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    • 4. 发明授权
    • Bifunctional chelating agents
    • 双功能螯合剂
    • US5395946A
    • 1995-03-07
    • US566343
    • 1990-08-07
    • Wilhelmus T. GoedemansKarel J. Panek
    • Wilhelmus T. GoedemansKarel J. Panek
    • A61K47/48A61K51/04A61K51/08A61K51/10C07D333/36C07D335/02
    • C07D335/02A61K47/48238A61K51/0478A61K51/081A61K51/088A61K51/1048A61K51/1093C07D333/36A61K2121/00A61K2123/00Y02P20/55
    • The invention related to a method of preparing a protein or a proteinaceous material labelled with a metalradionuclide and intended for diagnostic or therapeutic application, by reacting a protein or a proteinaceous material with an agent for coupling the radionuclide to the protein or the proteinaceous material, a protein conjugate being formed, and by then complexing the radionuclide with the conjugate thus formed to a radionuclide complex. A coupling agent is used which consists at least substantially ofa thio compound of the general formulaY--R--S--XwhereinX is a hydrogen atom or a suitable protective group,R is a branched or non-branched, optionally substituted hydrocarbon radical having 1-10 carbon atoms, which may be interrupted by one or more hereto atoms, andY is at least one terminal reactive group capable of reacting with a functional group from the protein or the proteinaceous material; ora cyclic condensation product of the thio compound of formula I having 5-7 ring atoms, wherein X and Y together constitute a reactive group capable of reacting with a functional group from the protein or the proteinaceous material;or a water-soluble salt of this condensation product.
    • PCT No.PCT / US89 / 00500 Sec。 371日期1990年10月24日第 102(e)1990年10月24日PCT PCT 1989年2月8日提交PCT本发明涉及一种制备用金属放射性核素标记并用于诊断或治疗应用的蛋白质或蛋白质材料的方法,通过使蛋白质或 蛋白质材料与用于将放射性核素偶联到蛋白质或蛋白质材料的试剂,蛋白质缀合物形成,然后使放射性核素与由此形成的缀合物络合成放射性核素复合物。 使用偶联剂,其至少基本上由通式YRSX的硫代化合物组成,其中X是氢原子或合适的保护基,R是具有1-10个碳原子的支链或非支链的任选取代的烃基 ,其可以被一个或多个原子间隔,Y是能够与蛋白质或蛋白质物质与官能团反应的至少一个末端反应性基团; 或具有5-7个环原子的式I的硫代化合物的环状缩合产物,其中X和Y一起构成能够与蛋白质或蛋白质物质与官能团反应的反应性基团; 或该缩合产物的水溶性盐。
    • 5. 发明授权
    • Radiolabelled particulate composition
    • 放射性标记颗粒组成
    • US5362473A
    • 1994-11-08
    • US678252
    • 1991-12-18
    • Karel J. Panek
    • Karel J. Panek
    • A61K51/00A61K51/12A61K49/02
    • A61K51/1251A61K2121/00A61K2123/00
    • The invention relates to a metal-radionuclide-labelled particulate composition which may be used in the form of a dry aerosol for lung scintigraphy, in particular, for the examination of the mucociliary transport, or for radiotherapy. The composition comprises radioactive labelled particles on a base of silica gel, another silicaceous material or a non-swelling polymer, at the surface of which organic ligands are bound covalently which comprise thiol-, amino-, alkylamino-, oxime-, dithiocarbamate-, xanthate-, thiosemicarbazone-, or dithiosemicarbazone groups or combinations thereof.The invention further relates to a method of preparing the composition and to a kit for carrying out the method.
    • PCT No.PCT / US89 / 04490 Sec。 371 1991年12月18日第 102(e)1991年12月18日的PCT日期1989年10月6日PCT。本发明涉及一种金属放射性核素标记的微粒组合物,其可以用于肺闪烁扫描的干燥气溶胶的形式,特别是用于 检查粘液纤毛运输或放射治疗。 该组合物包含在硅胶基底上的放射性标记的颗粒,另一种硅质材料或非溶胀性聚合物,其表面上共价键合有机配体,其包含硫醇,氨基,烷基氨基,肟,二硫代氨基甲酸盐, 黄原酸酯,缩氨基硫脲或二硫代缩氨基脲类或其组合。 本发明还涉及一种制备该组合物的方法和一种用于实施该方法的试剂盒。