发明名称 AMINO ACID ANALOGS FOR TUMOR IMAGING
摘要 The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of 1-amino-cycloalkyl-1-carboxylic acids, namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes including fluorine-18, iodine-123, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77 and bromine-82. In one aspect, the invention features amino acid compounds that have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds show a target to non-target ratio of at least 5:1, are stable in vivo and substantially localized to target within 1 hour after administration. An especially preferred amino acid compound is ¢18F!-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC). In another aspect, the invention features pharmaceutical compositions comprised of an .alpha.-amino acid moiety attached to either a four-, five-, or a six-member carbon-chain ring. In addition, the invention features analogs of .alpha.aminoisobutyric acid.
申请公布号 CA2237218(A1) 申请公布日期 1997.05.15
申请号 CA19962237218 申请日期 1996.11.08
申请人 EMORY UNIVERSITY 发明人 SHOUP, TIMOTHY;GOODMAN, MARK M.
分类号 A61K51/00;A61K51/04;C07B59/00;C07C45/30;C07C45/59;C07C229/20;C07C229/30;C07C229/48;C07F13/00;C07F17/00;(IPC1-7):C07F13/00 主分类号 A61K51/00
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