发明名称 |
GLUCOSE-RESPONSIVE INSULIN CONJUGATES |
摘要 |
Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates 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 such as Con A. |
申请公布号 |
US2016251407(A1) |
申请公布日期 |
2016.09.01 |
申请号 |
US201415025912 |
申请日期 |
2014.10.02 |
申请人 |
LIN Songnian;YAN Lin;KEKEC Ahmet;ZHU Yuping;HUNTER David N.;HUO Pei;FENG Danqing;NARGUND Ravi P.;MOYES Christopher R.;ZHAO Zhiqiang;PIPIK Brenda;PISSARNITSKI Dimitri;DUFFY Joseph L.;GUIDRY Erin N.;MERCK SHARP & DOHME CORP. |
发明人 |
Lin Songnian;Yan Lin;Kekec Ahmet;Zhu Yuping;Hunter David N.;Huo Pei;Feng Danqing;Nargund Ravi P.;Moyes Christopher R.;Zhao Zhiqiang;Pipik Brenda;Pissarnitski Dmitri;Duffy Joseph L.;Guidry Erin |
分类号 |
C07K14/62;A61K38/28;A61K47/48 |
主分类号 |
C07K14/62 |
代理机构 |
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代理人 |
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主权项 |
1: A conjugate comprising:
an insulin or insulin analog molecule covalently attached to at least one branched linker having a first arm and second arm, wherein the first arm is linked to a first ligand that includes a first saccharide and the second arm is linked to a second ligand that includes a second saccharide and wherein the first saccharide is fucose and wherein the second saccharide is a mannose, glucosamine, glucose, bisaccharide, trisaccharide, tetrasaccharide, branched trisaccharide, bimannose, trimannose, tetramannose, or branched trimannose. |
地址 |
Kenilworth NJ US |