NEW PYRIMIDINE DERIVATIVE WITH AN EFFECT OF INHIBITING GROWTH OF CANCER CELLS AND PHARMACEUTICAL COMPOSITION CONTAINING IT Russian patent published in 2021 - IPC C07D403/14 C07D401/14 A61K31/506 A61P35/00 

FIELD: chemistry, medicine.

SUBSTANCE: present invention relates to a new pyrimidine derivative. New pyrimidine derivative is represented by chemical formula 1, or a pharmaceutically acceptable salt thereof, where X and Y each independently appear as carbon or nitrogen, Z represents oxygen or C1-C4 alkyl group, R₁ is C1-C4 alkyl group, C3-C6 cycloalkyl group, CF₃ or dimethylamino group, R₂ represents C1-C4 alkyl group, R₃ is hydrogen or halogen group, R₄ represents hydrogen, halogen group, CN, CF₃, C1-C4 alkyl group or aminocarbonyl group, R₅ appears as hydrogen or C1-C4 alkyl group a group, R₆ is C1-C4 alkyl group, R₇ presents hydrogen, amino group substituted with one or more C1-C4 alkyl groups, or piperazinyl group, unsubstituted or substituted with one or more C1-C4 alkyl groups, when Z is oxygen, Z forms a double bond with S, which forms a single bond with N, or when Z represents C1-C4 alkyl group, Z forms a single bond with S, which generates a double bond with N; and R₄ and R₅ can also be bonded to form pyrrole, imidazole or thiophene. The invention also relates to the pharmaceutical composition for lung cancer treatment and containing an effective amount of the compound represented by Formula 1 or pharmaceutically acceptable salt thereof.

EFFECT: new pyrimidine derivative is obtained and described, which effectively inhibits the growth of cancer cells with the expression of C797S-mutant EGFR and MET-amplification, which are the main mechanisms of resistance to third-generation anti-cancer drugs targeting EGFR, and thus can be effectively used for lung cancer treatment.

Formula I

7 cl, 2 tbl, 18 ex