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1. 发明专利

IL298338A Pth analogs for the treatment of hypoparathyroidism 未知
公开(公告)号：IL298338A
公开(公告)日：2023-01-01
申请号：IL29833822
申请日：2022-11-17
申请人： INDIANA UNIV RESEARCH AND TECHNOLOGY CORPORATION , DIMARCHI RICHARD D , ZHANG FA
发明人： ZHANG FA , DIMARCHI RICHARD D
IPC分类号： C07K14/635
摘要： A novel derivative of parathyroid hormone is provided that has an extended time of action relative to known native parathyroid hormone agonist peptides, while minimizing excessive action shortly after administration. Compositions comprising the novel parathyroid hormone conjugates can be used to treat hypoparathyroidism and osteoporosis.

2. 发明专利

IL278171D0 Gip derivatives and uses thereof 未知
公开(公告)号：IL278171D0
公开(公告)日：2020-11-30
申请号：IL27817120
申请日：2020-10-20
申请人： NOVO NORDISK AS , HOGENDORF WOUTER FREDERIK JOHAN , TH?GERSEN HENNING , COX NICHOLAS RAYMOND , KNERR PATRICK J , DIMARCHI RICHARD , FINAN BRIAN , LAU JESPER F , REEDTZ RUNGE STEFFEN , LIU FA
发明人： HOGENDORF WOUTER FREDERIK JOHAN , TH?GERSEN HENNING , COX NICHOLAS RAYMOND , KNERR PATRICK J , DIMARCHI RICHARD , FINAN BRIAN , LAU JESPER F , REEDTZ-RUNGE STEFFEN , LIU FA
IPC分类号： A61K38/00 , A61K38/22 , A61K38/26 , A61P3/10 , C07K14/575 , C07K14/605 , C07K14/645
摘要： The present invention relates to novel peptides that are derivatives of glucose-dependent insulinotropic polypeptide (GIP) analogues having improved physical stability in solution and a protracted profile of action. More particularly the invention relates to such peptides that are agonists at the GIP receptor and to their use in weight management or for treatment of diseases such as obesity, diabetes or non-alcoholic steatohepatitis (NASH). The peptides comprise a lysine residue at a position corresponding to position 24 of hGIP(1-31), and comprise a negatively charged modifying group attached to the epsilon amino group of the lysine residue.

3. 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。

4. 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。

5. 发明申请

WO2011162968A1 DIPEPTIDE LINKED MEDICINAL AGENTS 审中-公开
标题翻译：替代物连接药物
公开(公告)号：WO2011162968A1
公开(公告)日：2011-12-29
申请号：PCT/US2011/039755
申请日：2011-06-09
申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION , DiMARCHI, Richard, D.
发明人： DiMARCHI, Richard, D.
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： A61K47/48246 , A61K38/00 , A61K38/08 , A61K47/64 , A61K47/65 , C07K2/00 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06086 , C07K5/06095 , C07K5/06104 , C07K5/06113 , C07K5/06147 , C07K5/06156 , C07K5/06165 , C07K14/62
摘要： A non-enzymatically self cleaving dipeptide element is provided that can be linked to known medicinal agents via an amide bond. The dipeptide will spontaneously be cleaved from the medicinal agent under physiological conditions through a reaction driven by chemical instability. Accordingly, the dipeptide element provides a means of linking various compounds to known medicinal agents wherein the compounds are subsequently released from the medicinal agent after a predetermined time of exposure to physiological conditions. For example, the dipeptide can be linked to an active site of a drug to form a prodrug and/or the dipeptide may comprise a depot polymer to sequester an injectable composition comprising the complex at the point of administration.
摘要翻译：提供了可以通过酰胺键与已知药物连接的非酶促自切割二肽元件。通过化学不稳定驱动的反应，二肽将在生理条件下自发地从医药上裂解。因此，二肽元件提供了将各种化合物与已知药物连接的方法，其中化合物随后在暴露于生理条件的预定时间后从药物释放。例如，二肽可以连接到药物的活性位点以形成前体药物和/或二肽可以包含贮库聚合物，以在给药点隔离包含该复合物的可注射组合物。

6. 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。

7. 发明申请

WO2011075393A2 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：WO2011075393A2
公开(公告)日：2011-06-23
申请号：PCT/US2010/059724
申请日：2010-12-09
申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION , 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：本文提供的是包含显示胰高血糖素受体活性，GLP-1受体活性或每种胰高血糖素转录因子和GLP-1受体的活性的天然人胰高血糖素（SEQ ID NO：2）的修饰氨基酸序列的胰高血糖素类似物， I受体。在一些实施方案中，胰高血糖素类似物在胰高血糖素受体上表现出天然胰高血糖素的至少100％或更高的活性和/或天然GLP-1在GLP-1受体上的至少100％或更多的活性。在一些实施方案中，胰高血糖素类似物在GLP-1受体上具有在胰高血糖素受体的50倍或更小的EC 50内的EC 50。在一些实施方案中，胰高血糖素类似物在GLP-1受体上具有比胰高血糖素受体的EC50大2至10倍的EC 50。还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。

8. 发明申请

WO2010080605A1 DIPEPTIDE LINKED MEDICINAL AGENTS 审中-公开
标题翻译：替代物连接药物
公开(公告)号：WO2010080605A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068711
申请日：2009-12-18
申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION , DIMARCHI, Richard, D.
发明人： DIMARCHI, Richard, D.
IPC分类号： A61K38/00 , A61K38/28
CPC分类号： A61K47/65
摘要： A non-enzymatically self cleaving dipeptide element is provided that can be linked to known medicinal agents via an amide bond. The dipeptide will spontaneously be cleaved from the medicinal agent under physiological conditions through a reaction driven by chemical instability. Accordingly, the dipeptide element provides a means of linking various compounds to known medicinal agents wherein the compounds are subsequently released from the medicinal agent after a predetermined time of exposure to physiological conditions. For example, the dipeptide can be linked to an active site of a drug to form a prodrug and/or the dipeptide may comprise a depot polymer to sequester an injectable composition comprising the complex at the point of administration.
摘要翻译：提供了可以通过酰胺键与已知药物连接的非酶促自切割二肽元件。通过化学不稳定驱动的反应，二肽将在生理条件下自发地从医药上裂解。因此，二肽元件提供了将各种化合物与已知药物连接的方法，其中化合物随后在暴露于生理条件的预定时间后从药物释放。例如，二肽可以连接到药物的活性位点以形成前体药物和/或二肽可以包含贮库聚合物，以在给药点隔离包含该复合物的可注射组合物。

9. 发明申请

WO2009058734A1 COMPOUNDS EXHIBITING GLUCAGON ANTAGONIST AND GLP-1 AGONIST ACTIVITY 审中-公开
标题翻译：显示胰高血糖素拮抗剂和GLP-1激动剂活性的化合物
公开(公告)号：WO2009058734A1
公开(公告)日：2009-05-07
申请号：PCT/US2008/081333
申请日：2008-10-27
申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION , 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：公开了胰高血糖素类似物，其表现出胰高血糖素拮抗剂和GLP-1激动剂活性。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氨基酸序列，其中天然胰高血糖素的第一个至五个N端氨基酸被缺失并且其中α螺旋被稳定。 p>

10. 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。

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