Pituitary adenylate cyclase activating peptide (PACAP)receptor 3 (R3) agonists and their pharmacological methods of use
    23.
    发明授权
    Pituitary adenylate cyclase activating peptide (PACAP)receptor 3 (R3) agonists and their pharmacological methods of use 失效
    垂体腺苷酸环化酶活化肽(PACAP)受体3(R3)激动剂及其药理学用途

    公开(公告)号:US06972319B1

    公开(公告)日:2005-12-06

    申请号:US09671773

    申请日:2000-09-27

    摘要: This invention provides novel peptides that function in vivo to stimulate insulin release from pancreatic beta cells in a glucose-dependent fashion. These insulin secretagogue peptides are shown to stimulate insulin release in rat islet cells in vitro, and in vivo. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VIP/PACAP-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.

    摘要翻译: 本发明提供了新的肽,其在体内起作用以以葡萄糖依赖的方式刺激胰腺β细胞的胰岛素释放。 这些胰岛素促分泌肽显示能够在体外和体内刺激大鼠胰岛细胞中的胰岛素释放。 本发明的肽为具有降低的内源性胰岛素分泌的患者特别是2型糖尿病患者提供了新的疗法。 特别地,本发明是选自VIP / PACAP相关多肽的特定组的多肽或其功能等同物。 本发明还涉及一种治疗哺乳动物代谢疾病的方法,包括向所述哺乳动物施用治疗有效量的胰岛素促分泌肽。 还公开了制备重组体和合成肽的方法。

    Pituitary adenylate cyclase activating peptide (PACAP) receptor 3 (R3) agonists and their pharmacological methods of use
    25.
    发明授权
    Pituitary adenylate cyclase activating peptide (PACAP) receptor 3 (R3) agonists and their pharmacological methods of use 有权
    垂体腺苷酸环化酶活化肽(PACAP)受体3(R3)激动剂及其药理学用途

    公开(公告)号:US07507714B2

    公开(公告)日:2009-03-24

    申请号:US10892981

    申请日:2004-07-15

    IPC分类号: A61K38/16 C07K14/00

    摘要: This invention provides novel peptides that function in vivo to stimulate insulin release from pancreatic beta cells in a glucose-dependent fashion. These insulin secretagogue peptides are shown to stimulate insulin release in rat islet cells in vitro, and in vivo. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VIP/PACAP-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.

    摘要翻译: 本发明提供了新的肽,其在体内起作用以以葡萄糖依赖的方式刺激胰腺β细胞的胰岛素释放。 这些胰岛素促分泌肽显示能够在体外和体内刺激大鼠胰岛细胞中的胰岛素释放。 本发明的肽为具有降低的内源性胰岛素分泌的患者特别是2型糖尿病患者提供了新的疗法。 特别地,本发明是选自VIP / PACAP相关多肽的特定组的多肽或其功能等同物。 本发明还涉及一种治疗哺乳动物代谢疾病的方法,包括向所述哺乳动物施用治疗有效量的胰岛素促分泌肽。 还公开了制备重组体和合成肽的方法。

    Pegylation of Vasoactive Intestinal Peptide (Vip) / Pituitary Adenylate Cyclase Activating Peptide (Pacap) Receptor 2 (Vpac2) Agonists and Methods of Use
    27.
    发明申请
    Pegylation of Vasoactive Intestinal Peptide (Vip) / Pituitary Adenylate Cyclase Activating Peptide (Pacap) Receptor 2 (Vpac2) Agonists and Methods of Use 审中-公开
    血管活性肽(Vip)/垂体腺苷酸环化酶活化肽(Pacap)受体2(Vpac2)激动剂和使用方法的PEG化

    公开(公告)号:US20080261863A1

    公开(公告)日:2008-10-23

    申请号:US11632465

    申请日:2005-06-10

    摘要: This invention relates to modified Vasoactive Intestinal Peptide (VIP)/Pituitary Adenylate Cyclase Activating Peptide (PACAP) Receptor 2 (VPAC2) agonists (VPAC2 agonists) comprising a VPAC2 agonist linked to a polyethylene glycol polymer, as well as related formulations, dosages, and methods of administration thereof for therapeutic purposes. These VPAC2 agonists, compositions, and methods are useful in providing a treatment option for those individuals afflicted with a metabolic disorder such as diabetes, impaired glucose tolerance, metabolic syndrome, or prediabetic states, by inducing glucose-dependent insulin secretion in the absence of the therapeutically limiting side effect of reducing or lowering blood pressure.

    摘要翻译: 本发明涉及包含与聚乙二醇聚合物连接的VPAC2激动剂的修饰的血管活性肠肽(VIP)/垂体腺苷酸环化酶活化肽(PACAP)受体2(VPAC2)激动剂(VPAC2激动剂)以及相关制剂,剂量和 给药方法用于治疗目的。 这些VPAC2激动剂,组合物和方法可用于通过在不存在葡萄糖的情况下诱导葡萄糖依赖性胰岛素分泌为那些患有代谢性疾病例如糖尿病,葡萄糖耐量降低,代谢综合征或前驱糖尿病状态的患者提供治疗选择 治疗上限制降低或降低血压的副作用。