Organic compounds -- part of the class 532-570 series – Organic compounds – Radioactive metal containing
Patent
1996-11-08
1998-10-06
Hollinden, Gary E.
Organic compounds -- part of the class 532-570 series
Organic compounds
Radioactive metal containing
534 10, 562504, 562505, 562507, 424 111, 424 165, C07F 1300
Patent
active
058177760
ABSTRACT:
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 F!-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.
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Goodman Mark M.
Shoup Timothy
Emory University
Hollinden Gary E.
Jones Dameron
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