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    METHODS FOR THE SYNTHESIS OF SUBSTITUTED PURINES
    2.
    发明公开
    METHODS FOR THE SYNTHESIS OF SUBSTITUTED PURINES 审中-公开
    合成取代嘌呤的方法

    公开(公告)号：EP1529048A2

    公开(公告)日：2005-05-11

    申请号：EP02801053.6

    申请日：2002-10-12

    申请人： IRM LLC ,  The Scripps Research Institute

    发明人： DING, Sheng ,  DING, Qiang ,  GRAY, Nathanael, S. ,  SCHULTZ, Peter, G.

    IPC分类号： C07D473/16 ,  C07D473/40 ,  C07D473/18

    CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D473/40

    摘要： The invention provides general methods for preparing 2,9-, 2,6,9-, O6-aryl- and O6-alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.

    摘要翻译： 本发明提供了以组合和无痕方式制备2,9-，2,6,9-，O6-芳基 - 和O6-烷基取代的嘌呤的一般方法。 在一些实施方案中，所述方法包括在N9处用溶液中的醇对2-氟-6-苯基亚磺酰嘌呤进行Mitsunobu烷基化，然后用树脂结合的胺C2-俘获嘌呤核心并随后氧化和置换C6磺酰基 与胺和苯胺。

    COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
    8.
    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.