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    Diagnostic imaging contrast agents with extended blood retention
    1.
    发明公开
    Diagnostic imaging contrast agents with extended blood retention 失效
    造影剂与血液中的延长停留时间，诊断成像

    公开(公告)号：EP1716871A3

    公开(公告)日：2011-04-27

    申请号：EP06016539.6

    申请日：1996-01-16

    申请人： EPIX Pharmaceuticals, Inc.

    发明人： McMurry, Thomas, J. ,  Sajiki, Hironao ,  Scott, Daniel, M. ,  Lauffer, Randall, B.

    IPC分类号： A61K49/00 ,  A61K51/04

    CPC分类号： A61K49/085 ,  A61B6/507 ,  A61K49/0002 ,  A61K49/10 ,  A61K49/103 ,  A61K49/106 ,  C07F9/091

    摘要： The present invention provides diagnostic imaging contrast agents which exhibit improved blood retention. The novel compounds comprise: a) an image-enhancing (or signal-generating) moiety (IEM); b) a plasma protein binding moiety (PPBM); and c) a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging. These contrast agents exhibit reduced rates of both renal and hepatocellular uptake and no apparent uptake by the RE system. The agents may be targeted to the blood pool or any other biological component. Since the agent is lost less rapidly from the bloodstream, lower doses can be used at a higher margin of safety. The approach is general to both large and small molecules.

    NEUE KASKADEN-POLYMER-KOMPLEXE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE MITTEL
    4.
    发明公开
    NEUE KASKADEN-POLYMER-KOMPLEXE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE MITTEL 审中-公开
    新CASCADE聚合物复合，方法用于生产和制药含

    公开(公告)号：EP2111236A2

    公开(公告)日：2009-10-28

    申请号：EP08701131.8

    申请日：2008-01-16

    申请人： Bayer Schering Pharma Aktiengesellschaft ,  EPIX Pharmaceuticals, Inc.

    发明人： SCHMITT-WILLICH, Heribert ,  SCHIRMER, Heiko ,  MISSELWITZ, Bernd ,  WEINMANN, Hanns-Joachim ,  CARAVAN, Peter

    IPC分类号： A61K49/12 ,  A61K47/48

    CPC分类号： A61K49/085 ,  A61K49/124

    摘要： The invention relates to novel cascade polymer complexes, to agents containing said compounds, to the use of said complexes in NMR diagnostics and to methods for producing said compounds and agents. The complex forming cascade polymer complexes according to the invention can be described by the following general formula (I): R - L - A -{ X - [ Y - ( Z - { W - Kw }z )y ]x }a-1, in which R represents an HSA binding unit, L represents a linker or a bond, A represents a cascade core of base multiplicity a containing nitrogen, X and Y independently of one another represent a direct bond or a cascade reproduction unit of reproduction multiplicity x or y, Z and W independently of one another represent a direct bond or a cascade reproduction unit of reproduction multiplicity z or w, K represents the group of a complex former, a represents the numbers 2 to 12, and x, y, z and w represent independently of one another the numbers 1 to 4, with the proviso that exactly one multiplicity of base multiplicity a of the cascade core A represents exactly one bond site to L and with the proviso that the cascade polymer complexes in the complex former groups K contain in total at least 4 ions of an element of the atomic number 20 to 29, 39, 42 to 44 or 57 to 83 and optionally comprise cations of inorganic and/or organic bases, amino acids or amino acid amides.