CONTRAST AGENTS FOR MYOCARDIAL PERFUSION IMAGING

• US 20080112884A1
• Filed: 01/15/2008
• Published: 05/15/2008
• Est. Priority Date: 02/13/2004
• Status: Active Grant

• Current Assignee: Lantheus Medical Imaging, Inc. (Lantheus Holdings, Inc.)
• Original Assignee: Bristol-Myers Squibb Pharma Company (Bristol-Myers Squibb Company)
• Inventors: CASEBIER, DAVID, Dischino, Douglas, Robinson, Simon, Azure, Michael, Radeke, Heike, Purohit, Ajay
• Granted Patent: US 8,226,929 B2
• Time in Patent Office: Days
• US Class Current: 424/1.11
• CPC Class Codes: A61K 49/00 Preparations for testing in vivo
• CPC Class Codes: A61K 49/0002 General or multifunctional contrast agents, e.g. chelated agents
• CPC Class Codes: A61K 49/0052 Small organic molecules oligomers, polymers, dendrimers A61K49/0054
• CPC Class Codes: A61K 49/10 Organic compounds
• CPC Class Codes: A61K 49/22 Echographic preparations; Ultrasound imaging preparations ; Optoacoustic imaging preparations
• CPC Class Codes: A61K 51/04 Organic compounds
• CPC Class Codes: A61K 51/0421 having six-membered rings with one oxygen as the only ring hetero atom
• CPC Class Codes: A61K 51/0453 having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
• 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: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07B 59/002 Heterocyclic compounds
• CPC Class Codes: C07D 237/16 Two oxygen atoms
• CPC Class Codes: C07D 239/88 Oxygen atoms

Abstract

The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

Claims

1. A contrast agent comprising an imaging moiety and a compound selected from pyridimifen, fenazaquin, a pyridimifen analog, and a fenazaquin analog.

2. The contrast agent of claim 1 wherein the imaging moiety is a radioisotope for nuclear medicine imaging, a paramagnetic species for use in MRI imaging, an echogenic entity for use in ultrasound imaging, a fluorescent entity for use in fluorescence imaging, or a light-active entity for use in optical imaging.

3. The contrast agent of claim 2 wherein the paramagnetic species for use in MRI imaging is Gd³⁺, Fe³⁺, In³⁺, or Mn²⁺.

4. The contrast agent of claim 2 wherein the echogenic entity for use in ultrasound imaging is a fluorocarbon encapsulated surfactant microsphere.

5. The contrast agent of claim 2 wherein the radioisotope for nuclear medicine imaging is ¹¹C, ¹³N, ¹⁸F, ¹²³I, ¹²⁵I, ^99mTc, ⁹⁵Tc, ¹¹¹In, ⁶²Cu, ⁶⁴Cu, ⁶⁷Ga, or ⁶⁸Ga.

6. The contrast agent of claim 1 wherein the imaging moiety is ¹⁸F.

7. The contrast agent of claim 1 wherein the imaging moiety is ^99mTc.

8. The contrast agent of claim 1 of formula (II),

9. The contrast agent of claim 8, wherein R²⁹ is C₁-C₆ alkyl wherein the C₁-C₆ alkyl is tert-butyl.

10. The contrast agent of claim 8, wherein R²⁸ is C₁-C₆ alkyl wherein the C₁-C₆ alkyl is methyl.

11. The contrast agent of claim 1 of formula (V)

12. The contrast agent of claim 11 wherein J is O.

13. The contrast agent of claim 11 of formula (VI)

14. The contrast agent of claim 1 wherein the contrast agent is selected from