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A class of small-molecule therapeutics for hypertension and inflammatory diseases

Summary

Epoxyeicosatrienoic acids (EETs) are lipid metabolites that regulate blood pressure and inflammation. EETs are metabolized by soluble epoxide hydrolase (sEH); therefore, inhibition of sEH may treat hypertension and other medical conditions caused by irregularities in blood pressure, vasodilation, endothelial cell function, and inflammation. However, treatments for these conditions, based on this strategy, do not currently exist because the best-known inhibitors of sEH have poor bioavailability. This technology is a class of potent sEH inhibitors with improved biocompatibility. These inhibitors may potentially be used to treat hypertension, metabolic syndrome, atherosclerosis, erectile dysfunction, stroke, diabetes, and aging in humans. Additionally, these inhibitors may be used to treat laminitis disease in horses.

Technology Benefits

Novel approach to treatment of hypertensionNo treatments for metabolic syndrome currently existImproved bioavailability and potentially improved pharmacokinetic profilePatent Information:Patent Issued (US 8,653,273)Tech Ventures Reference: IR 2436

Technology Application

Treatment for hypertensionTreatment for inflammationTreatment for metabolic syndrome and syndrome XTreatment for erectile dysfunctionTreatment for atherosclerosisTreatment for strokePreventative treatment for stroke and diabetesPotential anti-aging treatment

Detailed Technology Description

None

*Abstract

None

*Inquiry

Jerry KokoshkaColumbia Technology VenturesTel: (212) 854-8444Email: TechTransfer@columbia.edu

*IR

2436

*Principal Investigator

*Publications

Pecic S, Pakhomova S, Newcomer ME, Morisseau C, Hammock BD, Zhu Z, Rinderspacher A, Deng SX. "Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors." Bioorg Med Chem Lett. 2013 Jan 15;23(2):417-21.Pecic S, Deng SX, Morisseau C, Hammock BD, Landry DW. "Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase." Bioorg Med Chem Lett. 2012 Jan 1;22(1):601-5.Xie Y, Liu Y, Gong G, Smith DH, Yan F, Rinderspacher A, Feng Y, Zhu Z, Li X, Deng SX, Branden L, Vidovic D, Chung C, Schuerer S, Morisseau C, Hammock BD, Landry DW. "Discovery of potent non-urea inhibitors of soluble epoxide hydrolase." Bioorg Med Chem Lett. 2009 Apr 15;19(8):2354-9.

Country/Region

USA