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公开(公告)号：US09758563B2
公开(公告)日：2017-09-12
申请号：US14745859
申请日：2015-06-22
申请人： Michael Weiss
发明人： Michael Weiss
摘要： An insulin analog comprises a B-chain polypeptide incorporating a chlorinated phenylalanine. The chlorinated phenylalanine may be located at position B24. The chlorinated phenylalanine may be para-monochloro-phenylalanine. The analog may be of a mammalian insulin, such as human insulin. A nucleic acid encodes such an insulin analog. The chlorinated insulin analogs retain significant activity. A method of treating a patient comprises administering a physiologically effective amount of the insulin analog or a physiologically acceptable salt thereof to a patient. Chlorine substitution-based stabilization of insulin may reduce fibrillation and thereby enhance the treatment of diabetes mellitus in regions of the developing world lacking refrigeration.
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公开(公告)号：US20170252410A1
公开(公告)日：2017-09-07
申请号：US15468083
申请日：2017-03-23
摘要： The invention provides non-hormonal vitamin D conjugated to insulin peptides that result in the peptides having increased absorption, bioavailability or circulating half-life when compared to non-conjugated forms. The vitamin D targeting groups are coupled to the insulin peptides via the third carbon on the vitamin D backbone.
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公开(公告)号：US09745359B2
公开(公告)日：2017-08-29
申请号：US14402074
申请日：2013-05-17
申请人： ADDA Biotech Inc.
发明人： Shulin Qin
IPC分类号： A61K36/26 , C07K14/545 , C07K14/605 , C07K14/575 , C07K14/62 , C07K14/645 , A61K38/00
CPC分类号： C07K14/545 , A61K38/00 , C07K14/575 , C07K14/605 , C07K14/62 , C07K14/645 , C07K2319/00 , C07K2319/31 , C07K2319/74
摘要： The present invention relates to the field of biopharmaceutics, and in particular to a protein, a protein conjugate, a pharmaceutical composition and its use for treating diabetes. The fusion protein of the present invention is obtained by linking two polypeptides, wherein one polypeptide is an interleukin-1 receptor antagonistic protein or an analog thereof, and another polypeptide is GLP-1 receptor binding polypeptide or an analog thereof, or an insulin receptor binding polypeptide or an analog thereof, or a GIP receptor binding polypeptide or an analog thereof. The fusion proteins of the present invention and conjugates thereof have a significant efficacy in treating diabetes, and can be used in a lower dose, resulting in a marked reduction in side effects.
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公开(公告)号：US09718868B2
公开(公告)日：2017-08-01
申请号：US14424493
申请日：2013-08-28
IPC分类号： A61K47/48 , A61K38/29 , A61K31/663 , C07K14/635 , A61P19/02 , C07K14/62 , C07K14/65 , C08F299/02
CPC分类号： C07K14/62 , A61K31/663 , A61K38/29 , A61K47/548 , A61K47/60 , C07K14/635 , C07K14/65 , C08F299/02
摘要： Described herein is insulin, an insulin-like growth factor, parathyroid hormone, a fragment of parathyroid hormone, or a parathyroid hormone related protein that includes at least one bone targeting moiety, wherein the bone targeting moiety is covalently bonded to the peptide. Also described herein are the methods of making these compositions that prevent or treat conditions associated with bone loss and preventing bone fractures, and/or the inability to initiate de novo bone turnover and stimulate bone fracture repair.
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公开(公告)号：US09714274B2
公开(公告)日：2017-07-25
申请号：US14387456
申请日：2013-03-25
发明人： Wenshe Liu , Wei Wan
IPC分类号： C12N15/09 , C07K14/435 , C07K14/585 , C07K14/605 , C07K14/62 , C07K14/635
CPC分类号： C07K14/43595 , C07K14/585 , C07K14/605 , C07K14/62 , C07K14/635 , C07K2319/00 , C07K2319/21 , C07K2319/50
摘要： The present disclosure pertains to methods of producing recombinant peptides that contain between 10 and 200 amino acid residues using novel carrier proteins derived from superfolder green fluorescent protein and its mutants.
