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8 条记录 (耗时 0.031 秒)

    Indole derivatives
    4.
    发明授权
    Indole derivatives 有权
    吲哚衍生物

    公开(公告)号：US08790619B2

    公开(公告)日：2014-07-29

    申请号：US13258465

    申请日：2010-03-26

    申请人： Harry John Wadsworth ,  Bo Shan ,  Dennis O'Shea ,  Joanna Marie Passmore ,  William John Trigg ,  Amanda Ewan

    发明人： Harry John Wadsworth ,  Bo Shan ,  Dennis O'Shea ,  Joanna Marie Passmore ,  William John Trigg ,  Amanda Ewan

    IPC分类号： A61K51/00 ,  A61K36/14

    CPC分类号： C07D209/94 ,  A61K51/0446 ,  A61K51/0455 ,  A61K51/0468 ,  C07B59/002 ,  C07B2200/05 ,  C07D209/88 ,  C07D295/192 ,  C07D401/06 ,  C07D495/04

    摘要： An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

    摘要翻译： 通过本发明提供的以吲哚为基础的体内显像剂以高亲和力结合PBR，在给药后具有良好的摄入脑中，并具有良好的选择性结合PBR。 本发明还包括可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。 还提供了用于体内成像剂的自动合成的盒。 本发明的其它方面包括包含本发明的体内显像剂的放射性药物组合物和使用所述体内显像剂的方法。

    Imaging neuroinflammation
    6.
    发明授权
    Imaging neuroinflammation 有权
    成像神经炎症

    公开(公告)号：US09481685B2

    公开(公告)日：2016-11-01

    申请号：US13119450

    申请日：2009-10-02

    申请人： Harry John Wadsworth ,  Bo Shan ,  Dennis O'Shea ,  Joanna Marie Passmore ,  William John Trigg

    发明人： Harry John Wadsworth ,  Bo Shan ,  Dennis O'Shea ,  Joanna Marie Passmore ,  William John Trigg

    IPC分类号： A61K51/00 ,  A61M36/14 ,  C07D495/04 ,  A61K51/04

    CPC分类号： C07D495/04 ,  A61K51/0446

    摘要： The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.

    摘要翻译： 本发明涉及体内成像，特别是周边苯二氮卓受体（PBR）的体内成像。 提供四环吲哚体内显像剂，其以高亲和力与PBR结合，在给药后具有良好的摄入脑中，并优先结合表达较高水平的PBR的组织。 本发明还提供了可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒 。 还提供了用于体内成像剂的自动合成的盒。 此外，本发明提供了包含本发明的体内显像剂的放射性药物组合物，以及使用所述体内显像剂的方法。

    Aryloxyanilide imaging agents
    8.
    发明授权
    Aryloxyanilide imaging agents 失效
    芳氧基苯胺显像剂

    公开(公告)号：US08771641B2

    公开(公告)日：2014-07-08

    申请号：US13510041

    申请日：2010-12-16

    申请人： Harry John Wadsworth ,  Dennis O'Shea

    发明人： Harry John Wadsworth ,  Dennis O'Shea

    IPC分类号： A61K51/04 ,  A61K31/44

    CPC分类号： A61K51/0423 ,  A61K51/0419 ,  A61K51/0425 ,  B01L3/52 ,  C07D307/79 ,  C07D307/81 ,  C07D317/46 ,  C07D317/58 ,  C07D319/18 ,  C07D321/10

    摘要： The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.

    摘要翻译： 本发明提供适用于体内成像的新型放射性标记的芳氧基亚胺衍生物。 与已知的芳氧基亚胺衍生物体内显像剂相比，本发明的体内显像剂具有更好的体内成像性能。 本发明的体内显像剂与外用苯并二氮杂受体（PBR）具有良好的选择性结合，结合良好的脑摄取和给予受试者后的体内动力学。