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Heteroaryl pyridone and aza-pyridone compounds as inhibitors of Btk activity
- 专利权人:
- F. Hoffmann-La Roche AG
- 发明人:
- CRAWFORD, James John,ORTWINE, Daniel Fred,WEI, BinQing,YOUNG, Wendy B.
- 申请号：
- ES12783837
- 公开号：
- ES2555168T3
- 申请日:
- 2012.11.02
- 申请国别(地区):
- ES
- 年份:
- 2015
- 代理人:
- 摘要：
- A compound selected from Formula I: ** Formula ** or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein: X1 is CR1 or N； X2 is CR2 or N； X3 is CR3 or N； where one or two of X1, X2, and X3 are N； R1, R2 and R3 are independently selected from H, F, Cl, -NH2, -NHCH3, -N (CH3) 2, -OH, -OCH3, -OCH2CH3, -OCH2CH2OH, and C1-C3 alkyl； R4 is selected from H, F, Cl, CN, -CH2OH, -CH (CH3) OH, -C (CH3) 2OH, -CH (CF3) OH, -CH2F, -CHF2, -CH2CHF2, -CF3, -C (O) NH2, -C (O) NHCH3, -C (O) N (CH3) 2, -NH2, -NHCH3, -N (CH3) 2, -NHC (O) CH3, -OH, -OCH3, - OCH2CH3, - OCH2CH2OH, cyclopropyl, cyclopropylmethyl, 1-hydroxycyclopropyl, imidazolyl, pyrazolyl, 3-hydroxy-oxetan-3-yl, oxetan-3-yl, and azetidin-1-yl； R5 is C6-C20 aryl, C3-C12 carbocyclyl, C2-C20 heterocyclyl, C1-C20 heteroaryl, - (C6-C20 aryl) - (C2-C20 heterocyclyl), - (C1-C20 heteroaryl) - (C2-C20 heterocyclyl ), - (C1-C20 heteroaryl) - (C2-C20 heterocyclyl) - (C2-C20 heterocyclyl), - (C1-C20 heteroaryl) - (C2-C20 heterocyclyl) - (C1-C6 alkyl), - (C1 heteroaryl -C20) - (C1-C6 alkyl), - (heterocyclyl C2-C20) - (C1-C6 alkyl), - (heterocyclyl C2-C20) - (carbocyclyl C3-C12), - (heteroaryl C1-C20) - ( C3-C12 carbocyclyl), or - (C1-C20 heteroaryl) - C (>； = O) - (C2-C20 heterocyclyl), optionally substituted； R6 is H, -CH3, -CH2CH3, -CH2CH2OH, -CHF2, -NH2, or -OH； R7 is selected from the structures: where the wavy line indicates the junction site； and Y1 and Y2 are independently selected from CH and N, where Y1 and Y2 are not each N； wherein the alkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from F, Cl, Br, I, -CN, -CH3, -CH2CH3, -CH (CH3) 2, -CH2CH ( CH3) 2, - CH2OH, -CH2OCH3, -CH2CH2OH, -C (CH3) 2OH, -CH (OH) CH (CH3) 2, -C (CH3) 2CH2OH, -CH2CH2SO2CH3, - CH2OP (O) (OH) 2 , -CH2F, -CHF2, -CF3, -CH2CF3, -CH2CHF2, -CH (CH3) CN, -C (CH3) 2CN, -CH2CN, -CO2H, -COCH3, -CO2CH3, -CO2C (CH3) 3, - COCH (OH) CH3, -CONH2, -CONHCH3, -CON
- 来源网站：
- 中国工程科技知识中心
- 来源网址：
- http://www.ckcest.cn/home/
