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B Vitamin analogs & synthetic methods. Analogs of a

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B Vitamin analogs & synthetic methods. Analogs of a B Vitamin (Nicotinamide Riboside) ... Sirtuins are the apparent target of resveratrol ... – PowerPoint PPT presentation

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Title: B Vitamin analogs & synthetic methods. Analogs of a


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 Cardioprot
ection 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
  • 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
Nicotinamide Riboside (NR)
NR was found in milk in 1950s the enzyme that
converts NR to NAD not found until 2000s -- NR
is a vitamin. No NR on market as dietary
supplement
6
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
  • Developmental status
  • Novel compounds generated
  • in vitro testing underway
  • Intellectual Property
  • US and PCT patent applications pending
  • Availability
  • Exclusive licenses available by field-of-use
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