Details for Patent: 5,817,776

Title:	Amino acid analogs for tumor imaging
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 especially preferred amino acid compound is [.sup.18 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.
Inventor(s):	Goodman; Mark M. (Atlanta, GA), Shoup; Timothy (Decatur, GA)
Assignee:	Emory University (Atlanta, GA)
Filing Date:	Nov 08, 1996
Application Number:	08/744,444
Claims:	1. An amino acid analog having the general structure where R is ##STR24## where a is 1, 2 or 3 b is 0, 1 or 2 x is 0 or 1 y is 1 or 2 z is 1,2,3 or 4 and z>y if y is 2, q is 1 or 0 Z is ##STR25## 2. A compound according to claim 1 wherein Z is ##STR26## 3. A compound according to claim 2 wherein a is 1, 2 or 3 and b is 0. 4. A compound according to claim 2 wherein a is 1, 2 or 3 and b is 1. 5. A compound according to claim 2 wherein a is 1, 2 or 3 and b is 2. 6. A compound according to claim 2 wherein Z is ##STR27## 7. A compound according to claim 6 wherein a is 1, 2, or 3 and b is 0. 8. A compound according to claim 6 wherein a is 1, 2 or 3 and b is 1. 9. A compound according to claim 6 wherein a is 1, 2 or 3 and b is 2. 10. A compound according to claim 2 wherein Z is ##STR28## 11. A compound according to claim 10 wherein a is 1, 2, or 3 and b is 0. 12. A compound according to claim 10 wherein a is 1, 2, or 3 and b is 1. 13. A compound according to claim 10 wherein a is 1, 2, or 3 and b is 2. 14. A method of in situ tumor imaging by single photon emission tomography comprising: administering to a subject suspected of having a tumor an image-generating amount of a compound according to claim 1, and measuring the distribution of the compound in the subject by single photon emission tomography.