Radiolabelled angiotensin converting enzyme inhibitors

• US 5,601,801 A
• Filed: 08/02/1994
• Issued: 02/11/1997
• Est. Priority Date: 08/02/1994
• Status: Expired due to Term

• Current Assignee: Jubilant DraxImage Inc. (Jubilant Pharmova Limited)
• Original Assignee: Merck Frosst Canada & Company (Merck & Co., Inc.)
• Inventors: Zabel, Pamela, Quiquero, Vincenzo, Hunter, Duncan H., Flanagan, Richard J.
• Primary Examiner(s): Hollinden, Gary E.
• Assistant Examiner(s): Hartley, Michael G.
• Application Number:
  US08/284,767
• Time in Patent Office: 924 Days
• Field of Search: 424/1.85, 514/312, 514/300, 514/340, 514/252, 514/218, 514/384, 514/383, 260/112.5, 544/60, 548/250
• US Class Current: 424/1.85
• CPC Class Codes: A61K 51/08 Peptides, e.g. proteins , carriers being peptides, polyamino acids, proteins
• CPC Class Codes: C07D 207/16 Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

Angiotensin convening enzyme (ACE) inhibitors can be labelled with Iodine-123, Iodine-125, Iodine-127 or Iodine-131, useful to image the kidneys and lungs for diagnosis and treatment of diseases such as essential hypertension, renal artery stenosis, or diabetes which are associated with a change in the amount of ACE present in the human body.

Claims

1. A compound which is N.sup.α

-((S)-1-carboxy-3-phenylpropyl-N.sup.ε

-3-iodo-benzoyl-L-lysyl-L-proline, wherein iodo is selected from ¹²⁷ I, ¹²³ I, ¹²⁵ I, and ¹³¹ I.

2. A compound having the structure:

##STR6## wherein X is selected from ¹²⁷ I, ¹²³ I, ¹²⁵ I, and ¹³¹ I, and is located at the 2-, 3- or 4-position.

3. The compound of claim 2 wherein X is ¹³¹ I, and is located at the 3-position.