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    Small molecule antagonists of phosphatidylinositol-3,4,5-triphosphate (PIP3) and uses thereof
    1.
    发明授权
    Small molecule antagonists of phosphatidylinositol-3,4,5-triphosphate (PIP3) and uses thereof 有权
    磷脂酰肌醇-3,4,5-三磷酸（PIP3）的小分子拮抗剂及其用途

    公开(公告)号：US09040585B2

    公开(公告)日：2015-05-26

    申请号：US14103412

    申请日：2013-12-11

    Applicant: Tufts University ,  Council of Scientific and Industrial Research

    Inventor： Alexei Degterev ,  Chepuri Venkata Ramana ,  Benchun Miao

    IPC: A01N47/28 ,  A61K31/17 ,  C07C335/26 ,  A61K9/107 ,  C07C275/54 ,  A61K9/00

    CPC classification number: C07C335/26 ,  A61K9/0019 ,  A61K9/1075 ,  A61K31/17 ,  C07C275/54

    Abstract: Disclosed are new members of a class of non-lipid small molecule inhibitors which interfere with the interaction between phosphoinositol-3,4,5-triphosphate (PIP3) and pleckstrin homology (PH) domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo, with improved activity and selectivity toward particular PH domains. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL and with other Akt inhibitors in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided.

    Abstract translation: 公开了一类干扰磷酸肌醇-3,4,5-三磷酸（PIP3）和pleckstrin同源性（PH）结构域之间相互作用的非脂质小分子抑制剂的新成员。 这些分子在体外靶向广泛的PIP3依赖性信号传导事件，并在体内发挥显着的抗肿瘤活性，具有改善的对特定PH结构域的活性和选择性。 本发明的小分子抑制剂可以单独使用或与肿瘤坏死因子（TNF）相关的凋亡诱导配体（TRAIL）或其他癌症药物一起用于治疗癌症。 本发明的小分子抑制剂与TRAIL和其它Akt抑制剂协同治疗癌症协同作用。 提供了治疗癌症的药物组合物和方法。

    Small Molecule Antagonists of Phosphatidylinositol-3,4,5-Triphosphate (PIP3) and Uses Thereof
    3.
    发明申请
    Small Molecule Antagonists of Phosphatidylinositol-3,4,5-Triphosphate (PIP3) and Uses Thereof 有权
    磷脂酰肌醇-3,4,5-三磷酸（PIP3）的小分子拮抗剂及其用途

    公开(公告)号：US20140187639A1

    公开(公告)日：2014-07-03

    申请号：US14103412

    申请日：2013-12-11

    Applicant: Council of Scientific and Industrial Research ,  Tufts University

    Inventor： Alexei Degterev ,  Chepuri Venkata Ramana ,  Benchun Miao

    IPC: C07C335/26 ,  C07C275/54

    CPC classification number: C07C335/26 ,  A61K9/0019 ,  A61K9/1075 ,  A61K31/17 ,  C07C275/54

    Abstract: Disclosed are new members of a class of non-lipid small molecule inhibitors which interfere with the interaction between phosphoinositol-3,4,5-triphosphate (PIP3) and pleckstrin homology (PH) domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo, with improved activity and selectivity toward particular PH domains. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL and with other Akt inhibitors in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided.

    Abstract translation: 公开了一类干扰磷酸肌醇-3,4,5-三磷酸（PIP3）和pleckstrin同源性（PH）结构域之间相互作用的非脂质小分子抑制剂的新成员。 这些分子在体外靶向广泛的PIP3依赖性信号传导事件，并在体内发挥显着的抗肿瘤活性，具有改善的对特定PH结构域的活性和选择性。 本发明的小分子抑制剂可以单独使用或与肿瘤坏死因子（TNF）相关的凋亡诱导配体（TRAIL）或其他癌症药物一起用于治疗癌症。 本发明的小分子抑制剂与TRAIL和其它Akt抑制剂协同治疗癌症协同作用。 提供了治疗癌症的药物组合物和方法。

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