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    MODULAR TRANSPORT PLATFORM FOR TARGETED DELIVERY OF THERAPEUTIC AGENTS
    3.
    发明公开
    MODULAR TRANSPORT PLATFORM FOR TARGETED DELIVERY OF THERAPEUTIC AGENTS 审中-公开
    模块化传输平台药物靶向输送

    公开(公告)号：EP2714091A2

    公开(公告)日：2014-04-09

    申请号：EP12723905.1

    申请日：2012-02-13

    申请人： Contango Partners Group, Inc.

    发明人： SOBOLEV, Alexander, S. ,  ROSENKRANZ, Audrey, A. ,  JANS, David, A. ,  LUNIN, Vladimir, G.

    IPC分类号： A61K47/48 ,  A61K41/00 ,  A61K51/08 ,  A61P35/00

    CPC分类号： A61K47/48269 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/642 ,  A61K47/6445 ,  A61K51/081 ,  A61K51/088

    摘要： The invention relates to a modular transport platform (MTP) for delivering active, diagnostic or research substances to predesigned intracellular compartments of target cells. The MTP includes functional modules within one molecule to accomplish one or more of the following: penetration of the modular transport platform into a target cell type, pH-dependent membrane disruption activity within the target cell, directed intracellular transport into preselected intracellular compartment, and delivery of a substance to be transported to the intracellular compartment. The modular transport platform includes the following modules: (1) a ligand module to target a specific receptor on the surface of the target cell; (2) an endosomolytic module that provides pH-dependent membrane disruption activity within the target cell; (3) an intracellular transport module to cause delivery of the MTP to a particular subcellular compartment; (4) a module for intracellular retention to ensure retention of the MTP within the subcellular compartment of the target cell; (5) a module for subcellular recognition; (6) a substance to be transported by the MTP; and (7) a carrier module for unifying the modules and coupling the modules with the transported substance.

    GLP-1 PRODRUGS
    8.
    发明公开
    GLP-1 PRODRUGS 审中-公开
    GLP-1的前药

    公开(公告)号：EP2820038A1

    公开(公告)日：2015-01-07

    申请号：EP13705822.8

    申请日：2013-02-26

    申请人： Novo Nordisk A/S

    发明人： NORRILD, Jens Christian

    IPC分类号： C07K14/605 ,  A61K38/26

    CPC分类号： A61K47/48269 ,  A61K38/00 ,  A61K38/26 ,  A61K47/642 ,  C07K14/575 ,  C07K14/605

    摘要： The invention relates to a GLP-1 prodrug of the general formula I: R1-(NHXaa1)-Xaa2-(OHis)-(GLP-1 peptide) (Formula I), wherein GLP-1 peptide is GLP-1(8-37) (SEQ ID NO: 1) or an analog thereof having a maximum of nine amino acid changes as compared to GLP-1(8-37), R1 is lower alkyl, (NHXaa1) is an amino acid, Xaa2 is an amino acid, and (OHis) is a radical of imidazole-lactic acid; or a pharmaceutically acceptable salt, amide, or ester of the prodrug. The invention also relates to specific GLP-1 parent drugs of the general formula II: (HOHis)-(GLP-1 peptide) (Formula II), as well as specific intermediate products. The invention furthermore relates to a method of achieving release in vivo of an active and stabilized GLP-1 parent drug of the general formula II: (HOHis)-(GLP-1 peptide), by administering a GLP-1 prodrug; as well as to such GLP-1 prodrug, and such GLP-1 parent drug, respectively, for use as a medicament, in particular for use in the treatment and/or prevention of all forms of diabetes and related diseases. The prodrug may be used to alter the PK and/or absorption profile of the drug, for example to a desirable bell-shaped curve. The parent drug has a good biological activity, and is stabilized against degradation by DPP-IV.