TSPO-TARGETING COMPOUNDS AND USES THEREOF

• US 20110212025A1
• Filed: 02/24/2011
• Published: 09/01/2011
• Est. Priority Date: 02/24/2010
• Status: Active Grant

• Current Assignee: Johns Hopkins University
• Original Assignee: Johns Hopkins University
• Inventors: Guilarte, Tomas R., Wang, Haofan, Pomper, Martin G.
• Granted Patent: US 8,778,304 B2
• Time in Patent Office: Days
• US Class Current: 424/1.81
• CPC Class Codes: A61K 51/0459 having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• CPC Class Codes: C07B 59/002 Heterocyclic compounds
• CPC Class Codes: C07D 487/04 Ortho-condensed systems
• CPC Class Codes: G01N 2333/705 Assays involving receptors, cell surface antigens or cell surface determinants
• CPC Class Codes: G01N 2800/7095 Inflammation
• CPC Class Codes: G01N 33/60 involving radioactive labelled substances

Abstract

Translocator protein (TSPO) targeting compounds are described. Methods of making the compounds, and uses of the compounds for imaging are also described.

Claims

1. The compound having the structure

2. A compound according to claim 1 having the structure

3. A compound according to claim 2, where the compound is isotopically enriched in one of ¹²³I, ¹²⁴I, ¹²⁵I, or ¹³¹I.

4. A method of synthesizing the compound of claim 2, comprising reacting

5. The method of claim 4, further comprising reacting

6. A method for imaging cells, a sample, an organ or a subject comprising imaging cells, a sample, an organ or a subject with increased levels of translocator protein, TSPO, after administration of a detectably sufficient amount of a radioisotopically-enriched compound according to claim 2.

7. The method of claim 6, further comprising administering a detectably sufficient amount of a radioisotopically-enriched compound according to claim 2 before said imaging.

8. The method according to claim 6 wherein said imaging is autoradiography.

9. The method according to claim 6 wherein said imaging is single photon emission computed tomography and the compound is radioisotopically-enriched with ¹²³I or ¹²⁵I.

10. The method according to claim 6 wherein said imaging is positron emission tomography and the compound is radioisotopically-enriched with ¹²⁴I.

11. A method according to claim 6 wherein cells are glial cells or immune cells.

12. A method according to claim 6, wherein the organ is the brain.

13. A method according to claim 6, wherein the organ is the lungs.

14. A method according to claim 6, wherein the organ is the heart.

15. A method according to claim 6, wherein the subject has inflammation.

16. A method according to claim 6, wherein the subject has an autoimmune disease.

17. A method according to claim 6, wherein the subject has inflammatory arthritides.

18. A method according to claim 6, wherein the subject has a neurodegenerative disease.

19. A method according to claim 6, wherein the subject has atherosclerosis.