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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO2012088116A3 GLUCAGON ANALOGS EXHIBITING GIP RECEPTOR ACTIVITY 审中-公开
标题翻译： GLUCAGON ANALOGS展示GIP受体活性
公开(公告)号：WO2012088116A3
公开(公告)日：2012-11-15
申请号：PCT/US2011066164
申请日：2011-12-20
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , WARD BRIAN
发明人： DIMARCHI RICHARD D , WARD BRIAN
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00
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。

6. 发明申请

WO2010011439A3 GIP-BASED MIXED AGONISTS FOR TREATMENT OF METABOLIC DISORDERS AND OBESITY 审中-公开
标题翻译：基于GIP的混合促效剂治疗代谢性疾病和肥胖症
公开(公告)号：WO2010011439A3
公开(公告)日：2010-05-14
申请号：PCT/US2009047447
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , TAO MA
发明人： DIMARCHI RICHARD D , TAO MA
IPC分类号： A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/60
摘要： Glucagon peptides that exhibit GIP agonist activity in addition to glucagon and/or GLP-I activity are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods of using such peptides are also provided.
摘要翻译：提供了除胰高血糖素和/或GLP-1活性之外还表现出GIP激动剂活性的胰高血糖素肽。还提供了包含这种胰高血糖素肽的药物组合物以及使用这些肽的治疗方法。

7. 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。

8. 发明申请

WO2011163462A3 AMIDE-BASED INSULIN PRODRUGS 审中-公开
标题翻译：基于氨基酸的胰岛素原料
公开(公告)号：WO2011163462A3
公开(公告)日：2012-04-05
申请号：PCT/US2011041603
申请日：2011-06-23
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , KOU BINBIN , CHENG SHUJIANG
发明人： DIMARCHI RICHARD D , KOU BINBIN , CHENG SHUJIANG
IPC分类号： C07K14/62 , A61K38/00
CPC分类号： C07K14/62 , A61K38/00
摘要： Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
摘要翻译：提供了胰岛素和胰岛素类似物的前药制剂，其中胰岛素肽已经通过二肽前药成分的酰胺键键修饰。本文公开的前体药物的半衰期延长至少10小时，更典型地大于2小时，20小时和小于70小时，并通过化学不稳定驱动的非酶反应在生理条件下转化为活性形式。

9. 发明申请

WO2011159882A3 NOVEL STABILIZED INSULIN AGONISTS 审中-公开
标题翻译：新型稳定胰岛素激素
公开(公告)号：WO2011159882A3
公开(公告)日：2012-03-22
申请号：PCT/US2011040677
申请日：2011-06-16
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , HAN JIE , MROZ PIOTR
发明人： DIMARCHI RICHARD D , HAN JIE , MROZ PIOTR
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： C07K14/62 , A61K38/00
摘要： As disclosed herein a series of novel high potency insulin agonists have been designed, synthesized and characterized that relate to stabilization of the native alpha helical secondary structure of the insulin A and B chains. In accordance with one embodiment an insulin agonist analog is provided, comprising an A chain and a B chain sequence wherein the native alpha helical secondary structure has been stabilized in one or both of said A chain and B chain sequences by substitutions and/or additions of the native sequence with alpha, alpha disubstituted amino acids (e.g., amino isobutyric acid, Aib) or with amino acids that foster intramolecular interactions between amino acid side chains including the formation of lactams, lactones or salt bridges, or any combination thereof.
摘要翻译：如本文所公开的，已经设计，合成和表征了一系列新型高效胰岛素激动剂，其涉及胰岛素A和B链的天然α-螺旋二级结构的稳定化。根据一个实施方案，提供胰岛素激动剂类似物，其包含A链和B链序列，其中所述天然α螺旋二级结构已经通过置换和/或添加所述A链和B链序列稳定在所述A链和B链序列的一个或两个中具有α，α二取代氨基酸（例如，氨基异丁酸，Aib）的天然序列或者促进包括形成内酰胺，内酯或盐桥的氨基酸侧链之间的分子内相互作用的氨基酸或其任何组合。

10. 发明申请

WO2011075393A3 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：WO2011075393A3
公开(公告)日：2011-08-11
申请号：PCT/US2010059724
申请日：2010-12-09
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D
发明人： DIMARCHI RICHARD D
IPC分类号： A61K38/26
CPC分类号： C07K14/605 , A61K38/00
摘要： Provided herein are glucagon analogs comprising a modified amino acid sequence of native human glucagon (SEQ ID NO: 2) that exhibit activity at the glucagon receptor, activity at the GLP-I receptor, or activity at each of the glucagon recpeotr and the GLP-I receptor. In some embodiments, the glucagon analog exhibits at least 100% or more of the activity of native glucagon at the glucagon receptor and/or at least 100% or more of the activity of native GLP-I at the GLP-I receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is within 50-fold or less than the EC50 at the glucagon receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is two- to ten-fold greater than the EC50 at the glucagon receptor. Related conjugates, dimers and multimers, and pharmaceutical compositions, and uses thereof, are further provided.
摘要翻译：本文提供了包含天然人胰高血糖素（SEQ ID NO：2）的经修饰的氨基酸序列的胰高血糖素类似物，其对胰高血糖素受体表现出活性，对GLP-1受体的活性或对胰高血糖素复制剂和GLP- I受体。在一些实施方案中，胰高血糖素类似物展现天然胰高血糖素对胰高血糖素受体的至少100％或更多的活性和/或天然GLP-1对GLP-1受体的至少100％或更多的活性。在一些实施方案中，胰高血糖素类似物对GLP-1受体具有比胰高血糖素受体的EC 50小50倍或更小的EC 50。在一些实施方案中，胰高血糖素类似物对GLP-1受体具有比对胰高血糖素受体的EC 50大2至10倍的EC 50。进一步提供了相关的缀合物，二聚体和多聚体，以及药物组合物及其用途。

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