2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND/OR ALK4 RECEPTOR INHIBITORS Russian patent published in 2009 - IPC C07D401/04 C07D405/14 A61K31/4178 A61K31/4439 A61K31/498 

FIELD: chemistry.

SUBSTANCE: invention concerns new compounds of formula I or its pharmaceutically acceptable salts: , where R₁ is phenyl group optionally substituted by substitutes selected out of halogen atom, -O-C_1-6-alkyl; or R₁ is phenyl condensed with aromatic or non-aromatic 5-7-member ring where the ring can optionally include up to three heteroatoms selected independently out of N, O and S; R₂ is hydrogen, -O-C_1-6-alkyl, -C_1-6-alkyl or halogen atom; R₃ is C_1-6-alkyl, -(CH₂)_P-NO₂, -(CH₂)_p-NR₄R₅, -(CH₂)_P-CONHOH, -(CH₂)_p-CN, -(CH₂)_P-CO₂H, -(CH₂)_p-CO₂R₄, -(CH₂)_P-CONR₄R₅, -(CH₂)_p-OR₄, -(CH₂)_p-NHCOR₄ or -(CH₂)_p-NHSO₂R₄; R₄ and R₅ are independently hydrogen or C_1-6-alkyl; p is 0, 1, 2, 3 or 4; X is C_1-10-alkylene group; one of A₁ and A₂ is nitrogen atom, while the other is NR₇; and R₇ is hydrogen atom or OH-group. Also invention concerns pharmaceutical composition, method of TGF-β and/or activine signal transit route inhibition, method of reduction of excessive exocellular matrix accumulation for mammals, method of tumour cell metastasis inhibition for mammals, method of treatment of cancer neoplasm caused by TGF-β superexpression by TGF-β signal transit route inhibition for mammals, method of disease treatment, and method of thrombosis inhibition for mammals.

EFFECT: new compounds with useful biological properties.

16 cl, 19 ex, 2 tbl, 8 dwg