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    METHODS FOR BLOCKING CELL PROLIFERATION AND TREATING DISEASES AND CONDITIONS RESPONSIVE TO CELL GROWTH INHIBITION
    4.
    发明申请
    METHODS FOR BLOCKING CELL PROLIFERATION AND TREATING DISEASES AND CONDITIONS RESPONSIVE TO CELL GROWTH INHIBITION 审中-公开
    阻断细胞增殖和治疗细胞生长抑制的疾病和病症的方法

    公开(公告)号：US20130266636A1

    公开(公告)日：2013-10-10

    申请号：US13816218

    申请日：2011-08-12

    申请人： David Cheresh ,  Eric Murphy ,  Ainhoa Mielgo

    发明人： David Cheresh ,  Eric Murphy ,  Ainhoa Mielgo

    IPC分类号： A61K31/506

    CPC分类号： A61K31/506 ,  A61K31/4164 ,  A61K31/4196

    摘要： In alternative embodiments, the invention provides methods for regulating or modulating RAF kinases. In alternative embodiments, the invention provides methods for ameliorating, preventing and/or treating diseases, infections and/or conditions having unwanted, pathological or aberrant cell proliferation, or that are responsive to inhibition or arrest of cell growth, by administration of an allosteric RAF inhibitor and/or any agent which prevents localization of RAF to mitotic spindles or mid-bodies.

    摘要翻译： 在替代实施方案中，本发明提供了调节或调节RAF激酶的方法。 在替代实施方案中，本发明提供了通过施用变构的RAF来改善，预防和/或治疗具有不想要的，病理学或异常细胞增殖或对抑制或阻止细胞生长有反应的疾病，感染和/或病症的方法 抑制剂和/或阻止RAF定位于有丝分裂心轴或中间体的任何药剂。

    PROTEIN KINASE MODULATING COMPOUNDS AND METHODS FOR MAKING AND USING THEM
    7.
    发明申请
    PROTEIN KINASE MODULATING COMPOUNDS AND METHODS FOR MAKING AND USING THEM 审中-公开
    蛋白激酶调节化合物及其制备和使用方法

    公开(公告)号：US20100209488A1

    公开(公告)日：2010-08-19

    申请号：US12602759

    申请日：2008-07-15

    申请人： Wolfgang Wrasidlo ,  Eric Murphy ,  David Cheresh

    发明人： Wolfgang Wrasidlo ,  Eric Murphy ,  David Cheresh

    IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61K9/127 ,  A61K9/14 ,  C12N9/99 ,  A61P35/00 ,  A61P9/00 ,  A61P25/00 ,  A61P3/10 ,  A61P29/00 ,  A61P9/12 ,  A61P35/02 ,  A61P35/04

    CPC分类号： C07D403/12

    摘要： The invention provides compositions, e.g., small molecules, that disrupt the activity of protein kinases, including constitutively activated protein kinases, such as kinases constitutively activated through mutations, and kinases in their native inactivated state, and methods for making and using them. In one aspect, compositions of the invention bind a protein kinase in its inactive conformation involving the conserved asparagine-phenylalanine-glycine residue motif, or “Asp-Phe-Gly” or “DFG” motif, of the activation loop in the allosteric binding site. The small molecule protein kinase inhibitors of the invention comprise or are derivatives or analogs of oxadiazoles, thiadiazoles, oxazoles, thiazoles, arylamides, quinolones, pyrazoles, pyrazolones, imides, pyrolles, imidazoles and/or triazoles.

    摘要翻译： 本发明提供了破坏蛋白激酶（包括组成型激活的蛋白激酶）的组合物，例如小分子，例如通过突变组成型激活的激酶，以及其天然失活状态的激酶，以及制备和使用它们的方法。 在一个方面，本发明的组合物结合涉及保守的天冬酰胺 - 苯丙氨酸 - 甘氨酸残基基序的无活性构象的蛋白激酶或者在变构结合位点中的活化环的“Asp-Phe-Gly”或“DFG”基序 。 本发明的小分子蛋白激酶抑制剂包含恶二唑，噻二唑，恶唑，噻唑，芳基酰胺，喹诺酮，吡唑，吡唑啉酮，酰亚胺，吡咯烷，咪唑和/或三唑的衍生物或类似物。