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    GLP-1 ANALOGUE, ITS PREPARATION METHODS AND USE THEREOF
    1.
    发明申请
    GLP-1 ANALOGUE, ITS PREPARATION METHODS AND USE THEREOF 审中-公开
    GLP-1类似物，其制备方法及其用途

    公开(公告)号：US20150274799A1

    公开(公告)日：2015-10-01

    申请号：US14405060

    申请日：2012-02-08

    申请人： Min Gong ,  Gang Fu ,  Weiren Xu ,  Lida Tang ,  Xiaowen Ren ,  Peng Liu ,  Yuli Wang ,  Jiang Wu ,  Meixiang Zou

    发明人： Min Gong ,  Gang Fu ,  Weiren Xu ,  Lida Tang ,  Xiaowen Ren ,  Peng Liu ,  Yuli Wang ,  Jiang Wu ,  Meixiang Zou

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605 ,  A61K38/00

    摘要： Provided is a GLP-1 analogue having the structure as shown in the general formula A: 7HAEX10TFTSX15VSSYLEX22QAAKEFIX30WLX33KGRG37n1X1Cn2X2   (general formula A), wherein X10 is glycine or cysteine, X15 is aspartic acid or cysteine, X22 is glycine or cysteine, X30 is alanine or cysteine, X33 is valine or cysteine, and at least one of X10, X15, X22, X30 and X33 is cysteine, X1 and X2 respectively is glycine, alanine or valine, n1=1-30, n2=1-30. The general formula A contains two cysteines to form disulfide bonds. Also provided are the preparation methods and the use of said GLP-1 analogue. Said GLP-1 analogue has a prolonged blood half-life compared with GLP-1, and can be used for the treatment of diabetes and obesity.

    摘要翻译： 本发明提供具有通式A所示结构的GLP-1类似物：7HAEX10TFTSX15VSSYLEX22QAAKEFIX30WLX33KGRG37n1X1Cn2X2（通式A），其中X10为甘氨酸或半胱氨酸，X15为天冬氨酸或半胱氨酸，X22为甘氨酸或半胱氨酸，X30为丙氨酸或半胱氨酸 X33是缬氨酸或半胱氨酸，X10，X15，X22，X30和X33中的至少一个是半胱氨酸，X1和X2分别是甘氨酸，丙氨酸或缬氨酸，n1 = 1-30，n2 = 1-30。 通式A包含形成二硫键的两个半胱氨酸。 还提供了所述GLP-1类似物的制备方法和用途。 所述GLP-1类似物与GLP-1相比具有延长的血液半衰期，并且可用于治疗糖尿病和肥胖症。

    GLUCAGON-LIKE PEPTIDE-1 ANALOGUE MONOMER AND DIMER, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
    2.
    发明申请
    GLUCAGON-LIKE PEPTIDE-1 ANALOGUE MONOMER AND DIMER, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF 审中-公开
    GLUCAGON-like肽类1型模拟单体和二聚体，其制备方法及其应用

    公开(公告)号：US20150232527A1

    公开(公告)日：2015-08-20

    申请号：US14405066

    申请日：2012-03-28

    申请人： Min Gong ,  Weiren Xu ,  Lida Tang ,  Gang Fu ,  Meixiang Zou ,  Jiang Wu

    发明人： Min Gong ,  Weiren Xu ,  Lida Tang ,  Gang Fu ,  Meixiang Zou ,  Jiang Wu

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K38/26

    摘要： Provided are a glucagon-like peptide-1 (GLP-1) analogue monomer and dimmer, a preparation method thereof, and an application thereof. The GLP-1 analogue monomer comprises one cysteine; and the dimer is formed by two monomer molecules connected via an intermolecular disulfide bond formed by the cysteine. The GLP-1 monomer comprising cysteine has the following general formula: 7HAEX10TFTSX15VSSYLEX22X23AAKEFIX30WLX33KGRG37, wherein X10 is glycine or cysteine, X15 is aspartate or cysteine, X22 is glycine or cysteine, X23 is glutamine or cysteine, X30 is alanine or cysteine, and X33 is valine or cysteine; and only one of X10, X15, X22, X23, X30, and X33 is cysteine. The glucagon-like peptide-1 analogue dimer of the present invention has an in vivo half-life of more than 8 to 96 hours, thus facilitating clinical promotion and application.

    摘要翻译： 提供胰高血糖素样肽-1（GLP-1）类似物单体和二聚体，其制备方法及其应用。 GLP-1类似物单体包含一个半胱氨酸; 并且二聚体由通过由半胱氨酸形成的分子间二硫键连接的两个单体分子形成。 包含半胱氨酸的GLP-1单体具有以下通式：7HAEX10TFTSX15VSSYLEX22X23AAKEFIX30WLX33KGRG37，其中X10是甘氨酸或半胱氨酸，X15是天冬氨酸或半胱氨酸，X22是甘氨酸或半胱氨酸，X23是谷氨酰胺或半胱氨酸，X30是丙氨酸或半胱氨酸，X33是缬氨酸 或半胱氨酸; 并且X10，X15，X22，X23，X30和X33中只有一个是半胱氨酸。 本发明的胰高血糖素样肽-1类似物二聚体的体内半衰期大于8〜96小时，因此有助于临床推广和应用。