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DABCO ion channel modulators

DABCO ion channel modulators. DABCO Ion Channel Modulators. Inventors: Geoffrey W. Abbott, PhD Department of Medicine, Weill Cornell.

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DABCO ion channel modulators

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  1. DABCO ion channel modulators DABCO Ion Channel Modulators Inventors: Geoffrey W. Abbott, PhD Department of Medicine, Weill Cornell Dr. Abbott is an inventor of US Patent 6,864,364 covering MinK-related genes, important in long QT syndrome. Investors seek his ion channel expertise for diligence on drug candidates that may cause this side effect. Dr. Engel is an expert organic chemist, and is the inventor of DABCO, under development as an anti-infective fabric coating; Dr. Rizzo is Dr. Engel’s protégé. And: Dr. Robert Engel City University of New York; Dr. Jaimie Lee Rizzo Pace University

  2. DABCO ion channel modulators Ion channel modulation in a nutshell

  3. DABCO ion channel modulators Market Pain ~$27B Epilepsy ~$13B Multiple Sclerosis ~$5B Cancer ~$15B Other potential applications, as yet unexplored

  4. DABCO ion channel modulators tetraethylammonium (TEA) DABCO DiDABCO – generalized structure

  5. DABCO ion channel modulators Why DABCO? • Similar to TEA • Quaternary ammonium ions have historical precedent as Kv channel blockers • Infinitely expandable structural platform • Quaternization provides the charge necessary for activity and can introduce any of a massive range of functional groups • No adverse effects on key cardiac ion channels • TEA does not show high affinity for hERG or KCNQ1 • As hypothesized, neither do DABCO compounds, therefore overcoming the significant hurdle of acting on some Kv channels but avoiding key drug-induced arrhythmia channels

  6. DABCO ion channel modulators Mechanisms of action

  7. DABCO ion channel modulators • Developmental Status • In vitro testing of members of several structural classes performed; no animal studies yet • SAR studies underway • Extracellular blocker binding site identified • Intellectual Property • US Patent application pending with broad Markush claims • Availability • Exclusive licenses available

  8. DABCO ion channel modulators Next Steps • Accelerate evaluation of derivatives in current model • Move to medium or high-throughput screening • Expand studies to other ion channels • Other Kv channel subfamilies, other K+ channels • TRP channels – (pain, cancer) • neurotransmitter-gated ion channels (pain, depression) • Begin animal studies • Toxicity testing • Efficacy in models of pain, cancer, epilepsy, MS etc

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