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1. 发明申请

WO2012177444A3 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 审中-公开
标题翻译： GLUCAGON / GLP-1受体协同作用
公开(公告)号：WO2012177444A3
公开(公告)日：2013-04-25
申请号：PCT/US2012042085
申请日：2012-06-12
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , SMILEY DAVID L , YANG BIN
发明人： DIMARCHI RICHARD D , SMILEY DAVID L , YANG BIN
IPC分类号： C07K14/605 , A61K38/17 , A61P3/10 , C07K14/435 , C07K14/575 , C07K19/00
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.
摘要翻译：本文提供了与天然胰高血糖素相比显示增强的GLP-1受体活性的肽和变体肽。

2. 发明申请

WO2007056362A3 GLUCAGON ANALOGS EXHIBITING PHYSIOLOGICAL SOLUBILITY AND STABILITY 审中-公开
标题翻译： GLUCAGON ANALOGS展现生理学可溶性和稳定性
公开(公告)号：WO2007056362A3
公开(公告)日：2009-04-23
申请号：PCT/US2006043334
申请日：2006-11-06
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , SMILEY DAVID L
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
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.
摘要翻译：公开了具有改善的溶解度和稳定性的改良的胰高血糖素肽，其中天然胰高血糖素肽已经被聚乙二醇化修饰，或者加入选自SEQ ID NO：19，SEQ ID NO：20，SEQ ID NO：20的羧基末端肽 NO：21，或两者兼而有之。

3. 发明申请

WO2009155258A3 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 审中-公开
标题翻译： GLUCAGON / GLP-1受体协同作用
公开(公告)号：WO2009155258A3
公开(公告)日：2010-02-18
申请号：PCT/US2009047438
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
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。

4. 发明申请

WO2012177443A3 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 审中-公开
标题翻译： GLUCAGON / GLP-1受体激动剂
公开(公告)号：WO2012177443A3
公开(公告)日：2013-04-25
申请号：PCT/US2012042084
申请日：2012-06-12
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , SMILEY DAVID L
发明人： DIMARCHI RICHARD D , SMILEY DAVID L
IPC分类号： A61K38/26 , A61K38/16 , A61K38/17 , A61P3/00 , A61P3/04 , A61P3/10
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。

5. 发明申请

WO2009155257A8 GLUCAGON ANALOGS EXHIBITING ENHANCED SOLUBILITY AND STABILITY IN PHYSIOLOGICAL PH BUFFERS 审中-公开
标题翻译： GLUCAGON ANALOGS展现增强的生理PH缓冲液中的溶解性和稳定性
公开(公告)号：WO2009155257A8
公开(公告)日：2010-03-25
申请号：PCT/US2009047437
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN
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.
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。

6. 发明申请

WO2009058734A4 COMPOUNDS EXHIBITING GLUCAGON ANTAGONIST AND GLP-1 AGONIST ACTIVITY 审中-公开
标题翻译：化合物展示GLUCAGON ANTAGONIST和GLP-1激动剂活性
公开(公告)号：WO2009058734A4
公开(公告)日：2009-07-23
申请号：PCT/US2008081333
申请日：2008-10-27
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , YANG BIN , OUYANG CHENGUANG
发明人： DIMARCHI RICHARD D , YANG BIN , OUYANG CHENGUANG
IPC分类号： A61K38/00 , A61K39/00 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/16 , A61K38/22 , A61K38/26 , C07K7/02
摘要： Glucagon analogs are disclosed that exhibit both glucagon antagonist and GLP-1 agonist activity. In one embodiment, the glucagon antagonist/GLP-1 agonist comprises a modified amino acid sequence of native glucagon, in which the first one to five N-terminal amino acids of native glucagon is deleted and in which the alpha helix is stabilized.
摘要翻译：公开了显示胰高血糖素拮抗剂和GLP-1激动剂活性的胰高血糖素类似物。在一个实施方案中，胰高血糖素拮抗剂/ GLP-1激动剂包含天然胰高血糖素的修饰的氨基酸序列，其中天然胰高血糖素的前一至五个N-末端氨基酸被缺失，并且其中α螺旋被稳定。

7. 发明申请

WO2009058662A2 GLUCAGON ANTAGONISTS 审中-公开
公开(公告)号：WO2009058662A2
公开(公告)日：2009-05-07
申请号：PCT/US2008080973
申请日：2008-10-23
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , YANG BIN
发明人： DIMARCHI RICHARD D , YANG BIN
IPC分类号： A61K39/395
CPC分类号： C07K14/605 , A61K38/00
摘要： Glucagon antagonists are provided which comprise amino acid substitutions and/or chemical modifications to glucagon sequence. In one embodiment, the glucagon antagonists comprise a native glucagon peptide that has been modified by the deletion of the first two to five amino acid residues from the N-terminus and (i) an amino acid substitution at position 9 (according to the numbering of native glucagon) or (ii) substitution of the Phe at position 6 (according to the numbering of native glucagon) with phenyl lactic acid (PLA). In another embodiment, the glucagon antagonists comprise the structure A-B-C as described herein, wherein A is PLA, an oxy derivative thereof, or a peptide of 2-6 amino acids in which two consecutive amino acids of the peptide are linked via an ester or ether bond.
摘要翻译：提供了包含对胰高血糖素序列的氨基酸取代和/或化学修饰的胰高血糖素拮抗剂。在一个实施方案中，胰高血糖素拮抗剂包含通过从N-末端缺失前两个至五个氨基酸残基而修饰的天然胰高血糖素肽，以及（i）在第9位的氨基酸取代（根据天然胰高血糖素）或（ii）用苯基乳酸（PLA）取代第6位的Phe（根据天然胰高血糖素的编号）。在另一个实施方案中，胰高血糖素拮抗剂包含如本文所述的结构ABC，其中A是PLA，其氧衍生物或2-6个氨基酸的肽，其中肽的两个连续氨基酸经由酯或醚连接键。

