PYRAZOLE COMPOUNDS SUBSTITUTED BY HETEROARYL AND THEIR APPLICATION IN PHARMACEUTICS Russian patent published in 2023 - IPC C07D403/14 C07D401/14 A61K31/4439 A61K31/506 A61P3/10 A61P43/00 

FIELD: pharmaceutics.

SUBSTANCE: heteroaryl-substituted pyrazole compounds, or pharmaceutically acceptable salts thereof, which have SGLT1 inhibitory activity, pharmaceutical compositions containing them and their use in pharmaceuticals. A compound having the formula [X] is described, where R¹ represents a hydrogen atom or a halogen; R² represents C_1-6 alkyl or halogen-C_1-6 alkyl; the Het ring represents: (1) pyridyl substituted with R³; or (2) pyrimidinyl, optionally substituted with R⁴ ; R³ represents a cyano group, halogen or halogen-C_1-3 alkyl; R⁴ represents halogen, hydroxy, C_1-3 alkyl, halogen-C_1-3 alkyl, C_1-3 alkoxy or -N(R⁵)(R⁶); and R⁵ and R⁶ each independently represent a hydrogen atom or a C_1-3 alkyl, or a pharmaceutically acceptable salt thereof. Also the compounds having formulas [I], [II], [III], [IV] are described, or their pharmaceutically acceptable salts, a pharmaceutical composition having inhibitory activity against SGLT1, containing any of the above compounds or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and an SGLT1 inhibitor containing any of the above compound or a pharmaceutically acceptable salt thereof. The claimed invention discloses the use of any of the above compounds or a pharmaceutically acceptable salt thereof for the production of an SGLT1 inhibitor, and the use of any of these compounds or a pharmaceutically acceptable salt thereof for the inhibition of SGLT1.

EFFECT: production of pyrazole compounds that have SGLT1-inhibiting activity.

13 cl, 16 tbl, 20 ex