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公开(公告)号：US20100190701A1
公开(公告)日：2010-07-29
申请号：US12527140
申请日：2008-02-13
申请人： Jonathan Day , James Patterson , Joseph Chabenne , Maria Dimarchi , David Smiely , Richard D. Dimarchi
发明人： Jonathan Day , James Patterson , Joseph Chabenne , Maria Dimarchi , David Smiely , Richard D. Dimarchi
IPC分类号： A61K38/26 , C07K14/605 , A61P3/10 , A61P3/04
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 (K-RNRNNIA) 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（K-RNRNNIA）和SEQ ID NO：28（KRNR）。
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公开(公告)号：US20120172295A1
公开(公告)日：2012-07-05
申请号：US13378001
申请日：2010-06-16
申请人： Richard D. Dimarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian P. Ward , Tao Ma
发明人： Richard D. Dimarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian P. Ward , Tao Ma
IPC分类号： A61K38/26 , A61P3/10 , C07K14/605 , A61P3/04
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.
摘要翻译： 提供具有增加的GIP活性的胰高血糖素肽，任选地具有GLP-1和/或胰高血糖素活性。 在一些实施方案中，本文提供了包含与天然胰高血糖素基本相似的氨基酸序列的C-末端扩增的胰高血糖素肽。
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公开(公告)号：US08454971B2
公开(公告)日：2013-06-04
申请号：US12527140
申请日：2008-02-13
申请人： Jonathan Day , James Patterson , Joseph Chabenne , Maria Dimarchi , David L. Smiley , Richard D. Dimarchi
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
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 (K-RNRNNIA) 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（K-RNRNNIA）和SEQ ID NO：28（KRNR）。
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公开(公告)号：US20110257092A1
公开(公告)日：2011-10-20
申请号：US12999283
申请日：2009-06-16
申请人： Richard D. Dimarchi , David l. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian Ward
发明人： Richard D. Dimarchi , David l. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian Ward
IPC分类号： A61K38/26 , A61P3/04 , A61P3/10 , C07K14/605
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。 通过形成分子内桥或通过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。 通过聚乙二醇化，酰化，烷基化，羧基末端氨基酸的取代，C-末端截短或加入选自下组的羧基末端肽，可以进一步改善这些高效胰高血糖素类似物的溶解度和稳定性 由SEQ ID NO：26（GPSSGAPPPS），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）组成。
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公开(公告)号：US08546327B2
公开(公告)日：2013-10-01
申请号：US12999283
申请日：2009-06-16
申请人： Richard D. Dimarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian Ward
发明人： Richard D. Dimarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian Ward
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).
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6.发明申请GLUCAGON ANALOGS EXHIBITING ENHANCED SOLUBILITY AND STABILITY IN PHYSIOLOGICAL pH BUFFERS 有权GLUCAGON ANALOGS展示增强的生理pH缓冲液中的溶解性和稳定性公开(公告)号：US20110190200A1
公开(公告)日：2011-08-04
申请号：US12999284
申请日：2009-06-16
IPC分类号： A61K38/26 , C07K14/605 , A61P3/08
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.
摘要翻译： 公开了具有改善的溶解度和/或半衰期同时保留胰高血糖素激动剂活性的改良的胰高血糖素肽。 糖原肽已经通过用带氨基酸的氨基酸取代天然氨基酸和/或添加到肽的羧基末端而被修饰。 修饰的胰高血糖素激动剂可以通过聚乙二醇化，或加入选自SEQ ID NO：20，SEQ ID NO：21，SEQ ID NO：23或两者的羧基末端肽进一步修饰，以进一步增强溶解度 的胰高血糖素激动剂类似物。
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7.发明授权Glucagon analogs exhibiting enhanced solubility and stability in physiological pH buffers 有权在生理pH缓冲液中表现出增强的溶解度和稳定性的胰高血糖素类似物公开(公告)号：US08450270B2
公开(公告)日：2013-05-28
申请号：US12999284
申请日：2009-06-16
IPC分类号： A61K35/00
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.
摘要翻译： 公开了具有改善的溶解度和/或半衰期同时保留胰高血糖素激动剂活性的改良的胰高血糖素肽。 糖原肽已经通过用带氨基酸的氨基酸取代天然氨基酸和/或添加到肽的羧基末端而被修饰。 修饰的胰高血糖素激动剂可以通过聚乙二醇化，或加入选自SEQ ID NO：20，SEQ ID NO：21，SEQ ID NO：23或两者的羧基末端肽进一步修饰，以进一步增强溶解度 的胰高血糖素激动剂类似物。
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8.发明授权Glucagon analogs exhibiting enhanced solubility in physiological pH buffers 有权在生理pH缓冲液中表现出增强的溶解度的胰高血糖素类似物公开(公告)号：US08669228B2
公开(公告)日：2014-03-11
申请号：US12522129
申请日：2008-01-03
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605
摘要： Modified glucagon peptides are disclosed having improved solubility 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.
摘要翻译： 公开了改进的胰高血糖素肽，其具有改善的溶解性，同时保留胰高血糖素激动剂活性。 糖原肽已经通过用带氨基酸的氨基酸取代天然氨基酸和/或添加到肽的羧基末端而被修饰。 修饰的胰高血糖素激动剂可以通过聚乙二醇化，或加入选自SEQ ID NO：20，SEQ ID NO：21，SEQ ID NO：23或两者的羧基末端肽进一步修饰，以进一步增强溶解度 的胰高血糖素激动剂类似物。
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9.发明申请GLUCAGON ANALOGS EXHIBITING ENHANCED SOLUBILITY IN PHYSIOLOGICAL pH BUFFERS 有权GLUCAGON ANALOGS展现了生理pH值缓冲液中增强的溶解度公开(公告)号：US20100190699A1
公开(公告)日：2010-07-29
申请号：US12522129
申请日：2008-01-03
IPC分类号： A61K38/26 , C07K14/605 , A61P3/00 , A61P1/00
CPC分类号： C07K14/605
摘要： Modified glucagon peptides are disclosed having improved solubility 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.
摘要翻译： 公开了改进的胰高血糖素肽，其具有改善的溶解性，同时保留胰高血糖素激动剂活性。 糖原肽已经通过用带氨基酸的氨基酸取代天然氨基酸和/或添加到肽的羧基末端而被修饰。 修饰的胰高血糖素激动剂可以通过聚乙二醇化，或加入选自SEQ ID NO：20，SEQ ID NO：21，SEQ ID NO：23或两者的羧基末端肽进一步修饰，以进一步增强溶解度 的胰高血糖素激动剂类似物。
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