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公开(公告)号：US11566057B2
公开(公告)日：2023-01-31
申请号：US16643881
申请日：2018-09-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： Anandan Palani , Qiaolin Deng , Chunhui Huang , Yuping Zhu , Elisabetta Bianchi , Federica Orvieto
Abstract: Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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2.发明授权公开(公告)号：US11041009B2
公开(公告)日：2021-06-22
申请号：US16495703
申请日：2018-03-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： Danqing Feng , Pei Huo , Ahmet Kekec , Songnian Lin , Christopher R. Moyes , Ravi Nargund , Brenda Pipik , Dmitri A. Pissarnitski , Lin Yan , Yuping Zhu
Abstract: An insulin conjugate comprising or consisting of a tri-valent sugar cluster is described. In particular aspects, the insulin conjugate displays a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
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公开(公告)号：US20190092833A1
公开(公告)日：2019-03-28
申请号：US16199774
申请日：2018-11-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： 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
Abstract: 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：US20210177981A1
公开(公告)日：2021-06-17
申请号：US16771819
申请日：2018-12-13
Applicant: Merck Sharp & Dohme Corp. , SmartCells,Inc.
Inventor： Lin Yan , Pei Huo , Ahmet Kekec , Yuping Zhu , Dmitri Pissarnitski , Danqing D. Feng , Chris Moyes , Zhiqiang Zhao , David N. Hunter , Songnian Lin , Thomas M. Lancaster , Benjamin Chen
Abstract: 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：US10800827B2
公开(公告)日：2020-10-13
申请号：US16199774
申请日：2018-11-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： 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
Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
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Patent Agency Ranking
公开(公告)号：US11820805B2
公开(公告)日：2023-11-21
申请号：US16771818
申请日：2018-12-13
Applicant: Merck Sharp & Dohme Corp. , Lin Yan , Pei Huo , Ahmet Kekec , Danqing D. Feng , Yuping Zhu , Dmitri Pissarnitski , Chris Moyes , Songnian Lin
Inventor： Lin Yan , Pei Huo , Ahmet Kekec , Danqing D. Feng , Yuping Zhu , Dmitri Pissarnitski , Chris Moyes , Songnian Lin
CPC classification number: C07K14/62 , A61K47/549 , A61K47/61 , A61K38/00
Abstract: The present disclosure provides conjugates that comprise an insulin molecule conjugated via a conjugate framework to two or more separate ligands that each include a saccharide, wherein the framework, ligand, saccharide and insulin molecule optionally comprise a fatty chain (e.g., a C8-30 fatty chain), wherein when said insulin molecule is conjugated both to a C8-30 fatty chain and one or more separate ligands that each include a saccharide, said C8-30 fatty chain is linked to insulin molecule only, and wherein when the framework or ligand comprises a fatty chain the insulin molecule is conjugated to two or more separate ligands. 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：US20220233647A1
公开(公告)日：2022-07-28
申请号：US17614680
申请日：2020-06-01
Applicant: Merck Sharp & Dohme Corp.
Inventor： Danqing Feng , Songnian Lin , Dmitri A. Pissarnitski , Brenda Pipik , Lin Yan , Yuping Zhu
Abstract: Glucose-responsive insulin conjugates that contain one or more linear oligomer sugar cluster are provided. Such insulin conjugates that may display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose, even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule.
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公开(公告)号：US20190177393A1
公开(公告)日：2019-06-13
申请号：US16301010
申请日：2017-05-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： Songnian Lin , Lin Yan , Pei Huo , Dmitri Pissarnitski , Danqing Feng , Ravi Nargund , Christina Madsen-Duggan , Yuping Zhu , Ahmet Kekec , Zhicai Wu
Abstract: 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：US10017556B2
公开(公告)日：2018-07-10
申请号：US14945461
申请日：2015-11-19
Applicant: MERCK SHARP & DOHME CORP.
Inventor： 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
Abstract: 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：US20170107268A1
公开(公告)日：2017-04-20
申请号：US14945461
申请日：2015-11-19
Applicant: MERCK SHARP & DOHME CORP.
Inventor： 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: C07K14/62
Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
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