| 摘要 |
FIELD: medicine.SUBSTANCE: present invention refers to compounds having formula IIIsuch as below, wherein: Q represents C(Y) or N; R represents H, -R, -R-R-R, -R-Ror -R-R; Rrepresents heteroaryl or heterocyclyl each of which is optionally substituted by one or more Calkyls, hydroxyCalkyls, oxogroups or halogenCalkyls; Rrepresents -C(=O), -O, -C(R), -C(R)C(=O), -C(R)C(=O)NR, C(R)N(R)C(=O), -C(=NH), -C(R)NRor -S(=O); each Rindependently represents H or Calkyl; Rrepresents H or R; Rrepresents Calkyl, Calkoxygroup, aminogroup, Calkylaminogroup, di(Calkyl)aminogroup, heterocyclyl, Calkylheterocycloalkyl, heterocycloalkylCalkyl each of which is optionally substituted by one or more Calkyls, Calkylaminogroups, di(Calkyl)aminogroups, hydroxygroups, hydroxyCalkyls, Calkoxygroups, oxogroups or halogenCalkyls; 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 |
