BERTHEL STEVEN JOSEPH,FISHLOCK DANIEL,LOU YAN,OWENS TIMOTHY D,SWEENEY ZACHARY KEVIN,FIROOZNIA FARIBORZ,HONG JUN-BAE,LUCAS MATTHEW C,SARMA KESHAB,TAYGERLY JOSHUA PAUL GERGELY
申请号：
ZA201301679
公开号：
ZA201301679B
申请日:
2013.03.05
申请国别(地区):
ZA
年份:
2015
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&prime；, Y1, Y2, Y2&prime；, 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.
