| SUNDAY |
| 2:00 pm - 9:00 pm | Arrival and check-in |
| 5:00 pm - 6:00 pm | Welcome Mixer (Dining Center) |
| 6:00 pm | Dinner |
| Opening Remarks
Conference Chair: Peter Bernstein (AstraZeneca)
Colby-Sawyer Site Manager: Andrea Curless
|
| 7:30 pm - 9:30 pm | Inflammation |
| Discussion Leader: Mark Noe (Pfizer) |
| 7:30 pm - 7:55 pm | Gebhard Thoma (Novartis)
"Orally Bioavailable Competitive Antagonists for Human and Primate CCR5" |
| 7:55 pm - 8:00 pm | Discussion |
| 8:00 pm - 8:25 pm | Geraldine Harriman (Millennium)
"Chemokine Receptor Antagonists: Discovery of Novel CCR1 Antagonists as Potential Anti-inflammatories" |
| 8:25 pm - 8:30 pm | Discussion |
| 8:30 pm - 8:55 pm | Mark Dombrowski (Pfizer)
"Identification and Characterization of a Novel Class of IL-1 Post-Translational Processing and Release Inhibitors" |
| 8:55 pm - 9:00 pm | Discussion |
| 9:00 pm - 9:25 pm | Steve Tam (Wyeth)
"Discovery of cPLA2 Inhibitors for the Treatment of Inflammatory Diseases" |
| 9:25 pm - 9:30 pm | Discussion |
| MONDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Advances in GPCR Research |
| Discussion Leader: John Saunders (Neurocrine) |
| 9:00 am - 9:30 am | Brian Kobilka (Stanford University)
"Ligand-Induced Conformational Changes in the Beta2 Adrenoceptor" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | David Mark (Roche)
"Strategy for Identifying and Validating Orphan GPCRs as Drug Discovery Targets" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 11:00 am | Coffee Break / PHOTO |
| 11:00 am - 11:30 am | Ravi Nargund (Merck)
"Design and Biological Profile of Selective Agonists and Antagonists for the Melanocortin-4 Receptor" |
| 11:30 am - 11:40 am | Discussion |
| 11:40 am - 12:10 pm | Chen Chen (Neurocrine)
"Orally Active Small Molecule GnRH Antagonists" |
| 12:10 pm - 12:20 pm | Discussion |
| 12:30 pm | Lunch |
| 1:30 pm - 6:00 pm | Free Time (organized Mt. Kearsarge hike available) |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Approaches to Treating Cognition Impairment |
| Discussion Leader: Dave Wustrow (Pfizer) |
| 7:30 pm - 8:00 pm | Wayne Childers (Wyeth)
"The Serotonin 5-HT1A Antagonist SRA-333: A Novel Treatment for Cognitive Dysfunction in Alzheimer's Disease" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Craig Miller (Targacept)
"TC-1734: An Orally Active Neuronal Nicotinic Receptor Modulator with Long-lasting Cognitive Effects" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Marlon Cowart (Abbott)
"ABT-239 and Related H3 Antagonist Analogs Potently Enhance Cognition and Attention" |
| 9:20 pm - 9:30 pm | Discussion |
| 9:45 pm - 10:45 pm | Poster Session / Social Hour
Discussion Leader: Alfonzo Jordan (Johnson & Johnson) |
| TUESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Diabetes and Associated Pathologies |
| Discussion Leader: Uli Stilz (Aventis) |
| 9:00 am - 9:30 am | Tjeerd Barf (Biovitrum)
"Inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1 as a Novel Approach to Type 2 Diabetes Treatment" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Roger Butlin (AstraZeneca)
"Discovery and Optimisation of PDH Kinase Inhibitors with Potential for Treatment of Type 2 Diabetes" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:20 am | Gerhard Jaehne (Aventis)
"Selective Adenosine A1 Receptor Agonists - An SAR Study and a Possible Role of Adenosine A1 Receptor Agonists in the Treatment of Type 2 Diabetes" |
| 11:20 am - 11:30 am | Discussion |
| 11:30 am - 12:00 pm | Mark Bilodeau (Merck)
"Angiogenesis in Diabetic Retinopathy and Macular Edema: The Investigation of Oral and Topical KDR Kinase Inhibitors for Retinal Disease" |
| 12:00 pm - 12:10 pm | Discussion |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time (organized annual East/West Softball game) |
