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B Vitamin analogs & synthetic methods

B Vitamin analogs & synthetic methods. Analogs of a B Vitamin (Nicotinamide Riboside) that act on Sirtuin pathways and efficient, stereoselective methods to synthesize. Inventor: Anthony Sauve, PhD Assistant Professor of Pharmacology. Leader in the study of sirtuin biochemistry.

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B Vitamin analogs & synthetic methods

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  1. B Vitamin analogs & synthetic methods Analogs of a B Vitamin (Nicotinamide Riboside) that act on Sirtuin pathways and efficient, stereoselective methods to synthesize Inventor: Anthony Sauve, PhD Assistant Professor of Pharmacology Leader in the study of sirtuin biochemistry. Co-inventor on key sirtuin patents.

  2. B Vitamin analogs & synthetic methods Markets B vitamins (dietary supplement) ~$200M Cardioprotection in acute MI (drug) ~$1.3B Neuroprotection/anti-aging (drug) ~$1B Alleviate drug toxicity (e.g. statins) ~$?? Cancer ~$15B total

  3. B Vitamin analogs & synthetic methods The recent discovery of the sirtuin family of enzymes has generated enormous scientific and commercial excitement • Sirtuins are the apparent target of resveratrol • Sirtuins appear to be the long-sought biochemical agent responsible for the effects of caloric restriction – a dietary regime known to drastically retard aging (effect discovered at Cornell in 1934) Sirtris Pharmaceuticals, Inc. Completes Initial Public Offering CAMBRIDGE, Mass (BUSINESS WIRE) May 30, 2007. Sirtris Pharmaceuticals, Inc. (NASDAQ: SIRT), a biopharmaceutical company focused on discovering and developing small molecule drugs to treat diseases of aging such as Type 2 Diabetes, announced today the completion of its initial public offering of 6,900,000 shares of common stock…. All shares were sold at an initial public offering price of $10.00 per share, resulting in aggregate net proceeds to Sirtris of approximately $62.4 million….

  4. B Vitamin analogs & synthetic methods • Sirtuins are HDACs - they deacetylate proteins in a reaction that consumes nicotinamide adenine dinucleotide (NAD). • Cells produce NAD from niacin (the primary B vitamin), and use it to transport electrons in the citric acid cycle – the basic process of cellular respiration. • In the course of investigating sirtuin biochemistry, Prof. Sauve has been part of a group of investigators re-invigorating the study of B vitamins and NAD metabolism. • Increasing intracellular NAD levels can improve or preserve the health of a cell. • Compounds that poison NAD metabolic pathways can be toxic – two cancer drugs on the market do so: tiazofurin and benzamide riboside

  5. B Vitamin analogs & synthetic methods Nicotinamide Riboside (NR) NR was found in milk in 1950’s; the enzyme that converts NR to NAD not found until 2000’s -- NR is a vitamin. No NR on market as dietary supplement

  6. B Vitamin analogs & synthetic methods Until now, there has been no cost-efficient method to synthesize NR. • Scalable, one pot, high-yield method • Can stereoselectively synthesize NR and control creation of derivatives • Novel derivatives generated • Cell protective • Cell killing

  7. B Vitamin analogs & synthetic methods • Developmental status • Novel compounds generated • in vitro testing underway • Intellectual Property • US20070117765 • WO2007061798, nationalized in EU, India, China • Availability • Exclusive licenses available by field-of-use

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