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106.发明申请公开(公告)号：US20170204375A1
公开(公告)日：2017-07-20
申请号：US15321504
申请日：2015-06-26
发明人： Domenico Accili , Ryotaro Bouchi
IPC分类号： C12N5/071 , A61K35/38 , C12N15/113 , A61L27/36 , C07K14/62 , A61K38/28 , C07K16/40 , A61L27/38
CPC分类号： C12N5/0679 , A61K35/38 , A61K38/28 , A61L27/3687 , A61L27/3813 , A61L27/383 , A61L27/3882 , A61L2430/22 , C07K14/62 , C07K16/40 , C12N15/113 , C12N15/1137 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2310/531 , C12N2506/23 , C12Y114/16004 , C12Y401/01028
摘要： Disclosed herein are methods involving the targeting of 5HT biosynthesis in gut insulin-negative cells to convert them into insulin-positive cells. Also disclosed are methods for treating a disease or disorder in a mammal, preferably a human, associated with impaired pancreatic endocrine function, by administering a therapeutically effective amount of an enumerated active agent that reduces the expression, biosynthesis, signaling or biological activity of serotonin or increases its degradation, wherein administering comprises delivering the agent to Gut Ins− cells in the mammal. Other embodiments of the method are directed to therapy wherein an agent that significantly reduces FOXO1 expression, biosynthesis, signaling or biological activity or increases its degradation is administered in addition to the agent that reduces serotonin, or alternatively an agent that reduces FOXO1 expression is targeted to serotonin-positive gut enteroendocrine cells.
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公开(公告)号：US09644017B2
公开(公告)日：2017-05-09
申请号：US12820722
申请日：2010-06-22
申请人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
发明人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
摘要： The invention relates to novel insulin analogs having a basal time-action profile, which are characterized by the following features: a) the B chain end consists of an amidated basic amino acid residue such as lysine or arginine amide; b) the N-terminal amino acid residue of the insulin A chain is a lysine or arginine radical; c) the amino acid position A8 is occupied by a histidine radical; d) the amino acid position A21 is occupied by a glycine radical; and e) one or more substitutions and/or additions of negatively charged amino acid residues are carried out in the positions A5, A15, A18, B-1, B0, B1, B2, B3 and B4.
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公开(公告)号：US20170081359A1
公开(公告)日：2017-03-23
申请号：US15267995
申请日：2016-09-16
发明人： Dale Arlington Thomas, III , Alexander James Mijalis , Bradley L. Pentelute , Mark David Simon , Andrea Adamo , Patrick Louis Heider , Klavs F. Jensen
CPC分类号： C07K1/084 , B01J19/24 , B01J2219/24 , C07K1/045 , C07K7/06 , C07K14/47 , C07K14/60 , C07K14/61 , C07K14/62
摘要： Methods and system for solid phase peptide synthesis are provided. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. New amino acid residues are added via a coupling reaction between an activated amino acid and an amino acid residue of the immobilized peptide. Amino acids may be activated using, e.g., a base and an activating agent. Certain inventive concepts, described herein, relate to methods and systems for the activation of amino acids. These systems and methods may allow for fewer side reactions and a higher yield compared to conventional activation techniques as well as the customization of the coupling reaction on a residue-by-residue basis without the need for costly and/or complex processes.
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公开(公告)号：US20170081358A1
公开(公告)日：2017-03-23
申请号：US15268032
申请日：2016-09-16
发明人： Dale Arlington Thomas, III , Alexander James Mijalis , Bradley L. Pentelute , Mark David Simon , Surin Mong
IPC分类号： C07K1/04 , C07K14/47 , C07K14/61 , G01N21/33 , G01N33/487 , G01N21/27 , G01N21/3577 , C07K7/06 , C07K14/62
CPC分类号： C07K1/045 , C07K7/06 , C07K14/47 , C07K14/60 , C07K14/61 , C07K14/62 , G01N21/272 , G01N21/33 , G01N21/3577 , G01N33/48707 , G01N2021/8416
摘要： Methods and systems for control of solid phase peptide synthesis are generally described. Control of solid phase peptide synthesis involves the use of feedback from one or more reactions and/or processes (e.g., reagent removal) taking place in the solid phase peptide synthesis system. In some embodiments, a detector may detect one or more fluids flowing across a detection zone of a solid phase peptide synthesis system and one or more signals may be generated corresponding to the fluid(s). For instance, an electromagnetic radiation detector positioned downstream of a reactor may detect a fluid exiting the reactor after a deprotection reactor and produce a signal(s). In some embodiments, based at least in part on information derived from the signal(s), a parameter of the system may be modulated prior to and/or during one or more subsequent reactions and/or processes taking place in the solid phase peptide synthesis system. In some embodiments, the methods and systems, described herein, can be used to conduct quality control to determine and correct problems (e.g., aggregation, truncation, deletion) in reactions (e.g., coupling reactions) taking place in the solid phase peptide synthesis system.
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公开(公告)号：US09593156B2
公开(公告)日：2017-03-14
申请号：US14431040
申请日：2013-09-25
发明人： Richard D. Dimarchi , Yan Zhao
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，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。
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