公开(公告)号：US20190169257A1

公开(公告)日：2019-06-06

申请号：US16320997

申请日：2017-08-01

申请人： JIANGSU HENGRUI MEDICINE CO., LTD.

发明人： Deyu LIU ,  Hongwei WANG ,  Liang ZHAO ,  Feifei WANG ,  Xiang ZENG ,  Tao WANG ,  Yali WANG ,  Yulu DAI

IPC分类号： C07K14/62 ,  C07K1/06 ,  A61K38/28 ,  A61P3/10 ,  C07K1/107

摘要： Provided is an acylated derivative of human insulin or an analogue thereof. Specifically disclosed is an acylated derivative of a human insulin analogue, or zinc complex thereof; said acylated derivative is longer-lasting than existing insulin analogues and acylated derivatives thereof, its blood glucose reduction is more steady, and it is more stable in storage.

公开(公告)号：US10280206B2

公开(公告)日：2019-05-07

申请号：US15540829

申请日：2015-12-18

申请人： DH Technologies Development PTE Ltd.

发明人： Yves Le Blanc

IPC分类号： C12N9/00 ,  C07K14/62 ,  C07K16/00 ,  G01N30/06 ,  G01N30/12 ,  G01N30/30 ,  G01N30/72 ,  G01N30/88 ,  G01N33/68

摘要： Methods and systems are provided herein for on-line preparation of a sample for mass spectrometry. In accordance with various aspects of applicant's teachings, the methods and systems can provide for the reduction of a polypeptide, for example, on a liquid chromatography column and can reduce or eliminate the need to incubate the reducing agent with the polypeptide and/or expose the reduced polypeptide to an alkylating agent.

公开(公告)号：US10265416B2

公开(公告)日：2019-04-23

申请号：US15904248

申请日：2018-02-23

申请人： École Polytechnique Fédérale de Lausanne (EPFL)

发明人： Jeffrey A. Hubbell ,  Stephan Kontos ,  Karen Y. Dane

IPC分类号： A61K9/51 ,  C12N9/82 ,  C07K7/08 ,  C12N9/96 ,  A61K38/00 ,  A61K39/00 ,  A61K47/64 ,  A61K47/68 ,  A61K9/107 ,  C07K16/18 ,  C07K14/62 ,  C07K14/74 ,  C07K16/28

摘要： Peptides that specifically bind erythrocytes are described. These are provided as peptidic ligands having sequences that specifically bind, or as antibodies or fragments thereof that provide specific binding, to erythrocytes. The peptides may be prepared as molecular fusions with therapeutic agents, tolerizing antigens, or targeting peptides. Immunotolerance may be created by use of the fusions and choice of an antigen on a substance for which tolerance is desired.

公开(公告)号：US20190092833A1

公开(公告)日：2019-03-28

申请号：US16199774

申请日：2018-11-26

申请人： Merck Sharp & Dohme Corp.

发明人： Songnian Lin ,  Lin Yan ,  Pei Huo ,  Dmitri Pissarnitski ,  Danqing Feng ,  Ravi Nargund ,  Yuping Zhu ,  Ahmet Kekec ,  Christina B. Madsen-Duggan ,  Zhi-Cai Shi ,  Zhicai Wu ,  Yingjun Mu

IPC分类号： C07K14/62 ,  A61K47/60 ,  A61K38/28 ,  A61K47/55 ,  A61K38/00

摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

公开(公告)号：US10233225B2

公开(公告)日：2019-03-19

申请号：US15229942

申请日：2016-08-05

申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION

发明人： Richard D. DiMarchi ,  Yulia Azriel ,  Zachary Kaur ,  Jonathan Meyers ,  Todd Parody ,  Yan Zhao

IPC分类号： A61K38/00 ,  A61K38/18 ,  A61K38/28 ,  C07K14/62 ,  C07K14/475 ,  A61K47/60

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.

