11-Nonyloxy-Undec-8(Z)-Eonic Acid Derivatives as Therapy for Renal and Cardiovascular Diseases


Title: Epoxy Lipid Mimics as Lead Compounds for Endothelial Dysfunction


Current State of the Art: 

Endothelial cell dysfunction is an underlying cause of vascular disease and is also found in patients with coronary artery disease, diabetes, high cholesterol and high blood pressure (hypertension). Available treatments include nonsteroidal anti-inflammatory drugs (NSAIDS), angiotensin receptor blockers (ARB) and ACE (angiotensin converting enzyme) inhibitors. The NSAIDS target enzymes that metabolize arachidonic acid. These metabolites regulate angiotensin II function and subsequently endothelial cell behavior, producing anti-inflammatory and anti-hypertensive effects.


Disadvantages of the Current Art:

Available compounds such as the NSAIDS, most notably COX2 inhibitors, have broader effects that in some patients can result in organ damage, impaired liver function, progressive renal failure and even death. ACE inhibitors have fewer side effects but are contraindicated for some patients including those with Diabetes; with narrowing of a major artery in the kidney, as it can result in organ damage or with patients taking a combination of ACE inhibitors with aliskaren since patients can suffer from hypotension, renal failure and hypokalemia.


Advantage of the Invention:

Novel compounds are available that mimic epoxy lipids (EETs) which are metabolites of arachidonic acid. EETs in small animal studies reduced hypertension by regulating endothelial cell behavior and demonstrated a protective effect on the kidneys, reducing organ damage. In addition, EETs also exhibit other beneficial activities including anti-inflammatory and anti-platelet aggregation activity.


These compounds provide an alternative drug discovery opportunity for the treatment of renal and cardiovascular disease or other disorders where regulating endothelial cell function would be beneficial.


Patent Status: Patent Issued 7,550,617; 7,732,470


Inventors: John Imig, Ph.D; John Falck, Ph.D;


Case Number: GHSU 2006-017

Patent Information:
For Information, Contact:
Augusta University
John Imig
John Falck
Renal Disease
Vascular Disease
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