发明名称 Inhibitors of Bruton's tyrosine kinase
摘要 This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.
申请公布号 US8299077(B2) 申请公布日期 2012.10.30
申请号 US20100711312 申请日期 2010.02.24
申请人 BERTHEL STEVEN;FIROOZNIA FARIBORZ;FISHLOCK DANIEL;HONG JUN-BAE;LOU YAN;LUCAS MATTHEW;OWENS TIMOTHY D.;SARMA KESHAB;SWEENEY ZACHARY KEVIN;TAYGERLY JOSHUA PAUL GERGELY;ROCHE PALO ALTO LLC 发明人 BERTHEL STEVEN;FIROOZNIA FARIBORZ;FISHLOCK DANIEL;HONG JUN-BAE;LOU YAN;LUCAS MATTHEW;OWENS TIMOTHY D.;SARMA KESHAB;SWEENEY ZACHARY KEVIN;TAYGERLY JOSHUA PAUL GERGELY
分类号 A61K31/502;C07D237/32 主分类号 A61K31/502
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