NEW COMPOUNDS AS mPGES-1 INHIBITORS Russian patent published in 2023 - IPC C07C235/50 C07D311/66 C07D211/56 A61K31/165 A61K31/355 A61K31/197 A61K31/439 A61P1/00 A61P11/00 A61P17/00 A61P19/00 A61P21/00 A61P25/00 

FIELD: chemistry.

SUBSTANCE: substance has the general structure (I), where T corresponds to the structure (IIIa) or (IIIb), where each R⁷ individually represents a C₁-C₆ alkyl part; L is a linker between the nitrogen atom of the amide and the distal nitrogen atom, where the linker is a saturated aliphatic group, which may include straight chains, branched chains and cyclic groups containing 1-10 optionally substituted backbone atoms selected from carbon, nitrogen and oxygen, where double bonds may be present between adjacent backbone atoms, and the optional substituents are selected from the group consisting of R⁶, carboxy, oxo, primary amino and carboxyl group, or the backbone atom can be connected to R¹ to form a 5-8 membered ring structure and/or a backbone atom can be connected to R² to form a 5-8 membered ring structure, or two backbone atoms can be connected to form a 5-8 membered ring structure, where R⁶ is C₁-C₆ alkyl; N* corresponds to the structure (IIa) or (IIb), each of R¹ and R² is independently selected from hydrogen (H), C₁-C₆ alkyl or C₁-C₆ alkenyl, or R¹ and R² are connected together and , thus form a second linker between the amide nitrogen atom and the distal nitrogen atom, or R¹ is connected to the backbone atom of the linker L in a 5-8-membered ring structure and/or R² is connected to the backbone atom of the linker L in a 5-8-membered cyclic structure; R³ is selected from hydrogen (H), C₁-C₆ alkyl or C₁-C₆ alkenyl, where the alkyl or alkenyl moiety may be substituted by one or more halogen atoms, hydroxyl moieties or (halo)alkoxy moieties, or R³ is absent, when the distal nitrogen atom is part of the imino moiety, or R³ is optionally connected to the backbone atom of the linker in a 5-8 membered ring structure; and R⁴ is selected from hydrogen (H) or C₁-C₆ alkyl, where the alkyl moiety may be substituted with one or more halogen atoms or (halo)alkoxy moieties; Xis a pharmaceutically acceptable anion for the treatment, prevention or suppression of symptoms mediated by increased expression or activity of mPGES-1.

EFFECT: amide derivatives of 2-hydroxy-2-methyl-4-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)butanoic acid for the treatment of conditions in which inhibition of the activity and/or expression of the mPGES enzyme-1.

14 cl, 1 tbl, 6 dwg, 2 ex.