2-PYRIDYL SUBSTITUTED IMIDAZOLES AS ALK5 AND/OR ALK4 INHIBITORS Russian patent published in 2017 - IPC C07D487/04 A61K31/4188 A61K31/4427 A61P35/00 A61P13/12 A61P11/08 A61P17/02 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically to a novel 2-pyridyl-substituted imidazole derivative of formula (I), where R₁ is phenyl, pyridyl or thienyl, condensed with a structural fragment, which together with two ring members of said phenyl, pyridyl or thienyl forms a 5-6-member aromatic or non-aromatic saturated ring, wherein said ring optionally contains up to two heteroatoms, independently selected from O, N and S, and condensed phenyl ring is optionally substituted with one group, independently selected from halogen, -O-C-_1-6alkyl, -C_1-6alkyl, -O-(CH₂)_q-NR₄R₅, or 5-member heteroaryl containing up to two heteroatoms, independently selected from N; or R₁ is phenyl, substituted with one or more groups, independently selected from halogen, -O-C_1-6alkyl, -S-C_1-6alkyl, -C_1-6alkyl, -C₁haloalkyl, -CN, -(CH₂)_p-NR₄R₅, -(CH₂)_p-NHCOR₄, -(CH₂)_p-NHCO₂R₄; -(CH₂)_p-NHSO₂R₄ or N-bound 6-member heterocycle, where said heterocycle comprises two heteroatoms, independently selected from O, N, and optionally substituted with C_1-6alkyl; R₂ is -C_1-6alkyl; R₃ is H, -(CH₂)_p-NR₄R₅, -(CH₂)_p-CN, -(CH₂)_p-CO₂R₄, -(CH₂)_p-CONR₄R₅, -(CH₂)_p-OR₄, -(CH₂)_p-NHCOR₄; R₄ and R₅ independently denote H or -C_1-6alkyl; p denotes an integer ranging from 0 to 1; q denotes 2; n denotes an integer ranging from 1 to 2; X is NR₇; and R₇ is H or -CO-C_1-6alkyl. Invention also relates to use of a compound of formula (I), a pharmaceutical composition based on compound of formula (I) and to a method of preventing or treating diseases, based on use of compound of formula (I).

EFFECT: technical result is obtaining novel heterocyclic compounds effective in treating or preventing a disease, mediated by ALK5 and/or ALK4 receptors in a mammal.

8 cl, 44 ex, 1 tbl