PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS Russian patent published in 2019 - IPC C07D417/12 C07D473/18 C07D487/04 C07D519/00 C07D239/553 C07D239/545 C07D403/12 A61K31/506 A61K31/519 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (Ia) or a pharmaceutically acceptable salt thereof. In formula (Ia):

(Ia), R¹ is NR^cR^d, where R^c is a saturated 5-6 membered heterocyclic ring containing a nitrogen atom in the ring, where the specified saturated 5-6-membered heterocyclic ring is optionally substituted with OZ or C_1-4 alkyl which is then optionally substituted with OZ or NR₁₁R₁₂, where Z, R₁₁, R₁₂ independently are H or C_1-4 alkyl, or the indicated saturated 5-6-membered heterocyclic ring is optionally substituted with SO₂(CH₂)_qH, where q is 1–4, or C_1-4 alkyl, which is then optionally substituted by SO₂(CH₂)_qH, where q is 1–4, or R₈CO, where R₈ is C_1-4 alkyl; and R^d is H, C_1-4 alkyl, C_2-4 alkenyl or 3-membered cycloalkyl ring, where C_1-4 alkyl is optionally substituted with OZ, where Z is H or C_1-4 alkyl; R² is missing when Y is N, and R² is H or halo, when Y is C; R³ is C_1-4 alkoxy; R⁵ is H or halo; R⁶ is H or OMe; R⁷ is H; R⁹ is H; R¹⁰ is H; R⁴ is C₂ alkenyl; X is O, NH, CH₂ or CF₂; Y is C or N; and A is C; or its pharmaceutically acceptable salt.

EFFECT: compounds possess the properties of the inhibitor of activity of Bruton tyrosine kinase (Btk or BTK) or Janus kinase (JAK), and can be used to treat cancer such as sarcoma, squamous cell carcinoma, fibrosarcoma, cervical cancer, stomach cancer, skin cancer, leukemia, lymphoma, lung cancer, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, kidney cancer, prostate cancer, breast cancer, liver cancer, head and neck cancer, and pancreatic cancer.

40 cl, 6 dwg, 6 tbl, 73 ex