Molecular Medicine Tri-Conference 2008 - Mastering Medicinal Chemistry

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Wednesday, March 26

7:00am Registration (Open until 5:30pm)

8:00 Plenary Keynote Introduction
Edward G. Heidig, Chief Deputy Director, Department of Managed Health Care

8:10 Risk Diagnosis for Disease Prevention
C. Thomas Caskey, M.D., F.A.C.P., Director and Chief Executive Officer, Brown Foundation Institute of Molecular Medicine, University of Texas Health Science Center

8:55 Disruption of the Pharmaceutical Industry: Moving from Products to Solutions
Elizabeth L. Bewley, MBA, Vice President, Strategic Planning, Johnson & Johnson Health Care Systems Inc. - Speaker Biography

9:40 Grand Opening Refreshment Break in the Exhibit Hall

11:00 Chairperson’s Remarks
Hing L. Sham, Ph.D., Senior Vice President, Chemical Sciences, Elan Pharmaceuticals Inc.

11:10 Meeting the Challenges of Our Industry - The Role of Chemistry in a Winning R&D Strategy
Terence A. Kelly, Ph.D., Vice President, Medicinal Chemistry, Boehringer Ingelheim
Pharmaceuticals Inc.

11:40 Meeting the Challenges of Our Industry - The Role of Technology in a Winning R&D Strategy
James B. Summers, Ph.D. Divisional Vice President, Advanced Technology, Global Pharmaceutical Discovery, Abbott Laboratories
Powerful forces are challenging the future of the pharmaceutical industry. Increased pressure on health care spending, rising regulatory scrutiny, and escalating generic competition mandate an effective R&D strategy. More than ever before companies must drive toward best-in-class drugs with unquestionable benefit versus risk. They must maximize the investment in R&D through unprecedented levels of productivity and efficiency. This talk will look at how chemistry and related technologies can play a central role in achieving these critical goals and meeting the chal-lenging forces facing the industry.

12:10pm In Silico / Biological Fingerprinting: The Challenge of Experimental Data to Concepts of Structural and Activity Similarity and Risk Management
Jonathan S. Mason, Ph.D., Divisional Director, Early Lead Generation & Computational Chemistry, Lundbeck Research DK
The concept that similar compounds have similar activity is challenged by recent multi-target data. This affects a major challenge in the drug discovery process of the selection of a develop-ment candidate that is differentiated from other compounds with attrition risk minimized or at least orthogonalized for multiple candidates. The presentation will cover results from a major study of drug, attrited and project compounds using systematic biological profiling (Cerep BioPrintâ), the use of pharmacophore fingerprints to drive ligand-receptor interactions (FLAP) and a large scale biological data integration project.

12:40 Technology Spotlight
From Ideas to Preclinical Candidates: MedChem-Driven Drug Discovery
Dr. Pierfausto Seneci, Chief Business Officer, NiKem Research s.r.l.
A successful case study, starting from in silico studies and delivering meaningful preclinical candidates to our client, illustrates NiKem’s core competencies (medicinal and computational chemistry, biological and early ADMET/PK profiling) applied to key drug discovery phases (hit generation and validation, hit-to-lead and multi-parametric lead optimization).

1:10 Walk & Talk Luncheon in the Exhibit Hall

2:15 Chairperson’s Remarks
Mark J. Suto, Ph.D., Vice President, Chemistry, Icagen Inc.

2:20 Purinergic Receptor Antagonists: Novel Treatments for Inflammatory and Neuropathic Pain
Michael P. Dillon, Ph.D., Director, Medicinal Chemistry, Roche Palo Alto LLC
Purinergic receptors are a family of ligand gated ion channels whose endogenous ligand is ATP. Homomeric P2X3 and heteromeric P2X2/3 receptors are selectively localized at the peripheral and central terminals of non-myelinated afferent nerve fibers and, along with ATP, have been implicated in the transmission of sensory signals. Blockade of these signals with antagonists offers the potential to treat a broad range of pain conditions. This presentation will describe the lead discovery, optimization and SAR of selective drug-like antagonists; in vivo efficacy in a number of preclinical models outlining the therapeutic potential.

2:50 Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists for the Treatment of Migraine: Challenges in the Development of Clinical Candidate MK-0974
Christopher Steven Burgey, Ph.D., Director, Medicinal Chemistry, Merck Research Laboratories
Calcitonin gene-related peptide (CGRP) is a neuropeptide that may be involved in the pathogenesis of migraine headache and CGRP receptor antagonists represent a promising new ap-proach for the treatment of migraine. Since CGRP receptor antagonists lack direct vasoconstrictor activity, this approach may offer advantages over current 5–HT1B/1D receptor agonists, where cardiovascular liabilities are a perceived risk Elements of design and optimization leading to MK-0974, an orally bioavailable CGRP receptor antagonist currently in Phase III clinical trials, will be discussed.

3:20 Discovery of TRPV1 Antagonists for Treatment of Pain
Chih-Hung “Lance” Lee, Ph.D., Senior Group Leader, Abbott Neuroscience, Abbott
The vanilloid receptor TRPV1 is a membrane-bound, non-selective cation channel which can be activated by a number of noxious stimuli, including heat, protons, and ligand agonists such as capsaicin. TRPV1 antagonists have been discovered that show potent, competitive inhibition of capsaicin-induced Ca2+ influx in vitro, and potent antinociception in vivo. High-throughput screening of the Abbott compound library identified several hits. Lead optimization of these hits yielded compounds with improved pharmacokinetic and pharmaceutical properties. The dis-covery and characterization of lead compounds for clinical evaluation as potential novel agents for pain management will be discussed.

3:50 Potassium Channel Modulators for the Treatment of Pain
Mark J. Suto, Ph.D., Vice President, Chemistry, Icagen Inc.
The molecular correlates of M-channels Kv7.2 – Kv7.5, are also known as KCNQ2 to KCNQ5. They are expressed throughout the central and peripheral nervous system and regulate neuronal excitability. Therefore, small molecule modulation of these channels may provide an effective strategy to treat conditions of excessive neuronal excitability such as neuropathic pain and epilepsy. The presentation will describe several different series of compounds that selectively modulate endogenously expressed M-channels and are active in animal models of not only epilepsy but also pain.

4:20 Reception in the Exhibit Hall (Sponsorship Available)

5:00 - 6:00pm Break-out Discussions in the Exhibit Hall
Drug-Drug Interaction (DDI)
Moderator: David A. Price, Ph.D., Director, Cardiovascular Metabolic and Endocrine Diseases Chemistry, Pfizer Global Research and Development
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