PURINONE DERIVATIVE Russian patent published in 2016 - IPC C07D473/34 A61K31/522 A61P37/00 A61P35/00 A61P29/00 A61P7/02 

FIELD: chemistry.

SUBSTANCE: compounds demonstrate metabolic stability and do not possess hepatotoxicity, that is are safe therapeutic medications for treating diseases, involving B-cells or mast cells. Compounds can be used in treatment of allergic disease, autoimmune disease, inflammatory disease, thromboembolic disease or cancer, in particular in treatment of non-Hodgkin's lymphoma. In general formula (I) L represents (1) -O-, (5) -NH-, (6) -C(O)-, (7) -CH₂-O-, (8) -O-CH₂- or (9) -CH₂-; R¹ represents (1) halogen atom, (2) C_1-4alkyl group, (3) C_1-4alkoxy group, or (4) C_1-4halogenalkyl group ; cycle 1 represents cyclic group, selected from phenyl, C_4-7cycloalkyl and pyridinyl, which can be substituted with 1-2 substituents, each of which is independently selected from the group, consisting of (1) halogen atoms, (2) C_1-4alkyl groups, (3) C_1-4alkoxy groups and (5) C_1-4halogenalkyl groups, where in case of presence of two substituents in cycle 1 said substituents can form 4-7-membered cyclic group together with atoms in cycle 1, which said substituents are bound to, containing 2 oxygen atoms in cyclic group; cycle 2 represents 4-7-membered nitrogen-containing saturated heterocycle, which has from one to two substituents -K-R²; K represents -C(O)- (where left bond is connected with cycle 2); R² represents (2) C_2-4alkenyl or (3) C_2-4alkinyl group, each of which can be substituted with 1-2 substituents, each of which is independently selected from the group, consisting of (1) NR³R⁴, (2) halogen atoms, (3) CONR⁵R⁶, (4) CO₂R⁷ and (5) OR⁸; each of R³ and R⁴ independently represents (1) hydrogen atom or (2) (2) C_1-4alkyl group, which can have substituent OR⁹ or CONR¹⁰R¹¹; R³ and R⁴ together with nitrogen atom, they are bound to, can form 4-7-membered nitrogen-containing saturated heterocycle, which contains nitrogen atom and, optionally, one more heteroatom, selected from nitrogen, sulphur and oxygen, which can be substituted with oxo group or hydroxyl group; each of R⁵ and R⁶ independently represents (1) hydrogen atom; R⁷ represents (1) hydrogen atom or (2) C_1-4alkyl group; R⁸ represents (1) hydrogen atom, (2) C_1-4alkyl group or (4) benzotriazolyl group; R⁹ represents (1) hydrogen atom or (2) C_1-4alkyl group; each of R¹⁰ and R¹¹ independently represents (1) hydrogen atom; n represents 0 or 1; m represents integer number from 0 to 2.

EFFECT: invention relates to novel compounds of general formula (I), which possess Btk-selective inhibiting activity (Bruton's tyrosine kinase inhibitors).

15 cl, 3 tbl, 27 ex