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Generated: September 22, 2017

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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)
Application Number:08/554,906
Patent Claims: 1. An amino acid analog having the general structure ##STR20## where R.sub.1 is X, X--CH.dbd.CH--, or R.sub.3 R.sub.2 is H, or R.sub.3 if R.sub.1 is R.sub.3, ##STR21## such that ##STR22## is formed where 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 if n is 1 and j is 0,

n is 1 or 2, but 0 if m is 0,

m is 0 or 1,

j is 0 or 1, and

X is .sup.18 F, .sup.123 I, .sup.125 I, .sup.131 I, .sup.75 Br, .sup.76 Br, .sup.77 Br, or .sup.82 Br.

2. A compound of claim 1, wherein R.sub.1 and R.sub.2 =R.sub.3.

3. A cyclic compound according to claim 1 wherein

x is 0

y is 1

z is 2

q is 1

m is 0, and

j is 0.

4. A compound according to claim 3 wherein X is .sup.18 F, or .sup.123 I.

5. A compound according to claim 3 wherein X is .sup.18 F.

6. A compound according to claim 1 wherein R.sub.1 and R.sub.2 =R.sub.3,

x is 0 or 1

y is 2

z is 4

q is 1

m and j are each 0, and

X is .sup.18 F, or .sup.123 I.

7. A compound according to claim 6 wherein

x is 1

X is .sup.18 F.

8. The compound of claim 8 wherein x is 0 and X is .sup.123 I.

9. A compound according to claim 6 wherein x is 1 and X is .sup.123 I.

10. A compound according to claim 1

wherein R.sub.1 and R.sub.2 =R.sub.3

x is 0

y is 1

z is 2

q is 0

m is 1

n is 1

j is 0, and

X is .sup.18 F, or .sup.123 I.

11. A compound according to claim 10 wherein X is .sup.18 F.

12. A compound according to claim 1

wherein R.sub.1 and R.sub.2 =R.sub.3

x is 1

y is 1

z is 1

q is 0

m and j are 0, and

X is .sup.18 F, or .sup.123 I.

13. A compound according to claim 12 wherein X is .sup.123 I.

14. A compound according to claim 1

wherein R.sub.1 and R.sub.2 =R.sub.3

x is 0

y is 1

z is 2

q is 1

m is 1

n is 1

j is 1, and

X is .sup.18 F, or .sup.123 I.

15. The compound of claim 14 wherein X is .sup.123 I.

16. A compound according to claim 1

wherein R.sub.1 and R.sub.2 =R.sub.3

x is 0

y is 1

z is 2

q is 0

m is 0

j is 1, and

X is .sup.18 F, or .sup.123 I.

17. The compound of claim 16 wherein X is .sup.123 I.

18. A compound according to claim 1

wherein R.sub.1 and R.sub.2 =R.sub.3

x is 0 or 1

y is 2

z is 4

q is 1

m is 1

n is 1

j is 1, and

X is .sup.18 F, or .sup.123 I.

19. The compound of claim 18 wherein X is .sup.18 F.

20. The compound of claim 18 wherein X is .sup.123 I.

21. A compound according to claim 1

wherein R.sub.1 and R.sub.2 =R.sub.3

x is 0 or 1

y is 2

z is 4

q is 0

m is 0

j is 1, and

X is .sup.18 F, or .sup.123 I.

22. The compound of claim 21 wherein X is .sup.18 F.

23. The compound of claim 21 wherein X is .sup.123 I.

24. A compound of claim 1 wherein R.sub.1 and R.sub.2 .noteq.R.sub.3.

25. A compound according to claim 24 wherein X is .sup.18 F.

26. A compound according to claim 1 wherein R.sub.1 is X--CH.dbd.CH--, R.sub.2 is H, y is 1 and z is 2.

27. A compound of claim 26 wherein X is .sup.123 I.
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Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

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