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1.发明授权SINGLE CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR 有权具有高活性对胰岛素受体的单链胰岛素激动剂
公开(公告)号：EP2582719B1
公开(公告)日：2016-08-10
申请号：EP11796430.4
申请日：2011-06-16
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2.发明公开SINGLE CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR 有权具有高活性对胰岛素受体的单链胰岛素激动剂
公开(公告)号：EP2582719A2
公开(公告)日：2013-04-24
申请号：EP11796430.4
申请日：2011-06-16
发明人： DIMARCHI, Richard, D. , AZRIEL, Julia , KAUR, Zach , MEYERS, Jonathan , PARODY, Todd , ZHAO, Yan
摘要： Single chain insulin analogs are provided having high potency and specificity for the insulin receptor. As disclosed herein optimally sized linking moieties can be used to link human insulin A and B chains, or analogs or derivatives thereof, wherein the carboxy terminus of the B25 amino acid of the B chain is linked to the amino terminus of the A1 amino acid of the A chain via the intervening linking moiety. In on embodiment the linking moiety comprises a polyethylene glycol of 6-16 monomer units and in an alternative embodiment the linking moiety comprises a non-native amino acid sequence derived form the IGF-1 C-peptide and comprising at least 8 amino acids and no more than 12 amino acid in length. Also disclosed are prodrug and conjugate derivatives of the single chain insulin analogs.
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