2-PHENYL-OXAZOLE-4-CARBOXAMIDE DERIVATIVES, MODULATING ACTIVITY OF JAK AND TYK2 KINASE Russian patent published in 2018 - IPC C07D263/48 C07D403/12 C07D413/12 A61K31/421 A61K31/422 A61K31/4523 A61P25/00 A61P29/00 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically to novel oxazole derivatives of general formula (2) or a pharmaceutically acceptable salt or stereoisomer thereof; where R⁷ is chlorine; R⁶ is selected from chlorine and fluorine; R³, R⁴ and R⁵ are hydrogen; n is 0 or 1; Q¹ is selected from C(=O) and SO₂; A is absent or is NR²; R¹ is selected from: – hydrogen; – C_1-3 alkyl group optionally substituted with one or more substituents selected from hydroxy, amino and methylamino; and 5-6 membered heterocyclic rings selected from pyrrolidine and piperidine, wherein the heterocyclic rings are optionally substituted with a methyl group; R², if present, is selected from hydrogen and methyl; or NR¹R² forms a 5-6 membered heterocyclic ring selected from pyrrolidine and morpholine, wherein the heterocyclic ring is optionally substituted with hydroxymethyl. Invention also relates to a pharmaceutical composition based on a compound of formula (2) and use thereof.

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EFFECT: obtaining novel compounds that modulate the activity of JAK and TYK2 kinases and are useful in the treatment of inflammatory or autoimmune diseases.

11 cl, 8 tbl, 35 ex