8. 发明申请

WO2011094337A8 GLUCAGON ANTAGONIST - GIP AGONIST CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS AND OBESITY 审中-公开
标题翻译： GLUCAGON ANTAGONIST - GIP激素治疗组合物和组合物治疗代谢障碍和肥胖
公开(公告)号：WO2011094337A8
公开(公告)日：2012-08-16
申请号：PCT/US2011022608
申请日：2011-01-26
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , MA TAO
发明人： DIMARCHI RICHARD D , MA TAO
IPC分类号： A61K38/26
CPC分类号： C07K14/605 , A61K38/26 , A61K2300/00
摘要： Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided.
摘要翻译：本文提供了包含GIP激动剂肽和胰高血糖素拮抗肽的肽组合。在一些实施方案中，肽组合作为组合物例如药物组合物提供，而在其它实施方案中，肽组合作为试剂盒提供。在其它实施方案中，肽组合作为缀合物提供，例如融合肽，异二聚体。在具体方面，GIP激动剂肽是天然人胰高血糖素的类似物。在具体方面，胰高血糖素拮抗剂肽是天然人胰高血糖素的类似物。在一些实施方案中，GIP激动剂肽通过接头共价连接到胰高血糖素拮抗剂肽。进一步提供治疗疾病例如代谢紊乱（例如糖尿病和肥胖症）的方法，包括施用本文所述的肽组合物。

9. 发明申请

WO2011159895A2 SINGLE CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR 审中-公开
标题翻译：单链胰岛素激动剂在胰岛素受体中展示高活性
公开(公告)号：WO2011159895A2
公开(公告)日：2011-12-22
申请号：PCT/US2011040699
申请日：2011-06-16
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , AZRIEL JULIA , KAUR ZACH , MEYERS JONATHAN , PARODY TODD , ZHAO YAN
发明人： DIMARCHI RICHARD D , AZRIEL JULIA , KAUR ZACH , MEYERS JONATHAN , PARODY TODD , ZHAO YAN
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K38/00 , A61K38/18 , A61K38/28 , A61K47/60 , C07K14/475
摘要： Single chain insulin analogs are provided having high potency and specificity for the insulin receptor. As disclosed herein optimally sized linking moieties can be used to link human insulin A and B chains, or analogs or derivatives thereof, wherein the carboxy terminus of the B25 amino acid of the B chain is linked to the amino terminus of the Al amino acid of the A chain via the intervening linking moiety. In on embodiment the linking moiety comprises a polyethylene glycol of 6-16 monomer units and in an alternative embodiment the linking moiety comprises a non-native amino acid sequence derived form the IGF-1 C-peptide and comprising at least 8 amino acids and no more than 12 amino acid in length. Also disclosed are prodrug and conjugate derivatives of the single chain insulin analogs.
摘要翻译：提供具有对胰岛素受体具有高效力和特异性的单链胰岛素类似物。如本文所公开的，最佳尺寸的连接部分可用于连接人胰岛素A和B链或其类似物或衍生物，其中B链的B25氨基酸的羧基末端连接到A链的氨基酸的氨基末端 A链通过中间连接部分。在实施方案中，连接部分包含6-16个单体单元的聚乙二醇，并且在替代实施方案中，连接部分包含衍生自IGF-1 C-肽的非天然氨基酸序列，并且包含至少8个氨基酸且不包含长度超过12个氨基酸。还公开了单链胰岛素类似物的前药和缀合物衍生物。

10. 发明申请

WO2011163012A3 AMIDE BASED GLUCAGON SUPERFAMILY PEPTIDE PRODRUGS 审中-公开
标题翻译：基于氨基酸的GLUCAGON超级肽系列产品
公开(公告)号：WO2011163012A3
公开(公告)日：2013-07-11
申请号：PCT/US2011040330
申请日：2011-06-14
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , KOU BINBIN
发明人： DIMARCHI RICHARD D , KOU BINBIN
IPC分类号： A61K38/28 , A61K47/48 , C07K1/00 , C12P21/08
CPC分类号： C07K14/605 , A61K38/00
摘要： Prodrug formulations of glucagon superfamily peptides are provided wherein the glucagon superfamily peptide has been modified by the linkage of a dipeptide to the glucagon superfamily through an amide bond linkage. The prodrugs disclosed herein have extended half lives and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
摘要翻译：提供胰高血糖素超家族肽的前药制剂，其中胰高血糖素超家族肽已经通过二肽与胰高血糖素超家族通过酰胺键键连接而被修饰。本文公开的前体药物具有延长的半衰期并且通过由化学不稳定性驱动的非酶反应在生理条件下转化为活性形式。

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