Controlled HNO Release through Intramolecular Cyclization-Elimination

Case ID:
C12038

#C12038

Inventor(s): John Toscano, Art Sutton


Unmet Need:

An estimated 17.9 million people died from cardiovascular diseases in 2019, representing 32% of all global deaths (see WHO). Nitroglycerin has been used as a vasodilator to treat heart conditions for over 130 years. It wasn't until 2003 that scientists realized the beneficial effect was due to it being converted by the body to nitric oxide (NO). Nitroxyl (HNO) chemistry, which was largely ignored over the course of the 20th century, has experienced a resurgence since HNO and NO are redox-related. Treatment with HNO could provide a route as a drug treatment for cardiovascular disease. Due to its inherent reactivity, however, HNO cannot be used directly, and therefore must be generated within the body through the use of prodrugs. Therefore, there is a strong need to develop HNO prodrug compounds where the time scale for release within the body can be controlled by the chemistry.


Technology Overview:

Researchers at Johns Hopkins have developed chemically tunable compounds that are capable of undergoing intramolecular cyclic-elimination at neutral pH under physiological conditions to non-enzymatically release HNO. The rate of cyclization, and therefore HNO release, can be tuned by the substituents and chain length of the compounds. HNO has a short half-life in the body, so being able to control its release rate is desirable as a potential drug treatment.


Stage of Development:

Experimental data available.


Publication:

N/A

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Controlled HNO Release through Intramolecular Cyclization-Elimination PCT: Patent Cooperation Treaty United States 14/439,800 9,676,708 4/30/2015 6/13/2017 10/30/2033 Granted
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For Information, Contact:
Mohit Ganguly
mgangul1@jh.edu
410-614-0300
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