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    Methods and compositions useful for inhibition of alpha v beta 5 mediated angiogenesis
    2.
    发明申请
    Methods and compositions useful for inhibition of alpha v beta 5 mediated angiogenesis 审中-公开
    用于抑制αvβ5介导的血管生成的方法和组合物

    公开(公告)号：US20060165703A1

    公开(公告)日：2006-07-27

    申请号：US11290896

    申请日：2005-11-29

    申请人： Peter Brooks ,  David Cheresh ,  Martin Friedlander

    发明人： Peter Brooks ,  David Cheresh ,  Martin Friedlander

    IPC分类号： A61K39/395 ,  A61K39/00 ,  C07K14/82 ,  C07K16/30

    CPC分类号： A61K38/57 ,  A61K2039/505 ,  C07K16/2839 ,  C07K16/2848 ,  C07K2317/76

    摘要： The present invention describes methods for inhibiting angiogenesis in tissues using vitronectin αvβ5 antagonists. The αvβ5-mediated angiogenesis is correlated with exposure to cytokines including vascular endothelial growth factor, transforming growth factor-α and epidermal growth factor. Inhibition of αvβ5-mediated angiogenesis is particularly preferred in vascular endothelial ocular neovascular diseases, in tumor growth and in inflammatory conditions, using therapeutic compositions containing αvβ5 antagonists.

    摘要翻译： 本发明描述了使用玻连蛋白α5β5拮抗剂抑制组织中血管生成的方法。 α-β5介导的血管发生与包括血管内皮生长因子，转化生长因子-α和表皮生长因子在内的细胞因子的暴露相关。 使用含有αV的治疗组合物，在血管内皮细胞新生血管疾病，肿瘤生长和炎性病症中，对α5β5介导的血管生成的抑制是特别优选的 5β拮抗剂。

    METHODS FOR BLOCKING CELL PROLIFERATION AND TREATING DISEASES AND CONDITIONS RESPONSIVE TO CELL GROWTH INHIBITION
    5.
    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。

    Method of treatment of myocardial infarction
    7.
    发明申请
    Method of treatment of myocardial infarction 审中-公开
    心肌梗死的治疗方法

    公开(公告)号：US20060258686A1

    公开(公告)日：2006-11-16

    申请号：US10535325

    申请日：2003-11-18

    申请人： David Cheresh ,  Robert Paul ,  Brian Eliceiri

    发明人： David Cheresh ,  Robert Paul ,  Brian Eliceiri

    IPC分类号： A61K31/519

    CPC分类号： A61K31/519 ,  A01K67/0271 ,  A61K38/45 ,  A61K48/00

    摘要： Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof. The Src family tyrosine kinase inhibitors can be used to prepare medicaments for the treatment of myocardial infarction. Also disclosed are articles of manufacture containing a chemical Src family tyrosine kinase inhibitor.

    摘要翻译： 通过向哺乳动物施用治疗有效量的化学品Src家族酪氨酸激酶蛋白抑制剂和这种抑制剂化合物用于制备用于治疗心肌梗塞的药物的用途来治疗哺乳动物的心肌梗死。 可以通过向哺乳动物施用预防量的抑制剂来防止心肌梗死。 抑制剂优选是Src蛋白的抑制剂，其选自吡唑并嘧啶类Src家族酪氨酸激酶抑制剂，大环二烯酮类Src家族酪氨酸激酶抑制剂，吡啶并[2,3-d]嘧啶类Src家族酪氨酸激酶抑制剂 ，4-苯胺基-3-喹啉甲腈类Src家族酪氨酸激酶抑制剂及其混合物。 Src家族酪氨酸激酶抑制剂可用于制备用于治疗心肌梗死的药物。 还公开了含有化学Src家族酪氨酸激酶抑制剂的制品。

    PROTEIN KINASE MODULATING COMPOUNDS AND METHODS FOR MAKING AND USING THEM
    10.
    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。