NOVEL PYRIDINONES AND PYRIDAZINONES Russian patent published in 2014 - IPC C07D401/10 C07D401/14 A61K31/4725 A61P19/02 

FIELD: chemistry.

SUBSTANCE: invention relates to derivatives of 5-phenyl-1 H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one of general formulas I-III: , where: R represents H, -R¹, -R¹-R²-R³, -R¹-R³ or -R²-R³; R¹ represents heteroaryl, which stands for monocyclic radical, which contains 5-6 atoms in cycle and one or several heteroatoms N, optionally substituted by one or some lower alkyls; R² represents -C(=O), -C(=O)NR^2'; where R^2' represents H or lower alkyl; R³ represents H or R⁴; where R⁴ represents lower alkyl or heterocycloalkyl, which stands for monovalent saturated cyclic radical, consisting of one ring, which contains one or two ring-shaped heteroatoms, selected from N and O; X represents CH or N; Y¹ represents H, lower alkyl or lower halogenalkyl; each Y² independently represents lower alkyl, which is optionally substituted by one or several substituents, selected from group, which consists of hydroxygroup, lower alkoxygroup; n has value 0, 1, 2 or 4; Y³ represents Y^4a, Y^4b, Y^4c or Y^4d; where Y^4a represents H; Y^4b represents lower alkyl, optionally substituted by one or sseveral substituents, selected from group, consisting of lower halogenalkyl, halogen; Y^c represents lower cycloalkyl, optionally substituted by one or some substituents, selected from group, consisting of lower alkyl, lower halogenalkyl, halogen; and Y^4d represents aminogroup, optionally substituted by one or some lower alkyls; or to its pharmaceutically acceptable salt. Also described are: pharmaceutical composition, based on upper said compounds, as well as application of compounds of I-III formulas for treatment of inflammatory or autoimmune condition.

EFFECT: described are novel compounds, which can be useful for modulating Btk activity and treatment of diseases, associated with excess Btk activity.

14 cl, 102 ex, 1 tbl