公开(公告)号：US10227390B2

公开(公告)日：2019-03-12

申请号：US14898222

申请日：2014-06-13

申请人： President and Fellows of Harvard College

发明人： Gregory L. Verdine ,  Gerard Hilinski ,  Rebecca Yue Liang ,  Yvonne Alice Nagel ,  Minyun Zhou

IPC分类号： C07K14/62 ,  C07K14/72 ,  A61K38/00

摘要： Provided herein are stabilized α-CT polypeptides comprising an alpha-helical segment, and wherein the polypeptide is of Formula (I-1) or Formula (I-2): Rf—[XAA]s—XA1—XA2—XA3—XA4—XA5—XA6—XA7—XA8—XA9—XA10—XA11—XA12—XA13—XA14—[XAA]t—Re (I-1) Rf—[XAA]s—XC1—XC2—XC3—XC4—XC5—XC6—XC7—XC8—XC9—XC10—XC11—XC12—XC13—XC14—XC15—XC16—XC17—XC18—XC19—XC20—[XAA]t—Re (I-2) wherein the α-CT polypeptide binds to the insulin receptor, and wherein the α-CT polypeptide includes at least one staple (i.e. two cross-linked amino acids) and/or at least one stitch (i.e. three cross-linked amino acids). Further provided are insulin analogs including the stapled or stitched α-CT polypeptides, pharmaceutical compositions thereof, methods of use, e.g., methods of treating a diabetic condition or complications thereof.

公开(公告)号：US10179151B2

公开(公告)日：2019-01-15

申请号：US14983657

申请日：2015-12-30

申请人： ORGENESIS LTD. ,  TEL HASHOMER-MEDICAL RESEARCH, INFRASTRUCTURE AND SERVICES LTD.

发明人： Sarah Ferber

IPC分类号： C12N5/07 ,  A61K35/39 ,  C12N15/09 ,  C12N15/63 ,  C07K14/62 ,  C12N5/071 ,  C12N15/86 ,  A61K38/00

摘要： Disclosed herein is a method for manufacturing a population of human insulin producing cells from non-pancreatic β-cells, wherein the resulting insulin producing cells have increased insulin content, or increased glucose regulated secretion of insulin, or a combination of both.

公开(公告)号：US20190010206A1

公开(公告)日：2019-01-10

申请号：US15754173

申请日：2016-08-24

申请人： Novo Nordisk A/S

发明人： Peter Madsen ,  Martin Muenzel ,  Claudia Ulrich Hjoerringgaard ,  Susanne Hostrup ,  Tine Glendorf ,  Mathias Norrman ,  Christian Fledelius

IPC分类号： C07K14/62 ,  A61K38/28 ,  A61K31/4406 ,  A61P3/10

摘要： The present invention is in the therapeutic fields of drugs for medical conditions relating to diabetes. More specifically the invention relates to novel acylated derivatives of human insulin analogues. The invention also provides pharmaceutical compositions comprising such insulin derivatives, and relates to the use of such derivatives for the treatment or prevention of medical conditions relating to diabetes.

公开(公告)号：US20180371045A1

公开(公告)日：2018-12-27

申请号：US16040684

申请日：2018-07-20

申请人： Novo Nordisk A/S

发明人： Thomas Hoeg-Jensen ,  Palle Jakobsen ,  Ulrich Sensfuss ,  Christian Fledelius ,  Ulla Ribel-Madsen

IPC分类号： C07K14/62 ,  A61K38/00

摘要： The novel insulin derivates delivers, after administration to humans, insulin as a function of the glucose concentration in the tissue.

公开(公告)号：US20180340015A1

公开(公告)日：2018-11-29

申请号：US15983167

申请日：2018-05-18

申请人： Eli Lilly and Company

发明人： Wen Liu ,  Adam Robert Mezo ,  Francisco Alcides Valenzuela

IPC分类号： C07K14/62 ,  A61P3/10

CPC分类号： C07K14/62 ,  A61K38/00 ,  A61K47/542 ,  A61K47/65 ,  A61P3/10

摘要： The presently described compounds relate to the treatment of diabetes and/or hyperglycemia. More particularly, the described compounds relate to acylated insulin compounds that lower blood glucose, pharmaceutical compositions containing such compounds, therapeutic uses of such compounds, and an intermediate compound used to make the acylated insulin compounds.