DERIVATIVES OF N-(SUBSTITUTED PHENYL)-SULFONAMIDE AS KINASE INHIBITORS Russian patent published in 2021 - IPC C07D487/04 C07D491/48 C07D495/04 C07D513/04 A61K31/519 A61K31/4355 A61K31/4365 A61P25/28 A61P31/18 A61P35/00 A61P37/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds of the formula (I) and its pharmaceutically acceptable salts having the properties of an inhibitor of the activity of protein kinase RNA-like ER kinase (hereinafter – PERK kinase), a method for producing them, a pharmaceutical composition and a product based on them, in vitro method for inhibiting the activity of PERK kinase and use of a compound of the formula (I) or its pharmaceutically acceptable salt in the production of a drug for the treatment of a disease caused and/or related to disturbance of the regulation of PERK kinase activity, where the specified disease is selected from a group consisting of carcinomas, hematological tumors, multiple myelomas and neurodegenerative diseases. In the general formula (I), R1 is a group selected from (C₃-C₆) cycloalkyl, phenyl, naphthyl, 5-6-element heteroaryl with 1-3 heteroatoms selected from N and O, phenyl substituted with 1-3 groups selected from (C₁-C₃) alkyl, (C₁-C₃) halogen alkyl, (C₁-C₃) alkoxy, (C₁-C₃) halogen alkoxy, halogen, hydroxy, nitro and cyano, and 5-6-element heteroaryl with 1-3 heteroatoms selected from N and S substituted with 1-2 groups selected from (C₁-C₃) alkyl and halogen, 4-methyl-3,4-dihydro-2H-benzo[1,4]oxazinyl and 2,3-dihydrobenzofuranyl; R2 is selected from halogen, (C₁-C₃) alkyl and cyano, where E₁ and E₂ are independently CH or N; A is O, S or NR5, where R5 is a group selected from (C₁-C₃) alkyl, 6-element heterocyclyl with 1 heteroatom selected from N and O, 6-element heteroaryl with 1 heteroatom N and 6-element heterocyclyl with 1 heteroatom N substituted with (C₁-C₃) alkyl, (C₃-C₆) cycloalkyl and carbo (C₁-C₄) alkoxy.

EFFECT: obtaining derivatives of N-(substituted phenyl)-sulfonamide used as kinase inhibitors.

16 cl, 2 tbl, 6 ex