Imaging agents for diagnosis of Parkinson's disease

• US 7,317,103 B2
• Filed: 01/13/2004
• Issued: 01/08/2008
• Est. Priority Date: 02/22/2000
• Status: Expired due to Fees

• Current Assignee: Molecular Insight Pharmaceuticals Incorporated (Lantheus Holdings, Inc.)
• Original Assignee: Molecular Insight Pharmaceuticals Incorporated (Lantheus Holdings, Inc.)
• Inventors: Smith, Miles P., Babich, John W.
• Primary Examiner(s): CHANG, CELIA C
• Application Number:
  US10/756,793
• Publication Number:
  US 20050026955A1
• Time in Patent Office: 1,456 Days
• Field of Search: 546/11, 546/223, 546/229, 546/232, 534/10, 534/751
• US Class Current: 546/299
• CPC Class Codes: A61K 51/0478 complexes from non-cyclic ligands, e.g. EDTA, MAG3
• CPC Class Codes: A61K 51/0497 conjugates with a carrier being an organic compounds

Abstract

Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson'"'"'s disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.

Claims

1. A complex comprising technetium-99m and a compound represented by A:

2. The complex of claim 1, wherein X is (H)₂.

3. The complex of claim 1, wherein R is alkyl.

4. The complex of claim 1, wherein R₃ is substituted phenyl.

5. The complex of claim 1, wherein each R₅ is H.

6. The complex of claim 1, wherein n is 1.

7. The complex of claim 1, wherein the compound is represented by the following structure:

10. A method of imaging dopamine transporters in brain tissue of a mammal, comprising the step of administering to a mammal a sufficient amount of a complex of claim 1 or 8 and scanning the brain tissue to detect the binding of the complex to the dopamine transporter in the mammal.

8. A complex comprising rhenium and a compound of represented by A:

9. The complex of claim 8, wherein the compound is represented by the following structure: