FXRreceptor. In this formula, R1 and R2 are independently selected from the group consisting of H, halogen and CF 3, provided that R1 and R2 are not H at the same time; R3 is C1-C3 alkyl; n is an integer selected from 1, 2 and 3; R4 is selected from the group consisting of phenyl unsubstituted or substituted with one R5 and biphenyl unsubstituted or substituted with one R5 ; R5 is selected from the group consisting of COOR6, CN, hydroxy-C1-C3 alkyl, C1-C3 alkyl-O-phenyl unsubstituted or substituted with one R7, and C1-C3 alkyl-O-biphenyl , unsubstituted or substituted with one R7; R6 is selected from the group consisting of H and C1-C3 alkyl, and R7 is selected from the group consisting of COOR6, CN and hydroxy-C1-C3 alkyl; provided that the compound is not 4-((3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl)methoxy)benzoic acid. The invention also relates to a pharmaceutical composition containing isoxazole formula (I) and its use as a drug for the prevention and/or treatment of FXR-dependent diseases.

EFFECT: drug for the prevention and/or treatment of FXR-dependent diseases.

9 cl, 1 tbl, 6 ex

I.

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RU 2 793 266 C2

Authors

Zampella Angela

Fiorucci Stefano

Dates

2023-03-30Published

2019-07-17Filed