| 摘要 |
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, -R, -R-R-R, -R-Ror -R-R; Rrepresents 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; Rrepresents -C(=O), -C(=O)NR; where Rrepresents H or lower alkyl; Rrepresents H or R; where Rrepresents 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; Yrepresents H, lower alkyl or lower halogenalkyl; each Yindependently 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; Yrepresents Y, Y, Yor Y; where Yrepresents H; Yrepresents lower alkyl, optionally substituted by one or sseveral substituents, selected from group, consisting of lower halogenalkyl, halogen; Yrepresents lower cycloalkyl, optionally substituted by one or some substituents, selected from group, consisting of lower alkyl, lower halogenalkyl, halogen; and Yrepresents 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 |
