-
公开(公告)号：US10232020B2
公开(公告)日：2019-03-19
申请号：US15513748
申请日：2015-09-23
Inventor： Richard D. Dimarchi , John P. Mayer , David L. Smiley , Fa Liu
IPC: A61K38/28 , A61K38/22 , A61K47/48 , C07K14/575 , C07K14/605 , C07K14/62 , A61K47/64 , A61K38/00 , A61K9/00 , A61K47/02 , C07K2/00
Abstract: Disclosed herein are insulin agonist peptides conjugated to incretins wherein the incretin-insulin conjugate has agonist activity at the insulin receptor and the corresponding incretin receptor, and stimulates weight loss in an individual administered the compound.
-
公开(公告)号：US20150368310A1
公开(公告)日：2015-12-24
申请号：US14408813
申请日：2013-06-18
Inventor： Richard D. Dimarchi , David L. Smiley , Konrad H. Bleicher , Eric A. Kitas
IPC: C07K14/605
CPC classification number: C07K14/605 , A61K38/26
Abstract: 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.
Abstract translation: 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。
-
公开(公告)号：US09573987B2
公开(公告)日：2017-02-21
申请号：US14366187
申请日：2012-12-19
Inventor： Richard D. Dimarchi , Pengyun Li
CPC classification number: C07K14/62 , A61K38/00 , A61K38/28 , A61K47/60 , A61K47/64 , C07K14/00 , C07K2319/31 , C07K2319/91
Abstract: Insulin analogs comprising a non-native glycosylation site sequence are provided having high potency and specificity for the insulin receptor. In one embodiment a peptide sequence of greater than 18 amino acids is used as a linking moiety to link human insulin A and B chains, or analogs or derivatives thereof, to provide high potency single chain insulin analogs. In one embodiment the linking moiety comprises one or more glycosylation sites. Also disclosed are prodrug and conjugate derivatives of the insulin analogs.
Abstract translation: 提供包含非天然糖基化位点序列的胰岛素类似物具有对胰岛素受体的高效力和特异性。 在一个实施方案中，大于18个氨基酸的肽序列用作连接部分以连接人胰岛素A和B链或其类似物或衍生物，以提供高效单链胰岛素类似物。 在一个实施方案中，连接部分包含一个或多个糖基化位点。 还公开了胰岛素类似物的前药和缀合物衍生物。
-
公开(公告)号：US10385107B2
公开(公告)日：2019-08-20
申请号：US15513762
申请日：2015-09-23
Inventor： Richard D. Dimarchi , Binbin Kou , Fa Zhang , John P. Mayer
Abstract: 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 and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
-
公开(公告)号：US10683334B2
公开(公告)日：2020-06-16
申请号：US16098236
申请日：2017-05-31
Inventor： Richard D. Dimarchi , John P. Mayer , Piotr Mroz
IPC: A61K38/26 , C07K14/605 , A61K38/28 , A61P3/10
Abstract: Modified glucagon peptides are disclosed having improved solubility and/or stability while retaining glucagon agonist activity. The glucagon peptides have been modified by the substitution of pyridyl-alanine for a native amino acid at one or more of positions 6, 10 or 13 and/or substitution with an amino acid in the D-conformation at position 20 or 21 compared to native glucagon.
-
Patent Agency Ranking
公开(公告)号：US10137170B2
公开(公告)日：2018-11-27
申请号：US15102340
申请日：2014-12-19
Inventor： Sara Belli , Konrad Bleicher , Richard D. Dimarchi , Eike Hoffmann , Eric A. Kitas , Anish A. Konkar
IPC: A61K38/26 , C07K14/605 , A61K45/06 , A61K47/54 , A61K38/00
Abstract: 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.
-
公开(公告)号：US09868772B2
公开(公告)日：2018-01-16
申请号：US14408813
申请日：2013-06-18
Inventor： Richard D. Dimarchi , David L. Smiley , Konrad H. Bleicher , Eric A. Kitas
IPC: A61K38/26 , A61K38/28 , A61K38/00 , A61P3/10 , A61P7/12 , C07K14/605 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC classification number: C07K14/605 , A61K38/26
Abstract: 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.
-
公开(公告)号：US09593156B2
公开(公告)日：2017-03-14
申请号：US14431040
申请日：2013-09-25
Inventor： Richard D. Dimarchi , Yan Zhao
Abstract: 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.
Abstract translation: 本文公开了具有基于胰岛素多肽序列，二聚化位点和连接两个胰岛素多肽的二聚连接体长度的独特的胰岛素受体激动剂活性的胰岛素类似物二聚体。 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，并且第一和第二胰岛素多肽通过B29-B29'，B1-C8，B1-B1或 C8-C8键。
-
公开(公告)号：US20160115215A1
公开(公告)日：2016-04-28
申请号：US14981187
申请日：2015-12-28
Inventor： Richard D. Dimarchi , Brian P. Ward
IPC: C07K14/605
CPC classification number: C07K14/605 , A61K38/00
Abstract: 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.
-
公开(公告)号：US20150274802A1
公开(公告)日：2015-10-01
申请号：US14431040
申请日：2013-09-25
Inventor： Richard D. Dimarchi , Yan Zhao
Abstract: 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.
Abstract translation: 本文公开了具有基于胰岛素多肽序列，二聚化位点和连接两个胰岛素多肽的二聚连接体长度的独特的胰岛素受体激动剂活性的胰岛素类似物二聚体。 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，并且第一和第二胰岛素多肽通过B29-B29'，B1-C8，B1-B1或 C8-C8键。
-
-
-
-
-
-
-
-
-
Search Results
10
records
(took 0.041 seconds)
