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1.发明公开O-GLYCOSYLATED CARBOXY TERMINAL PORTION (CTP) PEPTIDE-BASED INSULIN AND INSULIN ANALOGUES 有权基于带有CARBOXYTERMINIERTER零件和胰岛素类似物肽O-糖基化胰岛素
公开(公告)号：EP2925345A1
公开(公告)日：2015-10-07
申请号：EP13861070.4
申请日：2013-11-22
IPC分类号： A61K38/28
摘要： Compositions and formulations comprising insulin or insulin analogs comprising a carboxy terminal portion (CTP) peptide comprising amino acids 112-118 to 145 of the beta subunit of human chorionic gonadotropin (hCGβ) or a partial variant thereof that includes at least one O-glycosylation site of the CTP peptide, wherein the CTP peptide of the CTP peptide-based insulin or insulin analog is O-glycosylated are described. In particular embodiments, the O-glycosylated insulin analogs are produced in vivo and in further embodiments, the O-glycosylated CTP-based insulin analogs comprise predominantly mannotriose and mannotetrose O-glycans or predominantly mannose O-glycans.
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公开(公告)号：EP2249853A1
公开(公告)日：2010-11-17
申请号：EP09708686.2
申请日：2009-01-21
发明人： DIMARCHI, Richard, D. , DE, Arnab
IPC分类号： A61K38/00
CPC分类号： A61K38/28 , A61K9/0019 , A61K38/26 , A61K39/395 , A61K47/48215 , A61K47/48246 , A61K47/60 , A61K47/64
摘要： Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 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.
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3.发明公开AMIDE BASED GLUCAGON SUPERFAMILY PEPTIDE PRODRUGS 审中-公开AMIDBASIERTE PEPTID-PRODRUGS DER GLUCAGON-SUPERFAMILIE
公开(公告)号：EP3075385A1
公开(公告)日：2016-10-05
申请号：EP16164599.9
申请日：2009-12-18
发明人： DIMARCHI, Richard, D. , KOU, Binbin
CPC分类号： A61K38/26 , A61K2300/00
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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4.发明授权SINGLE CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR 有权具有高活性对胰岛素受体的单链胰岛素激动剂
公开(公告)号：EP2582719B1
公开(公告)日：2016-08-10
申请号：EP11796430.4
申请日：2011-06-16
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5.发明公开SINGLE CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR 有权具有高活性对胰岛素受体的单链胰岛素激动剂
公开(公告)号：EP2582719A2
公开(公告)日：2013-04-24
申请号：EP11796430.4
申请日：2011-06-16
发明人： DIMARCHI, Richard, D. , AZRIEL, Julia , KAUR, Zach , MEYERS, Jonathan , PARODY, Todd , ZHAO, Yan
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 A1 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.
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公开(公告)号：EP2376521A1
公开(公告)日：2011-10-19
申请号：EP09837985.2
申请日：2009-12-18
IPC分类号： C07K1/00
CPC分类号： C07K14/622 , A61K38/28 , A61K47/48246 , A61K47/64 , C07K14/62 , C07K14/625
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.
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公开(公告)号：EP2376097A1
公开(公告)日：2011-10-19
申请号：EP09833836.1
申请日：2009-12-18
发明人： DIMARCHI, Richard, D. , KOU, Binbin
CPC分类号： A61K38/26 , A61K2300/00
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.
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8.发明公开GLUCAGON ANALOGS EXHIBITING ENHANCED SOLUBILITY AND STABILITY IN PHYSIOLOGICAL PH BUFFERS 审中-公开胰高血糖素类似物具有改进的在生理pH缓冲液的溶解度和稳定性
公开(公告)号：EP2307037A1
公开(公告)日：2011-04-13
申请号：EP09767567.2
申请日：2009-06-16
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.
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9.发明公开
公开(公告)号：EP2300035A2
公开(公告)日：2011-03-30
申请号：EP09800752.9
申请日：2009-06-16
发明人： DIMARCHI, Richard, D. , MA, Tao
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。
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公开(公告)号：EP2376521B1
公开(公告)日：2016-04-13
申请号：EP09837985.2
申请日：2009-12-18
IPC分类号： C07K14/62 , C07K14/625 , A61K38/28 , A61K47/48
CPC分类号： C07K14/622 , A61K38/28 , A61K47/48246 , A61K47/64 , C07K14/62 , C07K14/625
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