| 5:00 pm - 6:00 pm | Poster Session
Discussion Leader: Alfonzo Jordan (Johnson & Johnson) |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Critical Topics in DMPK |
| Discussion Leader: Les McQuire (Novartis) |
| 7:30 pm - 8:00 pm | Scott Grossman (Bristol-Myers Squibb)
"What was Mother Nature Thinking? Dealing with the Inevitability of Reactive Metabolites in Pharmaceutical Development" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | William Elmquist (U. Minnesota)
"Role of Drug Transporters in ADME: Implications for Drug Design and Discovery" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | George Trainor (Bristol-Myers Squibb)
"Plasma Protein Binding and Drug Action" |
| 9:20 pm - 9:30 pm | Discussion |
| 9:45 pm - 10:45 pm | Poster Session / Social Hour
Discussion Leader: Alfonzo Jordan (Johnson & Johnson) |
| WEDNESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:45 am - 9:00 am | Conference Business meeting |
| 9:00 am - 12:30 pm | New Approaches to Cancer Chemotherapy |
| Discussion Leader: Dave Roberts (AstraZeneca) |
| 9:00 am - 9:30 am | Andrew Mortlock (AstraZeneca)
"The Development of Selective Aurora Kinase A and B Inhibitors" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | John Kath (Pfizer)
"Small Molecule Inhibitors of PDGFRb" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:20 am | Carlos Garcia-Echeverria (Novartis)
"The Discovery of Insulin-like Growth Factor I Kinase Inhibitors" |
| 11:20 am - 11:30 am | Discussion |
| 11:30 am - 12:00 pm | Craig Lindsley (Merck)
"Development of Pleckstrin Homology Domain-Dependent and Isozyme Selective Akt Kinase Inhibitors" |
| 12:00 pm - 12:10 pm | Discussion |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time (organized annual Vice-Chair elect Golf Tournament) |
| 5:00 pm - 6:00 pm | Poster Session
Discussion Leader: Alfonzo Jordan (Johnson & Johnson) |
| 7:30 pm - 9:30 pm | Addiction and Substance Abuse |
| Discussion Leader: Anabella Villalobos (Pfizer) |
| 7:30 pm - 8:00 pm | Jennifer Whistler (UCSF)
"Rave, Addiction and Trafficking: A GPCR's Journey" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | F. Ivy Carroll (RTI)
"Pharmacotherapies for Treatment of Cocaine Abuse - Preclinical Aspects" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Jotham Coe (Pfizer)
"Nicotine Meets its Match?" |
| 9:20 pm - 9:30 pm | Discussion |
| THURSDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Late Breaking Topics |
| Discussion Leader: Anandan Palani (Schering-Plough) |
| 9:00 am - 9:30 am | Rob Kania (Pfizer)
"Structure-Based Design, Synthesis and Evaluation of Potent and Selective Inhibitors of VEGFR2 Tyrosine Kinase" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Hartmut Strobel (Aventis)
"Activators of Ferric Soluble Guanylyl Cyclase - Discovering a Novel Pathomechanism for Coronary Heart Disease?" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:20 am | Gene Trybulski (Wyeth)
"The Identification of Ligands which Selectively Inhibit NF-KB Transcriptional Activity Through the Estrogen Receptor and their Utility in Rheumatoid Arthritis" |
| 11:20 am - 11:30 am | Discussion |
| 11:30 am - 12:00 pm | Robert Zamboni (Merck Frosst)
"The Development of L-888839, a Potent and Selective Prostaglandin D2 Receptor Antagonist, Lessons in Reactive Intermediates and Transporters" |
| 12:00 pm - 12:10 pm | Discussion |
| 12:30 pm | Lunch |
| 1:30 pm - 6:00 pm | Free Time |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Chair's Talk |
| Discussion Leader: Peter Bernstein (AstraZeneca) |
| 7:30 pm - 8:30 pm | George Milne (Pfizer - retired)
"Cracking Pharmaceutical Industry Productivity - The Leadership Imperative for Medicinal Chemistry" |
| 8:30 pm - 9:30 pm | Discussion |
| FRIDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am | Departure |
