HEXONE-GLUCOKINASE INHIBITOR AND ITS USE Russian patent published in 2023 - IPC C07D403/14 C07D403/12 C07D401/14 A61K31/517 A61P3/00 A61P9/12 C07D239/95 

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions includes a compound of formula (I), its pharmaceutically acceptable salt or stereoisomer, a pharmaceutical composition based on them, their use and method of preparation, as well as intermediate compounds of formulas (IV), (V), (IV-1) and 2,4-dichloro-7,7-difluoro-6,7-dihydro-5H-cyclopenta[d]pyrimidine, 4-chloro-8,8-difluoro-2-(methylthio)-5,6,7,8-tetrahydroquinazoline, 4-chloro-9,9-difluoro-2-(methylthio)-6,7,8,9-tetrahydro-5H-cyclohepta[d]pyrimidine, 2,4-dichloro-8,8-difluoro -5,6,7,8-tetrahydroquinazoline. In formula (I), each of Χ,Υ and Ζ independently represents -Ν -; ring A is selected from 3–7 membered cycloalkyl; R¹ is selected from -(L)_m-C(O)OR^a; L is selected from C_1-6ealkylene; R² is selected from the following groups, optionally substituted with 1–3 Q2 groups: a 3–6 membered saturated heterocyclic group containing one nitrogen atom as a heteroatom, triazolyl and N(C_1-6alkyl)(C_3-6cycloalkyl); each R³ is independently selected from hydrogen, halogen, C_1-6alkyl, C_1-6alkoxy, halo-C_1-6alkyl, halo-C_1-6alkoxy; each R^a is hydrogen; each of the Q2 groups is independently selected from halo, C_1-6alkyl, C_1-6alkoxy, halo-C_1-6alkyl, and halo-C_1-6alkoxy; each of m and n is independently an integer from 1 to 3. Substituent values for formulas (IV), (V), (IV-1) are as indicated in the claims.

EFFECT: compounds of formula (I) having the properties of a ketohexokinase inhibitor.

12 cl, 4 tbl, 17 ex