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    C-TERMINAL AMIDATION OF POLYPEPTIDES
    22.
    发明申请
    C-TERMINAL AMIDATION OF POLYPEPTIDES 有权
    聚氨酯的C-末端氨基化

    公开(公告)号：US20140058070A1

    公开(公告)日：2014-02-27

    申请号：US13822821

    申请日：2011-09-08

    申请人： Chengzao Sun ,  Behrouz Bruce Forood ,  Gary Luo ,  Soumitra S. Ghosh

    发明人： Chengzao Sun ,  Behrouz Bruce Forood ,  Gary Luo ,  Soumitra S. Ghosh

    IPC分类号： C07K1/00

    CPC分类号： C07K1/003 ,  C07C211/27 ,  C07D311/88 ,  C07K1/107

    摘要： There are provided compounds and methods for amidating the C-terminus of a polypeptide. The method include reacting a polypeptide which includes a C-terminal thioester or C-terminal selenoester with any one of a defined set of auxiliary molecules under conditions suitable to produce a polypeptide adduct which includes the auxiliary molecule chemically bound at the C-terminal of the polypeptide. In the subsequent step, the auxiliary molecule is removed from the C-terminal of the polypeptide adduct under conditions suitable to produce an amidated polypeptide.

    摘要翻译： 提供了用于酰胺化多肽的C末端的化合物和方法。 该方法包括在适于产生多肽加合物的条件下使包含C-末端硫酯或C-末端硒酸酯的多肽与定义的一组辅助分子中的任一个反应，所述多肽加合物包括在C末端化学结合的辅助分子 多肽。 在随后的步骤中，辅助分子在适于产生酰胺化多肽的条件下从多肽加合物的C-末端去除。

    N-terminus conformationally constrained GLP-1 receptor agonist compounds
    23.
    发明授权
    N-terminus conformationally constrained GLP-1 receptor agonist compounds 有权
    N末端构象约束的GLP-1受体激动剂化合物

    公开(公告)号：US08642544B2

    公开(公告)日：2014-02-04

    申请号：US13260702

    申请日：2010-03-26

    申请人： Josue Alfaro-Lopez ,  Abhinandini Sharma ,  Soumitra S. Ghosh

    发明人： Josue Alfaro-Lopez ,  Abhinandini Sharma ,  Soumitra S. Ghosh

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

    CPC分类号： C07K14/605 ,  A61K38/00 ,  C07K14/46

    摘要： The disclosure provides N-terminus conformationally constrained compounds, which may comprise peptide mimetics and/or amino acid substitutions, which may be used in peptides, such as GLP-1 receptor agonist compounds, to induce a β-turn secondary structure at the N-terminus. The N-terminus conformationally constrained compounds may be used for research purposes; to produce GLP-1 receptor agonist compounds having improved GLP-1 receptor binding activity, enzymatic stability, or in vivo glucose lowering activity; and to develop GLP-1 receptor agonist compounds which have fewer amino acid residues. The disclosure also provides GLP-1 receptor agonist compounds, such as exendins, exendin analogs, GLP-1 (7-37), GLP-1 (7-37) analogs, comprising the N-terminus conformationally constrained compounds. The compounds are useful for treating various diseases, such as diabetes and obesity. The disclosure also provides methods for chemically synthesizing the N-terminus conformationally constrained compounds.

    摘要翻译： 本公开提供了可以包含肽模拟物和/或氨基酸取代的N末端构象约束的化合物，其可以用于肽，例如GLP-1受体激动剂化合物，以在N-末端诱导β-匝二次结构， 终点。 N末端构象约束化合物可用于研究目的; 以产生具有改善的GLP-1受体结合活性，酶稳定性或体内葡萄糖降低活性的GLP-1受体激动剂化合物; 并开发具有较少氨基酸残基的GLP-1受体激动剂化合物。 本公开还提供了GLP-1受体激动剂化合物，例如包含N末端构象约束的化合物的毒蜥外泌肽，毒蜥外泌肽类似物，GLP-1（7-37），GLP-1（7-37）类似物。 该化合物可用于治疗各种疾病，如糖尿病和肥胖症。 本公开还提供了化学合成N末端构象约束化合物的方法。