- 专利标题: Conjugate based systems for controlled insulin delivery
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申请号: US16771818申请日: 2018-12-13
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公开(公告)号: US11820805B2公开(公告)日: 2023-11-21
- 发明人: Lin Yan , Pei Huo , Ahmet Kekec , Danqing D. Feng , Yuping Zhu , Dmitri Pissarnitski , Chris Moyes , Songnian Lin
- 申请人: Merck Sharp & Dohme Corp. , Lin Yan , Pei Huo , Ahmet Kekec , Danqing D. Feng , Yuping Zhu , Dmitri Pissarnitski , Chris Moyes , Songnian Lin
- 申请人地址: US NJ Rahway
- 专利权人: MERCK SHARP & DOHME LLC
- 当前专利权人: MERCK SHARP & DOHME LLC
- 当前专利权人地址: US NJ Rahway
- 代理商 Julie M. Lake; Catherine D. Fitch
- 国际申请: PCT/US2018/065318 2018.12.13
- 国际公布: WO2019/125878A 2019.06.27
- 进入国家日期: 2020-06-11
- 主分类号: C07K14/62
- IPC分类号: C07K14/62 ; A61K47/61 ; A61K47/54 ; A61K38/00
摘要:
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.
公开/授权文献
- US20210198339A1 CONJUGATE BASED SYSTEMS FOR CONTROLLED INSULIN DELIVERY 公开/授权日:2021-07-01
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