Small Molecule Inhibitors Of Kynurenine 3-Monooxygenase

OverviewKynurenic acid has neuroprotective activities in vivo while the metabolic byproduct of kynurenic acid, quinolinic acid, is neurotoxic. Kynurenine 3-monooxygenase catalyzes the conversion of kynurenine into 3-hydroxykynurenine, a precusor …

Overview

Kynurenic acid has neuroprotective activities in vivo while the metabolic byproduct of kynurenic acid, quinolinic acid, is neurotoxic. Kynurenine 3-monooxygenase catalyzes the conversion of kynurenine into 3-hydroxykynurenine, a precusor of neurotoxic quinolinic acid. In light the properties of kynurenic acid and quinolinic acid, pharmacological intervention directed at inhibiting quinolinic acid and/or increasing kynurenic acid is a viable therapeutic approach for treating neurological diseases and neurological manifestations of diseases. The invention relates to benzensulfonamide compounds that inhibit kynurenine 3-monooxygenase and methods of treatment using the same. (EXTENDED MARKETING SUMMARY AVAILABLE ON REQUEST)

Applications

-Novel methods of treating neurological diseases and neurological manifestations of diseases, ranging from Alzheimer's disease to diabetes -2nd generation production of kynurenine 3-monooxygenase inhibitors

Advantages

-The invention relates to small molecule inhibitors of kynurenine 3- monooxygenase. Small molecules have the advantage of cell permeability, blood- brain barrier permeability, not eliciting immune responses, enhanced stability, decreased biomaterial contamination potential, and the capacity for large-scale manufacturing. -The kynurenine 3-monooxygenase inhibitors of the invention can be used to increase concentrations of neutoprotective kynurenic acid while decreasing neurotoxic quinolinic acid.

Stage of Development

Small molecule inhibitors of kynurenine 3-monooxygenase have been developed and shown to inhibit the activity of kynurenine 3-monooxygenase.

R&D Required

Preclinical studies are required to provide safety and efficacy data, which will enable clinical trials to follow.