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公开(公告)号：US09868772B2
公开(公告)日：2018-01-16
申请号：US14408813
申请日：2013-06-18
IPC分类号： A61K38/26 , A61K38/28 , A61K38/00 , A61P3/10 , A61P7/12 , C07K14/605 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K14/605 , A61K38/26
摘要： Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.
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公开(公告)号：US08900593B2
公开(公告)日：2014-12-02
申请号：US13737232
申请日：2013-01-09
发明人： Jonathan Day , James Patterson , Joseph Chabenne , Maria DiMarchi , David L. Smiley , Richard D. DiMarchi
IPC分类号： A61K38/26 , C07K14/605 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/60 , C07K16/00 , C07K2317/52 , C07K2319/30
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 lactam 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, substitution of carboxy terminal amino acids, 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在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。 通过形成内酰胺桥或用酰胺基取代末端羧酸对胰高血糖素肽进一步修饰产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。 这些高效胰高血糖素类似物的溶解度和稳定性可以通过聚乙二醇化，多肽羧基末端氨基酸的取代或加入选自SEQ ID NO：26（GPSSGAPPPS ），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）。
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公开(公告)号：US10730923B2
公开(公告)日：2020-08-04
申请号：US16241932
申请日：2019-01-07
IPC分类号： A61K38/26 , C07K14/605 , A61K47/60 , G01N33/74 , A61K39/395 , C07K16/28 , A61K49/00 , A61K38/00
摘要： Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.
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公开(公告)号：US10232020B2
公开(公告)日：2019-03-19
申请号：US15513748
申请日：2015-09-23
发明人： Richard D. Dimarchi , John P. Mayer , David L. Smiley , Fa Liu
IPC分类号： A61K38/28 , A61K38/22 , A61K47/48 , C07K14/575 , C07K14/605 , C07K14/62 , A61K47/64 , A61K38/00 , A61K9/00 , A61K47/02 , C07K2/00
摘要： Disclosed herein are insulin agonist peptides conjugated to incretins wherein the incretin-insulin conjugate has agonist activity at the insulin receptor and the corresponding incretin receptor, and stimulates weight loss in an individual administered the compound.
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公开(公告)号：US09447162B2
公开(公告)日：2016-09-20
申请号：US14535853
申请日：2014-11-07
发明人： Jonathan Day , James Patterson , Joseph Chabenne , Maria DiMarchi , David L. Smiley , Richard D. DiMarchi
IPC分类号： C07K14/605 , A61K38/26 , A61K47/48 , A61K38/00 , C07K16/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/60 , C07K16/00 , C07K2317/52 , C07K2319/30
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 lactam 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, substitution of carboxy terminal amino acids, 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在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。 通过形成内酰胺桥或用酰胺基取代末端羧酸对胰高血糖素肽进一步修饰产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。 这些高效胰高血糖素类似物的溶解度和稳定性可以通过聚乙二醇化，多肽羧基末端氨基酸的取代或加入选自SEQ ID NO：26（GPSSGAPPPS ），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）。
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公开(公告)号：US20150368310A1
公开(公告)日：2015-12-24
申请号：US14408813
申请日：2013-06-18
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K38/26
摘要： Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.
摘要翻译： 本文提供了在GIP受体上表现出有效活性的胰高血糖素类似物，并且因此被预期用于治疗糖尿病和肥胖症。 在示例性实施方案中，本公开的胰高血糖素类似物在GIP受体下显示EC50，其在纳摩尔或皮摩尔范围内。
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公开(公告)号：US10174093B2
公开(公告)日：2019-01-08
申请号：US15670200
申请日：2017-08-07
IPC分类号： A61K38/26 , C07K14/605 , G01N33/74 , A61K39/395 , C07K16/28 , A61K47/60 , A61K49/00 , A61K38/00
摘要： Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.
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