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    Human glucagon-like-peptide-1 modulators and their use in treatment of diabetes and related conditions
    1.
    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。

    N-terminally modified GLP-1 receptor modulators
    4.
    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。

    N-TERMINALLY MODIFIED GLP-1 RECEPTOR MODULATORS
    5.
    发明申请
    N-TERMINALLY MODIFIED GLP-1 RECEPTOR MODULATORS 有权
    N-末端修饰的GLP-1受体调节剂

    公开(公告)号：US20080045461A1

    公开(公告)日：2008-02-21

    申请号：US11753616

    申请日：2007-05-25

    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： A61K38/08 ,  A61P3/00 ,  C07D213/04 ,  C07K7/06

    CPC分类号： A61K33/30 ,  A61K33/26 ,  A61K33/32 ,  A61K38/08 ,  A61K38/26 ,  A61K45/06 ,  C07K14/605 ,  A61K2300/00

    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 may 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。 所述化合物包括可刺激II型糖尿病患者胰岛素分泌的化学修饰的肽，但也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。