Treatment of inflammatory bowel disease using glucagon-like-peptide-2 (GLP-2) analogues
    62.
    发明授权
    Treatment of inflammatory bowel disease using glucagon-like-peptide-2 (GLP-2) analogues 有权
    使用胰高血糖素样肽-2(GLP-2)类似物治疗炎症性肠病

    公开(公告)号:US08163696B2

    公开(公告)日:2012-04-24

    申请号:US12643261

    申请日:2009-12-21

    IPC分类号: A61K38/00 A61K38/16 A61K38/26

    摘要: GLP-2 analogues are disclosed which comprise one of more substitutions as compared to [hGly2]GLP-2 and which improved biological activity in vivo and/or improved chemical stability, e.g., as assessed in in vitro stability assays. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 8, 16, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 (as mentioned in the introduction) and one or more of positions 3, 5, 7, 10 and 11, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy. Also disclosed are methods and kits for selecting a patient from populations suited for treatment with GLP-2 analogues.

    摘要翻译: 公开了GLP-2类似物,其包含与[hGly2] GLP-2相比更多的取代之一,并且其在体内的改善的生物活性和/或改善的化学稳定性,例如在体外稳定性测定中评估。 更具体地,本文公开的优选的GLP-2类似物包括在野生型GLP-2序列的8,16,24和/或28位的一个或多个位置上的取代,任选与第2位的进一步取代组合(如 引入)和位置3,5,7,10和11中的一个或多个,和/或缺失一个或多个氨基酸31至33和/或添加N-末端或C-末端稳定肽 序列。 类似物对于预防或治疗胃和肠相关疾病以及改善化学疗法的副作用特别有用。 还公开了用于从适合于用GLP-2类似物治疗的群体中选择患者的方法和试剂盒。

    GLP-1 AND METHODS FOR TREATING DIABETES
    67.
    发明申请
    GLP-1 AND METHODS FOR TREATING DIABETES 审中-公开
    GLP-1和治疗糖尿病的方法

    公开(公告)号:US20090088369A1

    公开(公告)日:2009-04-02

    申请号:US12277148

    申请日:2008-11-24

    申请人: Eva Steiness

    发明人: Eva Steiness

    IPC分类号: A61K38/17 A61P3/10 A61K38/28

    摘要: The present invention relates to use of GLP-1 or a related molecule having a GLP-effect for the manufacture of a medicament for preventing or treating diabetes in a mammal. The amount and timing of administration of said medicament are subsequently reduced to produce a “drug holiday.” Practice of the invention achieves effective therapy without continuous drug exposure and without continuous presence of therapeutic levels of the drug. The invention also discloses a method of treating diabetes and related disorders in a mammal by administering glucagon like peptide (GLP-1) or a related molecule having GLP-1 like effect and thereby providing a therapeutically effective amount of endogenous insulin.

    摘要翻译: 本发明涉及GLP-1或具有GLP效应的相关分子在制备用于预防或治疗哺乳动物中的糖尿病的药物中的用途。 随后减少所述药物的给药量和时间,以产生“药物假期”。 本发明的实践在没有持续的药物暴露并且不持续存在治疗水平的药物的情况下实现有效的治疗。 本发明还公开了通过施用胰高血糖素样肽(GLP-1)或具有GLP-1样作用的相关分子,从而提供治疗有效量的内源胰岛素来治疗哺乳动物中的糖尿病和相关疾病的方法。

    Stabilized exendin-4 compounds
    68.
    发明申请
    Stabilized exendin-4 compounds 失效
    稳定的毒蜥外泌肽-4化合物

    公开(公告)号:US20060194719A1

    公开(公告)日:2006-08-31

    申请号:US10529858

    申请日:2003-10-02

    IPC分类号: A61K38/17

    CPC分类号: C07K14/57563 A61K38/00

    摘要: The present invention disclosed compositions comprising a stabilized Exendin-4 (1-39) and related compounds. The invention describes stabilized Exendin-4 agonists that include at least one modified amino acid residue particularly at positions Gln 13, Met14, Trp25, or Asn28 of the Exendin-4 (1-39) molecule. Disclosed are preferred modifications of deaminated, hydrolyzed, oxidized, or isomerized reaction products of the specified amino acid residues corresponding to the same positions in the Exendin-4 molecule. The invention also relates to methods of making and using the stabilized Exendin compounds, such as for the treatment of diabetes.

    摘要翻译: 本发明公开了包含稳定的毒蜥外泌肽-4(1-39)和相关化合物的组合物。 本发明描述了稳定的毒蜥外泌肽-4激动剂,其包括至少一个修饰的氨基酸残基,特别是在毒蜥外泌肽-4(1-39)分子的Gln 13,Met14,Trp25或Asn28的位置。 公开了对应于毒蜥外泌肽-4分子中相同位置的特定氨基酸残基的脱氨基,水解的,氧化的或异构化的反应产物的优选修饰。 本发明还涉及制备和使用稳定的毒蜥外泌肽化合物的方法,例如用于治疗糖尿病。