申请人:Liu Shuang
公开号:US20050010038A1
公开(公告)日:2005-01-13
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.
螯合剂及其大环金属配合物,制备螯合剂和大环金属配合物的方法,以及包括大环金属配合物的放射性药物组合物被揭示。还揭示了将大环金属配合物用作用于诊断心血管疾病、传染病和癌症的放射性药物的方法。揭示了作为靶向特定生物分子(如蛋白质、肽、肽类似物、非肽受体配体、酶抑制剂和酶底物)的放射标记的双功能螯合剂(BFCs)的螯合剂。揭示了使用含有螯合剂-生物分子共轭物的大环金属配合物作为靶向特定诊断放射性药物的方法,这些药物选择性地定位于疾病部位,并允许使用伽马闪烁术获得部位的图像。进一步揭示了将放射性药物用作心血管疾病(如血栓栓塞病或动脉粥样硬化)、传染病和癌症的诊断成像剂的方法。