申请人:ELI LILLY AND COMPANY
公开号:EP1609789A1
公开(公告)日:2005-12-28
The present invention provides kinase inhibitors of Formula I:
wherein:
R1 is hydrogen, methyl, or tolyl;
W is piperidinyl, napthyl, or phenyl optionally substituted with halo;
X is a bond, -CH2-, -O-(CH2)n-, -O-, or -C(O)-;
n is 1 or 2;
Y is phenyl, piperidinyl, or piperazinyl;
Z is -C(O)-R2, -CH2-R3, or methylsulfonyl;
R2 is C1-C4 alkyl, C1-C4 alkoxy, benzyloxy, C3-C5 cycloalkyl optionally substituted with phenyl, pyridyl optionally substituted with 1-2 C1-C4 alkoxy or 1-2 halo, thienyl optionally substituted with halo or C1-C4 alkyl, pyrrolyl, imidazolyl, pyrazolyl optionally substituted with C1-C4, alkyl, or phenyl optionally substituted from the group selected from trifluoromethyl, trifluoromethoxy, and 1-2 halo, and
R3 is pyridyl;
or a pharmaceutically acceptale salt thereof.
本发明提供了化合物I的激酶
抑制剂:
其中:
R1为氢、甲基或
甲苯基;
W为
哌啶基、
萘基或苯基,可选择地取代为卤素;
X为键、-
CH2-、-O-( )n-、-O-或-C(O)-;
n为1或2;
Y为苯基、
哌啶基或
哌嗪基;
Z为-C(O)-R2、- -R3或甲磺酰基;
R2为C1-C4烷基、C1-C4烷氧基、苄氧基、C3-C5环烷基,可选择地取代为苯基,
吡啶基,可选择地取代为1-2个C1-C4烷氧基或1-2个卤素,
噻吩基,可选择地取代为卤素或C1-C4烷基,
吡咯基,
咪唑基,
吡唑基,可选择地取代为C1-C4烷基,或苯基,可选择地取代为三
氟甲基,三
氟甲氧基和1-2个卤素中选择的一种,以及
R3为
吡啶基;
或其药学上可接受的盐。