Chiral Synthesis of Pyrrolidine Core Compounds en route to Neuronal Nitric Oxide Synthase Inhibitors

Research output: Patent

Abstract

Chiral Synthesis for Production of Selective Neuronal Nitric Oxide Synthase Inhibitors for Treatment of Neurodegenerative Diseases NU 2010-008 Inventors Fengtian Xue Richard B. Silverman* Short Description Chemical synthesis method for a neurodegenerative disease drug candidate Abstract Neurodegenerative disorders, such as Alzheimer's, Parkinson's, and Huntington's diseases, affect millions of Americans. Hundreds of billions of dollars are spent annually to treat and care for patients with these generally incurable conditions. There is an urgent need for development of effective therapies for neurodegenerative disease. A key pathogenic phenomenon observed in a variety of these diseases is increased concentration of cerebral nitric oxide (NO). As a result, the neuronal isoform of nitric oxide synthase (nNOS) has been a target for therapy development. Northwestern investigators identified a compound useful for the inhibition of nNOS and demonstrated its effective in animal tests; however, the compound is difficult to synthesize and yields are low. The inventors have subsequently developed a method of chiral synthesize of the compounds to achieve greater quantities of the desired molecules. This method (plus additional purification steps) will yield quantities of the nNOS inhibitors suitable for further research and trials. Applications o Synthesis of selective neuronal nitric oxide synthase inhibitor for treatment of neurodegenerative disorders Advantages o Large scale production of precursors to a potential drug IP Status A patent application has been filed. Marketing Contact Allan Nader, PhD Invention Manager (e) a-nader@northwestern.edu (p) 847.491.4456
Original languageEnglish
Patent number8697879
StatePublished - Jan 5 2012

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