EP4 ANTAGONISTS Russian patent published in 2021 - IPC C07D487/04 C07D519/00 A61K31/4188 A61P35/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a heterocyclic compound of the formula (I) or its pharmaceutically acceptable salt, where R₁ is -CH₃, -CF₃, -CH₂CH₃, -CH₂F, CF₂CH₂OH, -CHF₂, -CH=CH₂, -CH₂OH or phenyl; R₂ is -H, -CH₂OH or -CH₃; R₃ is -H, or R₂ и R₃ taken together form cyclopropyl with carbon, to which they are attached; R₄ is -H, -F or -CH₃; R₅ is -C(O)OH, -C(O)OCH₃, -CH₂C(O)OH, cyclopropyl, -C(O)NHCN, or ; where R₆ is phenyl, -CH₃, cyclopropyl, or ; n is equal to 0-1; m is equal to 1-2; R₇ is -H, -CH₃ or is absent, when n is equal to 0; R₈ is -CF₃, -H, -Cl, -F, -CH₂CH₃, -OCH₃, -CH₃, -SCH₃, -CH₂OH, -CH₂F, -CH₂Cl, -I, -Br, -NH₂, -CH₂OCH₂CH₂F, -OCH₂CH₂F, -CH₂CH₂CH₂F, -OCF_3, -OH, -N(CH₃)₂, -CF₂CH₂OH or , or a bound connecting R₈ and ring A is a double bound, and R₈ is CH₂; R₉ is -H, -Cl or -CF₃; R₁₀ is -H, -CH₃, -CH₂F, -CH₂OH or -CH₂OCH₂-phenyl; X₁ and X₂ are either C, or one of them is C, and the other one is N; is a single bound or a double bound, and ring A is phenyl or cyclohexyl. The invention also relates to a pharmaceutical composition based on it.

EFFECT: new heterocyclic compounds are obtained having antagonistic activity relatively to E prostaglandin 4 receptor (EP4).

29 cl, 5 dwg, 1 tbl, 104 ex