DIHYDROPYRAZOLOPYRAZINONE DERIVATIVE WITH MGAT-2 INHIBITORY ACTIVITY Russian patent published in 2023 - IPC C07D487/10 C07D487/20 C07D491/20 A61K31/4985 A61K31/499 A61P3/04 A61P3/06 A61P3/10 A61P9/10 A61P43/00 

FIELD: organic chemistry; pharmaceuticals.

SUBSTANCE: group of inventions relates to compounds with inhibitory activity against monoacylglycerin acyl transferase 2 (MGAT2). A compound represented by formula (I) is disclosed, wherein R¹ is hydrogen; R^2a and R^2b together with the adjacent carbon atom form ring B; ring B is represented by the formula: where each R⁶ is independently halogen, C1-C4 alkyloxy optionally substituted with substituent(s) selected from the group consisting of halogen, C1-C4 alkyloxy and phenyl, and n is 1 or 2; R^3a is hydrogen; R^3b is hydrogen; R^4a is a group represented by the formula: where L³ is a single bond or C1-C4 alkylene optionally substituted with halogen, R⁷ is halogen, sulfamoyl optionally substituted with C1-C4 alkyl, C1-C4 alkyloxy optionally substituted with halogen, C1-C4 alkylsulfonyl, aromatic heterocyclyl which is 5-membered monocyclic group containing two heteroatoms selected from O and N, a non-aromatic heterocyclyl which is a 4-membered monocyclic group containing one heteroatom selected from S and optionally substituted with oxo, or a group represented by the formula: -S(= O)(=NR^N)-R^S1, R^N is hydrogen and R^S1 is C1-C4 alkyl; and R^4b is C1-C6 alkyl optionally substituted with substituent group α, phenyl optionally substituted with substituent group β, or pyridyl optionally substituted with substituent β, substituent group α is halogen and cyclopropanyl, and substituent group β is halogen, cyano, C1-C4 alkyl, haloC1-C4 alkyl, hydroxyalkyl, C1-C4 alkyloxy, haloC1-C4 alkyloxy, cyclopropanyl, cyclopropanyloxy, C1-C4 alkylsulfonyl, or a pharmaceutically acceptable salt thereof. In addition, specific compounds are disclosed, a pharmaceutical composition having MGAT2 inhibitory activity containing the above compound or a pharmaceutically acceptable salt thereof, and a method of treating or preventing an MGAT2-associated disease, comprising administering the above compound.

EFFECT: group of inventions provides effective treatment of MGAT2-associated disease.

18 cl, 24 tbl, 13 ex