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    • 4. 发明申请
    • ION BINDING COMPOUNDS, RADIONUCLIDE COMPLEXES, METHODS OF MAKING RADIONUCLIDE COMPLEXES, METHODS OF EXTRACTING RADIONUCLIDES AND METHODS OF DELIVERING RADIONUCLIDES TO TARGET LOCATIONS
    • 离子结合化合物,放射性核素复合物,制备放射性核素复合物的方法,提取放射性核素的方法和将放射性核素递送到目标位置的方法
    • WO99024396A1
    • 1999-05-20
    • PCT/US1998/024074
    • 1998-11-12
    • A61K47/48A61K51/12C07C259/06C07C311/29C22B3/26C22B3/32C22B59/00C22B60/00G21F9/12A61K51/04C07C59/74
    • B82Y5/00A61K47/6887A61K51/1268C07C259/06C07C311/29C07C2603/92C22B3/0006C22B3/0024C22B59/00C22B60/00G21F9/12Y02P10/234
    • The invention pertains to compounds for binding lanthanide ions and actinide ions. The invention further pertains to compounds for binding radionuclides, and to methods of making radionuclide complexes. Also, the invention pertains to methods of extracting radionuclides. Additionally, the invention pertains to methods of delivering radionuclides to target locations. In one aspect, the invention includes a compound comprising: a) a calix[n]arene group, wherein n is an integer greater than 3, the calix[n]arene group comprising an upper rim and a lower rim; b) at least one ionizable group attached to the lower rim; and c) an ion selected from the group consisting of lanthanide and actinide elements bound to the ionizable group. In another aspect, the invention includes a method of extracting a radionuclide, comprising: a) providing a sample comprising a radionuclide; b) providing a calix[n]arene compound in contact with the sample, wherein n is an integer greater than 3; and c) extracting radionuclide from the sample into the calix[n]arene compound. In yet another aspect, the invention includes a method of delivering a radionuclide to a target location, comprising: a) providing a calix[n]arene compound, wherein n is an integer greater than 3, the calix[n]arene compound comprising at least one ionizable group; b) providing a radionuclide bound to the calix[n]arene compound; and c) providing an antibody attached to the calix[n]arene compound, the antibody being specific for a material found at the target location.
    • 本发明涉及用于结合镧系离子和锕系离子的化合物。 本发明还涉及用于结合放射性核素的化合物以及制备放射性核素复合物的方法。 此外,本发明涉及提取放射性核素的方法。 此外,本发明涉及将放射性核素递送到目标位置的方法。 一方面,本发明包括一种化合物,其包含:a)杯[n]芳烃基,其中n是大于3的整数,所述杯[n]芳烃基包括上边缘和下边缘; b)连接到下边缘的至少一个可离子化基团; 和c)选自与可离子化基团结合的镧系元素和锕系元素的离子。 另一方面,本发明包括一种提取放射性核素的方法,包括:a)提供包含放射性核素的样品; b)提供与样品接触的杯[n]芳烃化合物,其中n是大于3的整数; 和c)将样品中的放射性核素提取到杯[n]芳烃化合物中。 在另一方面,本发明包括将放射性核素递送到目标位置的方法,包括:a)提供其中n为大于3的整数的杯[n]芳烃化合物,所述杯[n]芳烃化合物包含 至少一个可离子化基团; b)提供与杯[n]芳烃化合物结合的放射性核素; 和c)提供连接到杯[n]芳烃化合物的抗体,所述抗体对于在目标位置处发现的材料是特异性的。
    • 6. 发明申请
    • A RADIONUCLIDE-BINDING COMPOUND AND ITS DELIVERY SYSTEM
    • 一种放射性核素结合体及其输送系统
    • WO9924081A3
    • 1999-07-29
    • PCT/US9824169
    • 1998-11-12
    • BATTELLE MEMORIAL INSTITUTEIDAHO RES FOUND
    • FISHER DARRELL RWAI CHIEN MCHEN XIAOYUAN
    • A61K51/10A61K51/12
    • B82Y5/00A61K51/1093A61K51/1268
    • The invention pertains to compounds which specifically bind radionuclides, and to methods of making radionuclide complexing compounds. In one aspect, the invention includes a radionuclide delivery system comprising: a) a calix[n]arene-crown-[m]-ether compound, wherein n is an integer greater than 3, and wherein m is an integer greater than 3, the calix[n]arene-crown-[m]-ether compound comprising at least two ionizable groups; and b) an antibody attached to the calix[n]arene-crown-[m]-ether compound. In another aspect, the invention includes a method of making a radium complexing compound, comprising: a) providing a calix[n]arene compound, wherein n is an integer greater than 3, the calix[n]arene compound comprising n phenolic hydroxyl groups; b) providing a crown ether precursor, the crown ether precursor comprising a pair of tosylated ends; c) reacting the pair of tosylated ends with a pair of the phenolic hydroxyl groups to convert said pair of phenolic hydroxyl groups to ether linkages, the ether linkages connecting the crown ether precursor to the calix[n]arene to form a calix[n]arene-crown-[m]-ether compound, wherein m is an integer greater than 3; d) converting remaining phenolic hydroxyl groups to esters; e) converting the esters to acids, the acids being proximate a crown-[m]-ether portion of the calix[n]arene-crown-[m]-ether compound; and f) providing a Ra ion within the crown-[m]-ether portion of the calix[n]arene-crown-[m]-ether compound.
    • 本发明涉及特异性结合放射性核素的化合物,以及制备放射性核素络合化合物的方法。 一方面,本发明包括放射性核素递送系统,其包括:a)杯[n]芳烃 - 冠 - [m] - 醚化合物,其中n是大于3的整数,并且其中m是大于3的整数, 包含至少两个可离子化基团的杯[n]芳烃 - 冠 - [m] - 醚化合物; 和b)连接到杯[n]芳烃 - 冠 - [m] - 醚化合物的抗体。 另一方面,本发明包括制备镭络合化合物的方法,包括:a)提供其中n为大于3的整数的杯[n]芳烃化合物,包含n个酚羟基的杯[n]芳烃化合物 ; b)提供冠醚前体,所述冠醚前体包含一对甲磺酰化的末端; c)使一对甲苯磺酰化的末端与一对酚羟基反应,将所述一对酚羟基转化为醚键,将冠醚前体连接到杯[n]芳烃上形成杯[n] 芳基 - 冠 - [m] - 醚化合物,其中m是大于3的整数; d)将剩余的酚羟基转化成酯; e)将酯转化为酸,酸接近杯[n]芳烃 - 冠 - [m] - 醚化合物的冠 - [m] - 醚部分; 和f)在杯[n]芳烃 - 冠 - [m] - 醚化合物的冠 - [m] - 醚部分内提供Ra 2+离子。