公开(公告)号：EP2307037A1

公开(公告)日：2011-04-13

申请号：EP09767567.2

申请日：2009-06-16

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L. ,  DIMARCHI, Maria ,  CHABENNE, Joseph ,  DAY, Jonathan

IPC分类号： A61K38/00

CPC分类号： C07K14/605 ,  A61K38/00

摘要： Modified glucagon peptides are disclosed having improved solubility and/or half-life while retaining glucagon agonist activity. The glycogen peptides have been modified by substitution of native amino acids with, and/or addition of, charged amino acids to the carboxy terminus of the peptide. The modified glucagon agonists can be further modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 20, SEQ ID NO: 21, SEQ ID NO: 23, or both to further enhance the solubility of the glucagon agonist analogs.

公开(公告)号：EP2443146A1

公开(公告)日：2012-04-25

申请号：EP10790117.5

申请日：2010-06-16

申请人： Indiana University Research And Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L. ,  DIMARCHI, Maria ,  CHABENNE, Joseph ,  DAY, Jonathan ,  PATTERSON, James ,  WARD, Brian, P. ,  TAO, Ma

IPC分类号： C07K14/605

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

摘要： Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein.

公开(公告)号：EP2443146B1

公开(公告)日：2016-10-05

申请号：EP10790117.5

申请日：2010-06-16

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L. ,  DIMARCHI, Maria ,  CHABENNE, Joseph ,  DAY, Jonathan ,  PATTERSON, James ,  WARD, Brian, P. ,  TAO, Ma

IPC分类号： C07K14/605

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

摘要： Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein.

公开(公告)号：EP2300037A2

公开(公告)日：2011-03-30

申请号：EP09767568.0

申请日：2009-06-16

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L. ,  DIMARCHI, Maria ,  CHABENNE, Joseph ,  DAY, Jonathan ,  PATTERSON, James ,  WARD, Brian, C.

IPC分类号： A61K38/00

CPC分类号： C07K14/605

摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP- 1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C- terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

摘要翻译： 公开了相对于天然胰高血糖素具有增强的胰高血糖素受体效力的修饰的胰高血糖素肽。 通过形成分子内桥或用酰胺基取代末端羧酸进一步修饰胰高血糖素肽产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。 溶解度和这些高胰高血糖素效价类似物的稳定性可以通过聚乙二醇化，酰化，烷基化，羧基末端氨基酸的取代，C-末端截短，或额外的羧基末端肽的选自多肽的修饰可以进一步提高 由SEQ ID NO：26（GPSSGAPPPS），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）组成。

公开(公告)号：EP1959986B1

公开(公告)日：2014-07-23

申请号：EP06827600.5

申请日：2006-11-06

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L.

IPC分类号： A61K38/00

CPC分类号： A61K38/26 ,  C07K14/605 ,  Y02E50/16 ,  Y02E50/17

公开(公告)号：EP2723766A2

公开(公告)日：2014-04-30

申请号：EP12803439.4

申请日：2012-06-12

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L. ,  YANG, Bin

IPC分类号： C07K14/605 ,  C07K14/575 ,  C07K19/00 ,  C07K14/435 ,  A61K38/17 ,  A61P3/10

CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K47/60 ,  C07K2319/00 ,  G01N33/74 ,  G01N2333/605 ,  G01N2800/042 ,  G01N2800/085 ,  G01N2800/2821 ,  G01N2800/2835

摘要： Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.

公开(公告)号：EP2723367A2

公开(公告)日：2014-04-30

申请号：EP12802005.4

申请日：2012-06-12

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L.

IPC分类号： A61K38/26 ,  A61K38/17 ,  A61K38/16 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00

CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K38/26 ,  A61K39/3955 ,  A61K47/60 ,  A61K49/00 ,  C07K16/283 ,  C07K2319/00 ,  C07K2319/30 ,  C07K2319/33 ,  G01N33/74 ,  G01N2333/605 ,  G01N2800/042 ,  G01N2800/085 ,  G01N2800/2821 ,  G01N2800/2835

摘要： Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.

摘要翻译： 与天然胰高血糖素相比，本文提供了对GLP-1受体表现出增强的活性的肽和变体肽。

公开(公告)号：EP1959986A2

公开(公告)日：2008-08-27

申请号：EP06827600.5

申请日：2006-11-06

申请人： Indiana University Research and Technology Corporation

发明人： DIMARCHI, Richard, D. ,  SMILEY, David, L.

IPC分类号： A61K38/26

CPC分类号： A61K38/26 ,  C07K14/605 ,  Y02E50/16 ,  Y02E50/17

摘要： Modified glucagon peptides are disclosed having improved solubility and stability, wherein the native glucagon peptide has been modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21, or both.