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    Method of identifying inhibitors of Lck
    5.
    发明授权
    Method of identifying inhibitors of Lck 有权
    鉴定Lck抑制剂的方法

    公开(公告)号：US07400979B2

    公开(公告)日：2008-07-15

    申请号：US10212346

    申请日：2002-08-05

    申请人： David W. Borhani ,  David Calderwood ,  Richard W. Dixon ,  Gavin C. Hirst ,  Peter Hrnciar ,  Andreas Loew ,  Adelaine Leung ,  Kurt Ritter

    发明人： David W. Borhani ,  David Calderwood ,  Richard W. Dixon ,  Gavin C. Hirst ,  Peter Hrnciar ,  Andreas Loew ,  Adelaine Leung ,  Kurt Ritter

    IPC分类号： G06F17/11 ,  G06F17/50 ,  G06F19/00

    CPC分类号： C12N9/1205 ,  C07K2299/00

    摘要： The present invention relates to polypeptides which comprise the ligand binding domain of Lck, crystalline forms of these polypeptides, and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Lck. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential selective inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain selectively.

    摘要翻译： 本发明涉及包含Lck的配体结合结构域，这些多肽的结晶形式的多肽，以及这些结晶形式用于确定Lck催化结构域的三维结构的多肽。 本发明还涉及在设计和/或鉴定Lck活性的潜在抑制剂的方法中单独或与抑制剂复合的Lck催化结构域的三维结构的用途，例如抑制结合的化合物 天然底物到Lck催化结构域。 本发明还涉及在设计和/或鉴定Lck活性的潜在选择性抑制剂的方法中单独或与抑制剂复合的Lck催化结构域的三维结构的用途，例如抑制Lck活性结合的化合物 选择性地对Lck催化结构域的天然底物。

    Indole derivatives as factor Xa inhibitors
    10.
    发明授权
    Indole derivatives as factor Xa inhibitors 有权
    吲哚衍生物作为因子Xa抑制剂

    公开(公告)号：US07196103B2

    公开(公告)日：2007-03-27

    申请号：US10848743

    申请日：2004-05-19

    申请人： Marc Nazare ,  Volkmar Wehner ,  Kurt Ritter ,  Volker Laux

    发明人： Marc Nazare ,  Volkmar Wehner ,  Kurt Ritter ,  Volker Laux

    IPC分类号： A61K31/44 ,  A61K31/445 ,  C07D413/00 ,  C07D401/00 ,  C07D211/68

    CPC分类号： C07D413/14

    摘要： The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.

    摘要翻译： 本发明涉及可用于抑制因子Xa的活性的式I化合物。 本发明还涉及含有所述化合物的组合物，其制备方法，其用途，例如用于抑制凝血酶的形成或用于治疗或预防性治疗患有或与疾病状态相关的患者或与之相关的患者 伴有心血管疾病。