TWO-SUBSTITUTED PYRAZOLE COMPOUNDS FOR DISEASE TREATMENT Russian patent published in 2022 - IPC C07D231/12 C07D401/04 C07D401/14 C07D405/14 A61K31/4439 A61K31/444 A61K31/506 A61P9/00 A61P35/00 A61P3/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of the formula (I), where R¹ is phenyl, pyridinonyl or pyridinyl, where phenyl and pyridinyl rings are optionally substituted with 1 R^1a, and where pyridinonyl nitrogen is substituted with R^1b; each R^1a is independently halogen, C_1-8alkyl, C_1-8halogenalkyl or heterocycloalkyl, where 1 heteroatom is present, which is N, and where heterocycloalkyl includes from 3 to 9 ring atoms; R^1b is hydrogen, C_1-8alkyl, C_1-8halogenalkyl, C_3-13cycloalkyl-C_1-8alkyl or heterocycloalkylalkyl, where 1 heteroatom is present, which is N, and where heterocycloalkyl includes from 3 to 9 ring atoms; R² is , where 0, 1 or 2 of X¹-X⁴ are nitrogen, and the remaining ones are CH or CR^2b, provided that 0-2 CR^2b are present; R^2a is -NR^5aS(O)₂R^5b or -NR^6aR^6b; each R^2b is independently halogen, C_1-8alkyl, C_1-8halogenalkyl or cyano; R³ is hydrogen or C_1-8alkyl; R⁴ is hydrogen or C_1-8alkyl; R^5a and R^6a are hydrogen; and R^5b and R^6b are independently C_1-8alkyl; C_1-8halogenalkyl; C_3-13cycloalkyl; C_3-13cycloalkyl-C_1-8alkyl; heterocycloalkyl or heterocycloalkyl-C_1-8alkyl, where for heterocycloalkyl and heterocycloalkylalkyl, 1 heteroatom is O, and where heterocycloalkyl includes from 3 to 9 ring atoms; at the same time, C_3-13cycloalkyl in R^5b and R^6b, individually or as part of another group, is independently optionally substituted with one C_1-8alkyl. A pharmaceutical composition containing a compound of the formula (I), and a method for the treatment of a condition, disease or disorder associated with abnormal activation of a pathway of sterol regulatory element-binding protein (hereinafter – SREBP).

EFFECT: proposed compounds can be used for the treatment of a condition, disease or disorder associated with abnormal activation of SREBP pathway, including metabolic disorders, cancer and non-alcoholic steatohepatitis (fatty liver disease) (NAFLD).

39 cl, 16 dwg, 2 tbl, 136 ex