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    • 58. 发明申请
    • Chelants and macrocyclic metal complex radiopharmaceuticals thereof
    • 螯合剂及其大环金属络合物放射性药物
    • US20050010038A1
    • 2005-01-13
    • US10864792
    • 2004-06-09
    • Shuang Liu
    • Shuang Liu
    • A61K51/04A61K51/08C07D213/81C07D213/82C07F9/58C07F13/00C07F5/00
    • C07F13/005A61K51/0478A61K51/0482C07D213/81C07D213/82C07F9/58
    • 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.
    • 公开了螯合剂及其大环金属络合物,制备螯合剂和大环金属配合物的方法,以及包含大环金属络合物的放射性药物组合物。 还公开了将大环金属络合物用作放射性药物用于诊断心血管疾病,感染性疾病和癌症的方法。 公开了用于靶标特异性生物分子例如蛋白质,肽,肽模拟物,非肽受体配体,酶抑制剂和酶底物的放射性标记的双功能螯合剂(BFC)的螯合剂。 公开了使用含有螯合剂 - 生物分子共轭物的大环金属络合物作为靶向特异性诊断放射性药物的方法,其在疾病部位选择性定位并允许使用γ闪烁扫描获得基因座的图像。 进一步公开了使用放射性药物作为诊断心血管疾病如血栓栓塞性疾病或动脉粥样硬化,感染性疾病和癌症的显像剂的方法。
    • 60. 发明授权
    • Ternary ligand complexes useful as radiopharmaceuticals
    • 用作放射性药物的三元配体配合物
    • US06403054B1
    • 2002-06-11
    • US08864586
    • 1997-05-28
    • Shuang Liu
    • Shuang Liu
    • A61K5104
    • C07F13/005A61K51/0478C07D213/77C07D213/82C07F9/5045
    • The present invention provides novel radiopharmaceuticals useful for imaging the heart, brain, lungs, liver or kidneys, kits useful for preparing the radiopharmaceuticals, and methods of imaging the heart, brain, lungs, liver or kidneys in a patient in need of such imaging. The radiopharmaceuticals are comprised of technetium or rhenium radionuclide complexes of a ternary ligand system: one hydrazido or diazenido ligand, one aminoalcohol ligand, and one pi-acid ligand selected from phosphines, arsines, and imine nitrogen-containing heterocycles. The radiopharmaceuticals have the formula, ML1L2L3, wherein the variables are as defined herein.
    • 本发明提供了可用于对心脏,脑,肺,肝或肾进行成像的新型放射性药物,可用于制备放射性药物的试剂盒,以及在需要这种成像的患者中对心脏,脑,肺,肝或肾进行成像的方法。 放射性药物由三元配体体系的锝或铼放射性核素配合物组成:一个肼基或二氮烯酸配体,一个氨基醇配体和一个选自膦,胂和亚胺含氮杂环的一个配位体。 放射性药物具有式ML1L2L3,其中变量如本文所定义。