GLP-1 ANALOGUE, ITS PREPARATION METHODS AND USE THEREOF
    7.
    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

    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。