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公开(公告)号：US11773150B2
公开(公告)日：2023-10-03
申请号：US17004395
申请日：2020-08-27
发明人： Paul E. Carrington , Grigori Ermakov , Robert M. Garbaccio , Wolfgang Seghezzi , Elisabetta Bianchi , Federica Orvieto , Dennis Gately , Nick Knudsen , Anthony Manibusan
CPC分类号： C07K14/605 , A61K47/6811 , A61K47/6843 , A61P3/10 , C07K16/26 , C07K16/2869 , A61K2039/505 , C07K2317/75 , C07K2319/00
摘要： Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
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公开(公告)号：US20230285514A1
公开(公告)日：2023-09-14
申请号：US17785279
申请日：2020-12-18
申请人： Elisabetta BIANCHI , Paul E. CARRINGTON , Qiaolin DENG , Songnian LIN , Federica ORVIETO , Anandan PALANI , Antonello PESSI , Tomi K. SAWYER , Merck Sharp & Dohme LLC
发明人： Elisabetta Bianchi , Paul E. Carrington , Qiaolin Deng , Songnian Lin , Federica Orvieto , Anandan Palani , Antonello Pessi , Tomi K. Sawyer
IPC分类号： A61K38/26 , A61K38/28 , C07K14/605
CPC分类号： A61K38/26 , A61K38/28 , C07K14/605
摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
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公开(公告)号：US20240287138A1
公开(公告)日：2024-08-29
申请号：US18429587
申请日：2024-02-01
发明人： Kaustav Biswas , Nicolas C. Boyer , Brandon D. Cash , Fa-Xiang Ding , John R. Frost , Michael B. Garrigou , James P. Jewell , Ahmet Kekec , Hu-Jung Julie Lee , Songnian Lin , Ashwin U. Rao , Daniel J. Sindhikara , Murray Wan , Yuping Zhu , Susan L. Zultanski , Tony Siu , Andrew M. Haidle , Claudio Mapelli , Luca Gambini , Federica Orvieto , Roberta Tozzi , Nicolo Maria Pasquini , Luigi Abate , Giordano Proietti , Michael Wuo , Ryan Chau
摘要： Provided are compounds of the Formula (I), or their pharmaceutically acceptable salts,
can inhibit TNFR1 and are expected to have utility as therapeutic agents, for example, for treating inflammatory bowel diseases, rheumatoid arthritis, junvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, ankylosing spondylitis, non-radiographic axial spondyloarthritis and hidradenitis suppurativa. The disclosure also provides pharmaceutical compositions which comprise the compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of inflammatory bowel diseases, rheumatoid arthritis, juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, ankylosing spondylitis, non-radiographic axial spondyloarthritis and hidradenitis suppurativa, and for preparing pharmaceuticals for this purpose.-
公开(公告)号：US20230063794A1
公开(公告)日：2023-03-02
申请号：US17785287
申请日：2020-12-18
发明人： Elisabetta Bianchi , Qiaolin Deng , Songnian Lin , Federica Orvieto , Anandan Palani , Antonello Pessi , Tomi K. Sawyer
IPC分类号： A61K38/26 , C07K14/605 , A61K38/28
摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
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公开(公告)号：US20230270825A1
公开(公告)日：2023-08-31
申请号：US17785772
申请日：2020-12-18
发明人： Elisabetta Bianchi , Qiaolin Deng , Songnian Lin , Federica Orvieto , Anandan Palani , Antonello Pessi , Tomi K. Sawyer
IPC分类号： A61K38/26 , C07K14/605 , A61K38/28 , C07K1/107
CPC分类号： A61K38/26 , A61K38/28 , C07K1/1077 , C07K14/605
摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
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公开(公告)号：US10800826B2
公开(公告)日：2020-10-13
申请号：US15765505
申请日：2016-10-04
发明人： Paul Carrington , Grigori Ermakov , Robert M. Garbaccio , Wolfgang Seghezzi , Elisabetta Bianchi , Federica Orvieto , Dennis Gately , Nick Knudsen , Anthony Manibusan
摘要： Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
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