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Short Courses | Day 1 | Day 2 | Day3 | Download Brochure Friday, February 5
STRATEGIES FOR EFFECTIVE MEDICINAL CHEMISTRY 8:30 AM Chairperson's Opening Remarks Kenneth A. Savin, Ph.D., Manager, Global External Research & Development, Eli Lilly & Co. 8:35 A Paradigm Change in the Application of ADME Resources to Early Lead Generation Activities
With the advent of new technology and processes, there are new possibilities for the application of ADME resources to projects at earlier phases in a project's life-cycle. We have been able to change the way ADME supports projects with the hope of improving our ability to come to decision points earlier in lead generation. 9:05 Understanding Structure-Toxicity Relationships as a Guide to Safer Drugs John C.L. Erve, Ph.D., DABT, Principal Research Scientist II, Drug Safety Metabolism, Wyeth Research Reactive metabolites are a concern due to their potential role in drug toxicity. Despite our understanding of bioactivation pathways and ability to minimize reactive metabolite formation, toxicity remains a cause of failure during drug development. This talk will review structure-toxicity relationships so that this knowledge can benefit drug discovery. 9:35 Biotransformation to Enable Chemistry SAR Douglas Spracklin, Ph.D., Director, Pharmacokinetics, Dynamics and Metabolism, Pfizer, Inc. Biotransformation science has evolved well beyond traditional structural elucidation of metabolites. Contemporary biotransformation data is especially well suited to aid chemistry SAR development, i.e., identifying metabolic hot spots, non-obvious metabolic pathways, potential reactive metabolites, etc. Knowledge around these attributes can be extremely helpful in prioritizing chemical series and selecting individual molecules for development. 10:05 Sponsored Presentation (Sponsorship Opportunity Available) 10:20 Coffee Break
IMAGING AS AN EXCITING TOOL IN DRUG DISCOVERY Chair: Michael A. Letavic, Research Fellow, Neuroscience, Johnson & Johnson Pharmaceutical R&D 11:00 Imaging Drug Action in the Human Brain Joanna Fowler, Ph.D., Senior Chemist, Brookhaven National Laboratory Radiotracers and drug molecules labeled with short-lived positron emitting isotopes such as carbon-11 (t1/2: 20.4 min), fluorine-18 (t1/2: 110 min) or nitrogen-13 (t1/2: 10 min) are unique scientific tools for measuring biochemical transformations and drug pharmacokinetics and pharmacodynamics in the living human and animal body. 11:30 Image Analysis Considerations for Preclinical, in vivo Medical Imaging Matt Silva, Head, Imaging Sciences, Millennium, The Takeda Oncology Company With the expanding role of preclinical and translational imaging in drug research, it is necessary to consider not only study design and imaging modality but also visualization and image quantification. This presentation will review the role of imaging technologies and show examples of experiments and image analysis procedures, including kinetic analysis of dynamic contrast-enhanced MRI and bone topology analysis from 3D CT data. 12:00 PM Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own
TARGETS IN HOT PURSUIT II 1:00 Chairperson's Remarks Nick Terrett, Ph.D., Chief Scientific Officer, Ensemble Discovery Corp. 1:05 Modulators and Consequences of Hsp90 Regulation by Small Molecules Brian S. J. Blagg, Ph.D., Associate Professor of Medicinal Chemistry, The University of Kansas; Winner of the 2009 David W. Robertson Award in Medicinal Chemistry The 90 kDa heat shock proteins (Hsp90) are molecular chaperones required for the refolding of denatured proteins and the maturation of nascent polypeptides into their biologically active, three-dimensional structures. In fact, numerous proteins represented in all six hallmarks of cancer are dependent upon Hsp90 for conformational maturation. Innovative approaches toward C-terminal inhibition of Hsp90 will be discussed. 1:35 Design and Synthesis of RDEA119, a Potent and Orally Bioavailable MEK Inhibitor Jean-Michel Vernier, Ph.D., VP, Chemistry Discovery, Ardea Biosciences This presentation will discuss the design, synthesis and structural-activity relationship that led to the discovery of RDEA119, a novel highly potent and selective MEK inhibitor currently in Phase I clinical trial. RDEA119 is being developed under a global license agreement with Bayer HealthCare. 2:05 From a Concept towards a First-In-Class Drug for a Human Amyloid Disease Jeffery W. Kelly, Ph.D., Chair, Molecular and Experimental Medicine, Lita Annenberg Hazen Professor of Chemistry, The Skaggs Institute, The Scripps Research Institute The seminar will cover the twenty-one year adventure from our initial demonstration that rate-limiting transthyretin tetramer dissociation and monomer misfolding was sufficient for transthyretin amyloidogenesis linked to neurodegeneration, to the recent clinical trial results of FoldRx demonstrating that a transthyretin kinetic stabilizer halts neurodegeneration in familial amyloid polyneuropathy. This is the first pharmacologic evidence supporting the validity of the amyloid hypothesis. 2:35 DNA-Programmed Chemistry Approach to Macrocyclic Lead Compounds Nick Terrett, Ph.D., CSO, Ensemble Discovery Corp. DNA-programmed chemistry is an integrated platform for the synthesis and screening of macrocycles that interact with protein-protein drug discovery targets such as the oncology target, BCL-XL. We have also discovered a series of macrocycles that competitively antagonize the interaction of TNFα with TNF receptors in both biochemical and cell-based assays, and that also have anti-inflammatory activity in vivo. 3:05 Close of Conference
Short Courses | Day 1 | Day 2 | Day3 | Download Brochure |
Kenneth A. Savin, Ph.D., Manager, Global External Research
& Development, Eli Lilly & Co.
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