DANIEL FISHLOCK,FARIBORZ FIROOZNIA,JOSHUA PAUL GERGELY TAYGERLY,JUN-BAE HONG,KESHAB SARMA,MATTHEW C. LUCAS,STEVEN JOSEPH BERTHEL,TIMOTHY D. OWENS,YAN LOU,ZACHARY KEVIN SWEENEY
申请号:
BRPI1009112
公开号:
BRPI1009112A2
申请日:
2010.02.25
申请国别(地区):
BR
年份:
2016
代理人:
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.