Chelants and macrocyclic metal complex radiopharmaceuticals thereof

    公开(公告)号:US07317104B2

    公开(公告)日:2008-01-08

    申请号:US10864857

    申请日:2004-06-09

    申请人: Shuang Liu

    发明人: Shuang Liu

    IPC分类号: C07D211/72

    CPC分类号: C07F13/005 C07F9/58

    摘要: Chelants and macrocyclic metal complexes thereof, methods of preparing the chelants and macrocyclic metal complexes, and radiopharmaceutical compositions comprising the macrocyclic metal complexes are disclosed. Methods of using the macrocyclic metal complexes as radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious diseases and cancer are also disclosed. Chelants as bifunctional chelators (BFCs) for the radiolabeling of target-specific biomolecules, such as proteins, peptides, peptidomimetics, non-peptide receptor ligands, enzyme inhibitors, and enzyme substrates are disclosed. Methods of using macrocyclic metal complexes containing the chelant-biomolecule conjugates as target-specific diagnostic radiopharmaceuticals that selectively localize at sites of disease and allow an image to be obtained of the loci using gamma scintigraphy are disclosed. Methods of use of the radiopharmaceuticals as imaging agents for the diagnosis of cardiovascular disorders, such as thromboembolic disease or atherosclerosis, infectious disease and cancer are further disclosed.

    Macrocyclic chelants for metallopharmaceuticals
    69.
    发明申请
    Macrocyclic chelants for metallopharmaceuticals 审中-公开
    金属药物的大环螯合剂

    公开(公告)号:US20050201933A1

    公开(公告)日:2005-09-15

    申请号:US11124537

    申请日:2005-05-06

    申请人: Shuang Liu

    发明人: Shuang Liu

    摘要: This invention relates to macrocyclic chelants comprised of one or two heteroatom-containing bridges, compositions containing them and their use in medicine, particularly in diagnostic imaging and radiotherapy. This invention relates especially to the use of metal chelates of the macrocyclic chelants as metallopharmaceuticals in Magnetic Resonance Imaging (MRI) and radiopharmaceuticals. This invention also relates to macrocyclic chelants as bifunctional chelating agents (BFC's) for the labeling of biologically active targeting molecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands, with metal ions and radioisotopes.

    摘要翻译: 本发明涉及由一个或两个含杂原子的桥组成的大环螯合剂,含有它们的组合物及其在医药中的用途,特别是在诊断成像和放射治疗中。 本发明特别涉及大环螯合物的金属螯合物作为磁共振成像(MRI)和放射性药物中的金属药物。 本发明还涉及用金属离子和放射性同位素标记生物活性靶向分子如蛋白质,肽,肽模拟物和非肽受体配体的双功能螯合剂(BFC's)的大环螯合剂。

    Macrocyclic chelants for metallopharmaceuticals

    公开(公告)号:US06916460B2

    公开(公告)日:2005-07-12

    申请号:US10663090

    申请日:2003-09-15

    申请人: Shuang Liu

    发明人: Shuang Liu

    摘要: This invention relates to macrocyclic chelants comprised of one or two heteroatom-containing bridges, compositions containing them and their use in medicine, particularly in diagnostic imaging and radiotherapy. This invention relates especially to the use of metal chelates of the macrocyclic chelants as metallopharmaceuticals in Magnetic Resonance Imaging (MRI) and radiopharmaceuticals. This invention also relates to macrocyclic chelants as bifunctional chelating agents (BFC's) for the labeling of biologically active targeting molecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands, with metal ions and radioisotopes.