BRUTON'S TYROSINE KINASE INHIBITORS Russian patent published in 2015 - IPC C07D401/14 C07D401/10 C07D403/14 C07D217/24 C07D237/32 A61K31/4725 A61K31/502 A61K31/497 A61K31/5355 A61K31/5377 A61K31/506 A61P29/00 A61P19/02 

FIELD: medicine.

SUBSTANCE: present invention refers to compounds having formula III such as below, wherein: Q represents C(Y³) or N; R represents H, -R¹, -R¹-R²-R³, -R¹-R³ or -R²-R³; R¹ represents heteroaryl or heterocyclyl each of which is optionally substituted by one or more C_1-6alkyls, hydroxyC_1-6alkyls, oxogroups or halogenC_1-6alkyls; R² represents -C(=O), -O, -C(R^2')₂, -C(R^2')₂C(=O), -C(R^2')₂C(=O)NR^2', C(R^2')₂ N(R^2')C(=O), -C(=NH), -C(R^2')₂NR^2' or -S(=O)₂; each R^2' independently represents H or C_1-6alkyl; R³ represents H or R⁴; R⁴ represents C_1-6alkyl, C_1-6alkoxygroup, aminogroup, C_1-6alkylaminogroup, di(C_1-6alkyl)aminogroup, heterocyclyl, C_1-10alkylheterocycloalkyl, heterocycloalkylC_1-10alkyl each of which is optionally substituted by one or more C_1-6alkyls, C_1-6alkylaminogroups, di(C_1-6alkyl)aminogroups, hydroxygroups, hydroxyC_1-6alkyls, C_1-6alkoxygroups, oxogroups or halogenC_1-6alkyls; X represents CH; X' represents CH; and the rest symbols have values as specified in the patent claim. The compounds of formula III inhibit Bruton's tyrosine kinase (Btk). There are also described compositions containing the compounds of formula III, and at least one carrier, thinner or excipient, and a method for producing the compound of formula X in accordance with the following procedure.

EFFECT: compositions are effective for modulating Btk activity and treating diseases related to Btk hyperactivity, and can be used for treating inflammatory and autoimmune diseases related to disturbed B-cell proliferation, such as rheumatoid arthritis.

22 cl, 2 tbl, 260 ex