发明名称 A RADIONUCLIDE-BINDING COMPOUND AND ITS DELIVERY SYSTEM
摘要 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<2+> ion within the crown-[m]-ether portion of the calix[n]arene-crown-[m]-ether compound.
申请公布号 WO9924081(A2) 申请公布日期 1999.05.20
申请号 WO1998US24169 申请日期 1998.11.12
申请人 BATTELLE MEMORIAL INSTITUTE;IDAHO RESEARCH FOUNDATION, INC. 发明人 FISHER, DARRELL, R.;WAI, CHIEN, M.;CHEN, XIAOYUAN
分类号 A61K51/10;A61K51/12 主分类号 A61K51/10
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