BRUTON'S TYROSINE KINASE INHIBITORS Russian patent published in 2018 - IPC C07D401/14 C07D403/06 C07D403/14 C07D409/14 A61K31/4155 A61K31/4439 A61K31/496 A61K31/5377 A61P11/06 A61P29/00 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula I or pharmaceutically acceptable salts thereof. In general formula I R¹ is H or halo; R² is H, halo or cyano; R³ is R⁴ or R⁵; R⁴ is halo; R⁵ is phenyl or benzyl optionally substituted with cyano, lower alkoxy or halo; 5-6 membered heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulphur optionally substituted with lower alkyl; -C(=O)R^5'; lower alkyl substituted with cyano or morpholinyl; R^5' is a 6-membered heterocycloalkyl containing two heteroatoms selected from nitrogen and oxygen, optionally substituted with lower alkyl, amino, (lower alkyl)amino, di(lower alkyl)amino, or lower alkoxy; X is lower alkyl. Compounds of formula I inhibit Btk (Bruton’s tyrosine kinase). Compounds of formula I are useful for modulating the activity of Btk and treating diseases associated with excessive Btk activity. Invention also relates to pharmaceutical compositions containing compounds of formula I and at least one carrier, diluent or excipient. I.

EFFECT: compounds are useful for the treatment of cancer, autoimmune and inflammatory diseases caused by aberrant B-cell activation.

24 cl, 2 tbl, 21 ex