PYRIMIDINE DERIVATIVE WITH INHIBITORY ACTIVITY ON PROTEIN KINASES AND THERAPEUTIC PHARMACEUTICAL COMPOSITION CONTAINING SAME Russian patent published in 2025 - IPC C07D401/12 C07D401/14 C07D405/14 A61K31/506 A61K31/5377 A61P35/00 

FIELD: chemistry.

SUBSTANCE: group of inventions relates to a compound selected from a pyrimidine derivative of formula 10, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing and treating cancer, containing said pyrimidine derivative. In formula 10, the values of the variables are as follows: R₁ represents a hydrogen atom, halogen, C₁-C₁₃ alkyl or C₁-C₆ alkoxy, R₂ represents a hydrogen atom, R₃ and R₄ each independently represent a hydrogen atom, R₅, R₆ and R₇ each independently represent a hydrogen atom, hydroxyl, halogen, C₁-C₁₃ alkyl, C₁-C₆ alkoxy, X₁ and X₃ each independently represents carbon, X₂ represents CH or nitrogen, A is C₃-C₁₀ heterocyclyl, B is selected from and

C₁-C₆ alkoxy or C₁-C₁₃ alkyl contains one or more substitutes selected from a group consisting of a hydrogen atom and a halogen, C₃-C₁₀ heterocyclyl contains one or more substitutes selected from the group consisting of hydrogen atom, halogen, C₁-C₃ alkyl, unsubstituted or substituted with halogen, C₁-C₃ alkoxy groups, unsubstituted or substituted with halogen, and C₃-C₁₀ heterocyclyl, and C₃-C₁₀ heterocyclyl contain at least one heteroatom N.

EFFECT: disclosed compounds have inhibitory activity on protein kinases, including EGFR, in particular, have a strong inhibitory effect on various drug-resistant EGFR mutants, including mutants of deletion 19 of exon-T790M-C797S-EGFR, L858R-T790M-C797S-EGFR, deletion 19 of exon-T790M-EGFR and L858R-T790M-EGFR, and can be used as a preventive and therapeutic agent against cancerous diseases caused by EGFR mutation.

12 cl, 1 tbl, 288 ex