CRAWFORD, James John,ORTWINE, Daniel Fred,WEI, BinQing,YOUNG, Wendy B.
申请号：
RSP20160001
公开号：
RS54505B1
申请日:
2012.11.02
申请国别(地区):
RS
年份:
2016
代理人:
摘要：
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X 1 , X 2 , and X 3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Jedinjenje odabrano od Formula I:ili stereoizomeri, tautomeri ili njihove farmaceutski prihvatljive soli, gde:X1 je CR1 ili N；X2 je CR2 ili N；X3 je CR3 ili N；pri čemu, jedan ili dva od X1, X2 i X3 su N；R1, R2 i R3 su nezavisno odabrani od: H, F, Cl, -NH2, -NHCH3, -N(CH3)2, -OH, -OCH3, -OCH2CH3, -OCH2CH2OH i C1-C3 alkila；R4 je odabran od 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, ciklopropila, ciklopropilmetila, 1-hidroksiciklopropila, imidazolila, pirazolila, 3-hidroksi-oksetan-3-ila, oksetan-3-ila i azetidin-1-ila；R5 je eventualno supstituisani C6-C20 aril, C3-C12 karbociklil, C2-C20 heterociklil, C1-C20 heteroaril, -(C6-C20 aril)-(C2-C20 heterociklil), -(C1-C20 heteroaril)-(C2-C20 heterociklil), -( C1-C20 heteroaril)-(C2-C20 heterociklil)-(C2-C20 heterociklil), -(C1-C20 heteroaril)-(C2-C20 heterociklil)-(C1-C6 alkil), -(C1-C20 heteroaril)-( C1-C6 alkil), -(C2-C20 heterociklil)-(C1-C6 alkil), -(C2-C20 heterociklil)-(C3-C12 karbociklil), -( C1-C20 heteroaril)-(C3-C12 karbociklil), ili -( C1-C20 heteroaril)-C(=O)-(C2-C20 heterociklil)；R6 je H, -CH3, -CH2CH3, -CH2CH2OH, -CHF2, -NH2, ili -OH；R7 je odabran od struktura:gde talasaste linije pokazuju položaj vezivanja； iY1 i Y2 su nezavisno odabrani od CH i N, gde Y1 i Y2 nisu svaki N；gde su alkil, karbociklil, heterociklil, aril i heteroaril eventualno supstituisani
