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公开(公告)号：US11827684B2
公开(公告)日：2023-11-28
申请号：US17234844
申请日：2021-04-20
发明人： Cristina Abrahams , Edward Bowman , Xiaofan Li , Songnian Lin , Willy Solis , Ryan Stafford , Aarron Willingham , Alice Yam , Junhao Yang , Gang Yin
CPC分类号： C07K14/55 , A61K38/2013 , A61K47/545 , A61K47/60 , A61P5/00 , C07K16/2818 , C07K16/2827 , A61K38/00
摘要： Interleukin-2 (IL-2) conjugates comprising at least one or more amino acid substitutions that bias binding to the IL-2 receptor βγc dimer over binding the IL-2 receptor αβγc trimer and a non-natural amino acid at or near the N-terminus conjugated to a water-soluble polymer are described. The IL-2 conjugates are useful for treatment and prevention of cell proliferation and cancer in a patient.
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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：US20230365646A1
公开(公告)日：2023-11-16
申请号：US18362417
申请日：2023-07-31
发明人： Sobhana Babu Boga , Ahmet Kekec , Songnian Lin , Craig A. Parish , Weijuan Tang , Lin Yan
摘要： The present invention relates to insulin analogues and processes of making such insulin analogues by direct conversion of a free amine to an azide via diazo-transfer with an azotransfer agent.
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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：US11413352B2
公开(公告)日：2022-08-16
申请号：US16771819
申请日：2018-12-13
发明人： Chris Moyes , Songnian Lin
摘要： The present disclosure provides conjugates which comprise an insulin molecule conjugated via a conjugate framework to one or more separate ligands that include a first saccharide, and wherein the conjugate framework also comprises a fatty chain (e.g., a C8-30 fatty chain). In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
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公开(公告)号：US20240101631A1
公开(公告)日：2024-03-28
申请号：US18484870
申请日：2023-10-11
发明人： Cristina Abrahams , Edward Bowman , Xiaofan Li , Songnian Lin , Willy Solis , Ryan Stafford , Aarron Willingham , Alice Yam , Junhao Yang , Gang Yin
CPC分类号： C07K14/55 , A61K38/2013 , A61K47/545 , A61K47/60 , A61P35/00 , C07K16/2818 , C07K16/2827 , A61K38/00
摘要： Interleukin-2 (IL-2) conjugates comprising at least one or more amino acid substitutions that bias binding to the IL-2 receptor βγc dimer over binding the IL-2 receptor αβγc trimer and a non-natural amino acid at or near the N-terminus conjugated to a water-soluble polymer are described. The IL-2 conjugates are useful for treatment and prevention of cell proliferation and cancer in a patient.
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公开(公告)号：US20240294596A1
公开(公告)日：2024-09-05
申请号：US18041815
申请日：2021-09-07
发明人： Dmitri A. Pissarnitski , Danqing Feng , Pei Huo , Ahmet Kekec , Songnian Lin , Ravi Nargund , Zhicai Shi , Zhicai Wu , Lin Yan , Yuping Zhu
CPC分类号： C07K14/62 , A61K38/28 , A61K45/06 , A61P3/10 , C07K1/1077
摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
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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：US20230310551A1
公开(公告)日：2023-10-05
申请号：US18041825
申请日：2021-08-24
发明人： Christina B. Madsen-Duggan , Danqing Feng , Pei Huo , Ahmet Kekec , Songnian Lin , Ravi Nargund , Christopher R. Moyes , Dmitri A. Pissarnitski , Zhicai Shi , Zhicai Wu , Lin Yan , Yuping Zhu
摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
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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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