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    PHOSPHORYLATED PYRONE ANALOGS AND METHODS
    2.
    发明申请
    PHOSPHORYLATED PYRONE ANALOGS AND METHODS 审中-公开

    公开(公告)号：US20100204089A1

    公开(公告)日：2010-08-12

    申请号：US12765580

    申请日：2010-04-22

    申请人： Wendye Robbins ,  Ving Lee

    发明人： Wendye Robbins ,  Ving Lee

    IPC分类号： A61K31/665 ,  A61K38/13 ,  A61P25/00 ,  A61P11/00 ,  A61P3/10

    CPC分类号： C07F9/65522 ,  A61K31/665 ,  C07F9/65744

    摘要： The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.

    Pyrone analogs for therapeutic treatment
    3.
    发明申请
    Pyrone analogs for therapeutic treatment 审中-公开
    吡喃类似物用于治疗

    公开(公告)号：US20100189653A1

    公开(公告)日：2010-07-29

    申请号：US12587704

    申请日：2009-10-09

    申请人： Wendye Robbins ,  Ving Lee ,  May Dean-Ming Lee

    发明人： Wendye Robbins ,  Ving Lee ,  May Dean-Ming Lee

    IPC分类号： A61K49/00 ,  A61K31/665 ,  A61P3/08 ,  A61P3/10

    CPC分类号： A61K31/352 ,  A61K31/661 ,  A61K31/665 ,  A61K45/06 ,  A61K2300/00

    摘要： Methods are described for the treatment and prevention of metabolic disorders or other diseases by administering a pyrone analog or a derivative thereof. Methods are also described for the treatment and prevention of metabolic disorders and other diseases by administering a pyrone analog, or a derivative thereof, in combination with one or more additional agents such as, for example, lipid lowering agents or glucose lowering agents. Methods are described for the modulation of lipid transporter activity to increase the efflux of lipid from a physiological compartment into an external environment. Methods disclosed herein may be used to assess treatment or prevention of a metabolic disorder following administration of a pyrone analog or a derivative thereof.

    摘要翻译： 描述了通过施用吡喃酮类似物或其衍生物来治疗和预防代谢紊乱或其它疾病的方法。 还描述了通过给予吡喃酮类似物或其衍生物与一种或多种另外的试剂例如降脂药或葡萄糖降低剂组合来治疗和预防代谢紊乱和其它疾病的方法。 描述了用于调节脂质转运蛋白活性以增加脂质从生理隔室进入外部环境的方法。 在给予吡喃酮类似物或其衍生物后，本文公开的方法可用于评估代谢紊乱的治疗或预防。

    PYRONE ANALOG COMPOSITIONS AND METHODS
    4.
    发明申请
    PYRONE ANALOG COMPOSITIONS AND METHODS 审中-公开
    吡喃类似物组合物和方法

    公开(公告)号：US20090258939A1

    公开(公告)日：2009-10-15

    申请号：US12182323

    申请日：2008-07-30

    申请人： Wendye Robbins ,  Ving Lee

    发明人： Wendye Robbins ,  Ving Lee

    IPC分类号： A61K31/352 ,  C07D311/28

    CPC分类号： C07D311/30

    摘要： Novel pyrone analogs are described which can enhance the effectiveness of a therapeutic agent when administered and/or reduce side effects caused by the administration of a therapeutic agent.

    摘要翻译： 描述了当施用和/或减少由施用治疗剂引起的副作用时可以增强治疗剂的有效性的新型吡喃酮类似物。

    N-terminally modified GLP-1 receptor modulators
    6.
    发明申请
    N-terminally modified GLP-1 receptor modulators 审中-公开
    N-末端修饰的GLP-1受体调节剂

    公开(公告)号：US20070021346A1

    公开(公告)日：2007-01-25

    申请号：US11442017

    申请日：2006-05-26

    申请人： William Ewing ,  Claudio Mapelli ,  Douglas Riexinger ,  Ving Lee ,  Richard Sulsky ,  Yeheng Zhu

    发明人： William Ewing ,  Claudio Mapelli ,  Douglas Riexinger ,  Ving Lee ,  Richard Sulsky ,  Yeheng Zhu

    IPC分类号： A61K38/10 ,  C07K7/08

    CPC分类号： C07K14/605 ,  A61K38/00

    摘要： The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

    摘要翻译： 本文所述的主题提供具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1）受体调节剂，因此可用于治疗或预防与GLP相关的疾病或病症 活动。 所述化合物包括化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。 这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。 所公开和要求保护的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

    Human glucagon-like-peptide-1 modulators and their use in treatment of diabetes and related conditions
    7.
    发明申请
    Human glucagon-like-peptide-1 modulators and their use in treatment of diabetes and related conditions 有权
    人胰高血糖素样肽-1调节剂及其在治疗糖尿病和相关病症中的应用

    公开(公告)号：US20060287242A1

    公开(公告)日：2006-12-21

    申请号：US11170968

    申请日：2005-06-30

    申请人： William Ewing ,  Claudio Mapelli ,  Richard Sulsky ,  Tasir Haque ,  Ving Lee ,  Douglas Riexinger ,  Rogelio Martinez ,  Yeheng Zhu

    发明人： William Ewing ,  Claudio Mapelli ,  Richard Sulsky ,  Tasir Haque ,  Ving Lee ,  Douglas Riexinger ,  Rogelio Martinez ,  Yeheng Zhu

    IPC分类号： A61K38/10 ,  C07K7/08

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K14/605

    摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

    摘要翻译： 本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症 。 此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。 这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。 本发明的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

    PHOSPHORYLATED PYRONE ANALOGS AND METHODS
    8.
    发明申请
    PHOSPHORYLATED PYRONE ANALOGS AND METHODS 审中-公开
    磷酸吡喃酮类似物和方法

    公开(公告)号：US20110028437A1

    公开(公告)日：2011-02-03

    申请号：US12856291

    申请日：2010-08-13

    申请人： Wendye Robbins ,  Ving Lee

    发明人： Wendye Robbins ,  Ving Lee

    IPC分类号： A61K31/665 ,  A61P25/00 ,  A61P15/00 ,  A61P13/12 ,  A61P1/16 ,  A61P3/10

    CPC分类号： A61K31/665 ,  C07F9/65522 ,  C07F9/65744

    摘要： The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.

    摘要翻译： 本发明涉及磷酸化多酚，磷酸化黄酮和磷酸化吡喃酮类似物。 描述了使用这种磷酸化化合物调节物质副作用的方法和组合物。 描述了用于调节血液 - 组织屏障（BTB）转运蛋白活性以增加药物和其它化合物从生理区室外流入外部环境的方法和组合物。 特别地，当磷酸化吡喃酮类似物与治疗剂共同施用时，本文公开的方法和组合物提供降低的副作用。