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    COMPOUNDS THAT MODULATE THE ACTIVITY OF PTP-1B AND TC-PTP
    4.
    发明公开
    COMPOUNDS THAT MODULATE THE ACTIVITY OF PTP-1B AND TC-PTP 审中-公开
    化合物FOR PTP-1B和TC-PTP的调节活性，

    公开(公告)号：EP1534264A2

    公开(公告)日：2005-06-01

    申请号：EP03713729.6

    申请日：2003-02-26

    申请人： Sunesis Pharmaceuticals, Inc.

    发明人： BARR, Kenneth ,  FAHR, Bruce ,  HANSEN, Stig ,  WIESMANN, Christian

    IPC分类号： A61K31/343 ,  C07D307/80

    CPC分类号： C07D405/12 ,  A61K31/343 ,  A61K31/635 ,  C07D307/80 ,  C07D417/12

    摘要： The present invention relates to a new and improved method for treating diabetes and or its associated complications by modulating the activity of protein tryosin phosphatase 1B (“PTP-1B”). The inventive compounds modulate the activity PTP-1B by binding to a novel binding site referred herein as the PTP-1B exosite that is distal to the active site of PTP-1B. The present invention also relates to a new and improved method of treating immune system disorders by modulating the activity of T-cell protein tyrosine phosphatase (“TC-PTP”). The inventive compound modulate the activity of TC-PTP by binding to a novel binding site referred herein as the TC-PTP exosite that is distal to the active site of PTP-1B.

    METHODS OF CHEMOTYPE EVOLUTION
    5.
    发明公开
    METHODS OF CHEMOTYPE EVOLUTION 有权
    程序对CHEMO式发展

    公开(公告)号：EP2257637A1

    公开(公告)日：2010-12-08

    申请号：EP09724229.1

    申请日：2009-03-25

    申请人： Sunesis Pharmaceuticals, Inc.

    发明人： HANSEN, Stig ,  ERLANSON, Dan ,  CANCILLA, Mark

    IPC分类号： C12Q1/48 ,  G01N33/531 ,  C40B50/04 ,  C40B30/04

    CPC分类号： G01N33/531 ,  C12Q1/485

    摘要： Herein is described a method to rapidly screen a large chemical space for a compound that binds to a target protein through an iterative fragment assembly approach that can be performed at low reagent cost and without requiring purification of the assembled product. The method employs a library of test ligands each of which comprise a 'bait' molecule, which is known from prior art or prior screening to have some intrinsic affinity for the target protein, and a test moiety.