IP Library Granted Patent US 8,722,014
Granted Patent B2
US 8,722,014 · App. 12/772,760 · Granted May 13, 2014

1

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Quick Facts
Patent No.
US 8,722,014
App. No.
12/772,760
Granted
May 13, 2014
Kind
B2
Abstract

Tracers for cationic amino acid transport systems and methods of synthesis are disclosed, including compounds comprising a 1H-[1,2,3]triazole moiety. Further disclosed are uses of the analogues, including in vivo imaging of tumors by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Claims (18)

1. A 1H-[1,2,3]triazole substituted amino acid of structure

wherein R 1 is CH 2 or O, n is an integer from 0 to 3, m is an integer from 0 to 1, and p is an integer from 0 to 1 wherein F is 18 F.

2. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 1 , wherein R 1 is CH 2 , n is from 1 to 3, m is 0, p is 1, and F is an 18 F.

3. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 1 , wherein R 1 is CH 2 , n is l, m is 0, p is 1, and F is an 18 F.

4. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 1 , wherein R 1 is CH 2 , n is 2, m is 0, p is 1, and F is an 18 F.

5. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 1 , wherein R 1 is CH 2 , n is 3, m is 0, p is 1, and F is an 18 F.

6. A 1H-[1,2,3]triazole substituted amino acid or salt thereof in accordance with claim 1 , wherein the acid is selected from the group consisting of

7. A 1H-[1,2,3]triazole substituted amino acid of structure

wherein R 2 is CH 2 or O, z is an integer from 0 to 3, y is an integer from 0 to 1, and x is an integer from 0 to 2 wherein F is 18 F.

8. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 7 , wherein R 2 is O, z is 1 to 3, y is 1, x is 2, and the F is an 18 F.

9. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 7 , wherein R 2 is O, z is 1, y is 1, x is 2, and the F is an 18 F.

10. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 7 , wherein R 2 is O, z is 2, y is 1, x is 2, and the F is an 18 F.

11. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 7 , wherein R 2 is O, z is 3, y is 1, x is 2, and the F is an 18 F.

12. A 1H-[1,2,3]triazole substituted amino acid in accordance with claim 7 , wherein the acid is selected from the group consisting of

13. A method of imaging a tumor in a mammal, the method comprising:

administering to the mammal a 1H-[1,2,3]triazole substituted amino acid of claim 1 ; and subjecting the mammal to PET scanning.

14. A method of imaging a tumor in a mammal in accordance with claim 13 , wherein the 1H-[1,2,3]triazole substituted amino acid is selected from the group consisting of

15. A method of imaging a tumor in a mammal in accordance with claim 13 , wherein the 1H-[1,2,3]triazole substituted amino acid is selected from the group consisting of

Assignments (4)
CONFIRMATORY LICENSE Recorded Dec 19, 2018
From: WASHINGTON UNIVERSITY IN ST. LOUIS
To: NATIONAL INSTITUTES OF HEALTH - DIRECTOR DEITR
Reel/Frame 047812/0478 →
CONFIRMATORY LICENSE Recorded Dec 18, 2018
From: WASHINGTON UNIVERSITY IN ST. LOUIS
To: NATIONAL INSTITUTES OF HEALTH - DIRECTOR DEITR
Reel/Frame 047949/0077 →
CONFIRMATORY LICENSE Recorded Mar 31, 2017
From: WASHINGTON UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 042125/0372 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 5, 2015
From: MACH, ROBERT; MCCONATHY, JONATHAN
To: WASHINGTON UNIVERSITY
Reel/Frame 035092/0279 →