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    PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF
    2.
    发明公开
    PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF 审中-公开
    蛋白激酶抑制剂和使用方法

    公开(公告)号：EP2076128A2

    公开(公告)日：2009-07-08

    申请号：EP07841388.7

    申请日：2007-08-27

    申请人： IRM LLC

    发明人： MI, Yuan ,  ALBAUGH, Pamela A.

    IPC分类号： A01N43/00 ,  A61K31/33

    CPC分类号： C07D403/14 ,  C07D405/14 ,  C07D413/14

    摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC , Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof.

    COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
    7.
    发明公开
    COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
    化合物和组合物作为蛋白激酶抑制剂

    公开(公告)号：EP1981870A2

    公开(公告)日：2008-10-22

    申请号：EP07717222.9

    申请日：2007-02-06

    申请人： IRM LLC

    发明人： DING, Qiang ,  REN, Pingda ,  ZHANG, Qiong ,  WANG, Xia ,  SIM, Taebo ,  ALBAUGH, Pamela A. ,  GRAY, Nathanael S.

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/4468

    CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particulary diseases or disorders that involve abnormal activation of the Abl.Bcr-Abl, Bmx, b-RAF, c-RAFI c-SRC,KDR,CSKlFGFR3,JAK2ILck,Met,PKCalpha,SAPK2alpha)Tie2,TrkB and P70S6K kinases. These compounds have the following structure: (Formula I); in which: R1 is selected from -NR6R7 and -NR6C(O)R8; wherein R6 is selected from hydrogen and C1-6alkyl; R7 is selected from hydrogen, C1-6alkyl. -NR9R10, C6-10aryl-C0-4alkyl, C1-10heteroaryl-C0-4alkyl, C3-12cycloalkyl-C0-4alkyl and C3-8heterocycloalkyl-C0-4alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R7 can be optionally substituted by 1 to 3 radicals independently selected from C1-6alkyl, C1-6alkoxy, -QNR9R10 and C3-8heterocycloalkyl-C0-4alkyl; wherein Q is selected from a bond and C1-4alkylene; R8 is selected from hydrogen and C1-4alkyl; R9 and R10 are independently selected from hydrogen and C1-6alkyl; R2 is selected from hydrogen and C1-6alkyl; R3 is selected from hydrogen and C1-6alkyl; R4 is selected from hydrogen, halo, C1-6alkyl, C1-6alkoxy, halosubstituted-C1-6alkyl and halosubsb'tuted-C1-6alkoxy; R5 is selected from -C(O)NHR11 and -NHC(O)R11; wherein R11 is selected from C6-10aryl and C1-10heteroaryl; wherein any aryl or heteroaryl of R11 is optionally substituted with 1 to 3 radicals independently selected from halo, C1-6alkyl, C1-6alkoxy, halosubstituted-C1-6alkyl, halosubstituted-C1-6alkoxy, di-C1-4alkyl-amino-C1-6alkoxy, di-C1-4alkyl-amino-C1-4alkyl(C1-4alkyl)amino, C1-10heteroaiyl-C0-4alkyl, C3-8heterocycIoalkyl-C0-4alkyl and C3-8heterocycloalkyl-oxy; wherein any heteroaryl or heterocycloalkyl substituent of R11 is further optionally substituted by 1 to 2 radicals independently selected from C1-6alkyl and hydroxy-C1-6alkyl; X and Y are independently selected from N and CH; and the pharmaceutically acceptable salts, hydrates, solvates and isomers thereof.