O2-Benzyl-substituted Dizeniumdiolates that Release Nitric Oxide at Controlled Rates Upon Photolysis

Nitric oxide (NO) is a critically important bioregulator, involved in a wide range of processes including neurotransmission, blood clotting, and blood pressure control. In addition, macrophages have been shown to kill cancerous tumor cells and intercellular parasites by releasing large amounts of NO. Deficiencies in these processes caused by a poor endogenous supply of NO are often treatable with NO-releasing drugs. This invention describes novel photochemical precursors to NO based on the photorelease of diazeniumdiolates (XN(O)NO-, where X = a nucleophile). These photochemical precursors (XN(O)NOP) are unique in that they candeliver NO specifically to a targeted site in a temporally controlled manner, allowing mechanistic investigations into the biological effects of NO that were previously impossible. Given the large number of biological phenomena known to be mediated by NO, such targeting is also critical to the success of most medical applications. The specificity of delivery is controlled by photolysis of an appropriately chosen photoprotecting group (P). The temporal aspects of delivery are controlled by the substituent X, which determines the ultimate rate of NO release from the photodeprotected diazeniumdiolate. Description (Set) Proposed Use (Set) This technology could be used as an investigational tool to probe the biological mechanisms of NO effects. - This technology could be used to develop pharmaceuticals that deliver NO to a specific target with controlled release.

Patent (Set) 7,122,529 B2; WO 03/006427

Patents:
US 7,122,529

Inventor(s): Toscano, John

Type of Offer: Licensing



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