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公开(公告)号：EP2986314A2
公开(公告)日：2016-02-24
申请号：EP14768322.1
申请日：2014-03-14
发明人： DIMARCHI, Richard D. , KOU, Binbin
IPC分类号： A61K38/26
CPC分类号： A61K47/48338 , A61K38/22 , A61K38/26 , A61K45/06 , A61K47/542 , C07K14/605 , A61K2300/00
摘要： Peptide-based prodrugs having significantly extended half lives are disclosed herein.
摘要翻译： 与亲本肽或多肽相比，提供生物活性肽（或多肽）的前药衍生物，其在血清中表现出延长的半衰期和体内延长的作用。 在一些实施方案中，肽选自胰高血糖素，毒蜥外泌肽-4，GLP-1，GLP-2，GIP，血管活性肠肽（VIP），垂体腺苷酸环化酶活化多肽27（PACAP-27），肽 组氨酸甲硫氨酸（PHM），胃泌酸调节素，促胰液素，骨钙素，生长激素释放激素，以及类似物，衍生物和缀合物。
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公开(公告)号：EP4236980A1
公开(公告)日：2023-09-06
申请号：EP21887298.4
申请日：2021-10-26
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3.发明授权
公开(公告)号：EP2780031B1
公开(公告)日：2018-03-07
申请号：EP12849285.7
申请日：2012-11-16
发明人： DIMARCHI, Richard D. , YANG, Bin
CPC分类号： C07K14/605 , A61K38/00 , A61K47/554 , C07K2319/715
摘要： Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.
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公开(公告)号：EP2900255A2
公开(公告)日：2015-08-05
申请号：EP13841334.9
申请日：2013-09-25
发明人： DIMARCHI, Richard D. , ZHAO, Yan
摘要： Disclosed herein are insulin analog dimers having unique insulin receptor agonist activity based on insulin polypeptide sequences, the site of dimerization and the length of the dimerization linker that connects the two insulin polypeptides. In accordance with one embodiment the first and second insulin polypeptide are independently a two chain insulin analog or a single chain analog and the first and second insulin polypeptides are linked to one another via a B29-B29', B1-C8, B1-B1 or C8-C8 linkage.
摘要翻译： 本文公开了具有基于胰岛素多肽序列的独特的胰岛素受体激动剂活性的胰岛素类似物二聚体，连接两个胰岛素多肽的二聚化位点和二聚连接体的长度。 根据一个实施方案，第一和第二胰岛素多肽独立地是双链胰岛素类似物或单链类似物，第一和第二胰岛素多肽通过B29-B29'，B1-C8，B1-B1或 C8-C8键。
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5.发明公开
公开(公告)号：EP2780031A1
公开(公告)日：2014-09-24
申请号：EP12849285.7
申请日：2012-11-16
发明人： DIMARCHI, Richard D. , YANG, Bin
CPC分类号： C07K14/605 , A61K38/00 , A61K47/554 , C07K2319/715
摘要： Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.
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6.发明公开LIPIDATED INCRETIN RECEPTOR LIGAND HUMAN IMMUNOGLOBULIN FC-REGION FUSION POLYPEPTIDES 审中-公开融合OFF脂化肠降血糖素受体配体和人免疫球蛋白Fc区
公开(公告)号：EP3082847A1
公开(公告)日：2016-10-26
申请号：EP14830920.6
申请日：2014-12-19
发明人： BELLI, Sara , BLEICHER, Konrad , DIMARCHI, Richard D. , HOFFMANN, Eike , KITAS, Eric A. , KONKAR, Anish A.
IPC分类号： A61K38/26 , C07K14/605 , A61K47/48
CPC分类号： A61K38/26 , A61K38/00 , A61K45/06 , A61K47/543 , C07K14/605 , C07K2319/30
摘要： Herein is reported a fusion polypeptide comprising i) one, two, three or four incretin receptor ligand polypeptides, and ii) one human immunoglobulin Fc-region, wherein at least one of the incretin receptor ligand polypeptides comprises an amino acid that is covalently conjugated to a lipid, and wherein each of the one, two, three or four incretin receptor ligand polypeptides is covalently conjugated by a peptide bond to a terminus of the human immunoglobulin Fc-region, whereby to each terminus of the human immunoglobulin Fc-region only a single incretin receptor ligand polypeptide is conjugated.
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公开(公告)号：EP2864351B1
公开(公告)日：2016-08-10
申请号：EP13731619.6
申请日：2013-06-18
发明人： DIMARCHI, Richard D.
IPC分类号： C07K14/435
CPC分类号： C07K14/605 , A61K38/16 , A61K38/17 , A61K38/26
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公开(公告)号：EP2970511A1
公开(公告)日：2016-01-20
申请号：EP14773636.7
申请日：2014-03-05
发明人： DIMARCHI, Richard D. , PARODY, Todd , HAN, Jie , LI, Pengyun
IPC分类号： C07K19/00
摘要： Disclosed herein are insulin agonist peptides conjugated to incretins wherein the insulin/incretin conjugate has agonist activity at both the insulin receptor and the corresponding incretin receptor. Insulin is a proven therapy for the treatment of juvenile-onset diabetes and later-stage adult-onset diabetes. The peptide is biosynthesized as a larger linear precursor of low potency (approximately 2% to 9% of native insulin), named proinsulin. Proinsulin is proteolytically converted to insulin by the selective removal of a 35-residue connecting peptide (C peptide).
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公开(公告)号：EP2864351A1
公开(公告)日：2015-04-29
申请号：EP13731619.6
申请日：2013-06-18
发明人： DIMARCHI, Richard D.
IPC分类号： C07K14/435
CPC分类号： C07K14/605 , A61K38/16 , A61K38/17 , A61K38/26
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.
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公开(公告)号：EP2900255B1
公开(公告)日：2019-01-30
申请号：EP13841334.9
申请日：2013-09-25
发明人： DIMARCHI, Richard D. , ZHAO, Yan
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