NOVEL PHENYLPYRAZINONES AS KINASE INHIBITORS Russian patent published in 2014 - IPC C07D403/10 C07D403/14 C07D413/14 C07D417/14 C07D401/14 C07D405/14 A61K31/4725 A61K31/497 A61P37/00 A61P29/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and specifically to 5-phenyl-1H-pyrazin-2-one derivatives of general formula II or pharmaceutically acceptable salts thereof, where R denotes -R¹ or - R¹-R²-R³; R¹ denotes aryl or heteroaryl, and is optionally substituted with one or two R^1'; where each R^1' independently denotes C_1-6alkyl, halogen or C_1-6halogenalkyl; R² denotes -C(=O), -CH₂-; R³ denotes R⁴; where R⁴ denotes an amino group or heterocycloalkyl, and is optionally substituted with one or two substitutes selected from C_1-6alkyl, hydroxy group, oxo group, C_1-6hydroxyalkyl, C_1-6alkoxy group; Q denotes CH₂; Y¹ denotes C_1-6alkyl; Y² denotes Y^2b; where Y^2b denotes C_1-6alkyl, optionally substituted with one Y^2b'; where Y^2b' denotes a hydroxy group, n and m are equal to 0; Y⁴ denotes Y^4c or Y^4d; where Y^4c denotes lower cycloalkyl, optionally substituted with halogen; and Y^4d denotes an amino group, optionally substituted with one or more C_1-6alkyl; where "aryl" denotes phenyl or naphthyl, "heteroaryl" denotes a monocyclic or bicyclic radical containing 5 to 9 atoms in the ring, which contains at least one aromatic ring containing 5 to 6 atoms in the ring, with one or two N or O heteroatoms, wherein the remaining atoms in the ring are carbon atoms, under the condition that the binding point of the heteroaryl radical is in the aromatic ring, "heterocycloalkyl" denotes a monovalent saturated cyclic radical consisting of one ring containing 5 to 6 atoms in the ring, with one or two ring heteroatoms selected from N, O or SO₂. The invention also relates to use of the compound of formula II or a pharmaceutical composition based on the compound of formula II.

EFFECT: obtaining novel compounds that are useful for modulating Btk activity and treating diseases associated with excessive activity of Btk.

7 cl, 2 tbl, 53 ex