| SUNDAY |
| 2:00 pm - 11:00 pm | Arrival and Check-in |
| 5:00 pm - 6:00 pm | Welcome Mixer (Dining Center) |
| 6:00 pm | Dinner |
| 7:15 pm - 7:30 pm | Welcome (George Hartman, Conference Chair) / Introductory Comments by GRC Site Staff |
| 7:30 pm - 9:30 pm | Application Of Targeted Prodrugs To Improve Pharmacokinetic And Pharmacodynamic Parameters |
| Discussion Leader: Manoj C. Desai (Gilead Sciences) |
| 7:30 pm - 8:00 pm | Dennis A. Smith (Pfizer)
"Do Prodrugs Deliver?" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Richard Mackman (Gilead Sciences)
"Discovery of GS9131, An Amidate Prodrug of a Novel Nucleoside Phosphonate HIV Reverse Transcriptase Inhibitor" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Mark Gallop (XenoPort)
"Actively Transported Prodrugs of GABA Analogs: Chemistry, Biology and Clinical Efficacy" |
| 9:20 pm - 9:30 pm | Discussion |
| 9:45 pm - 10:45 pm | Poster Session / Social Hour |
| Discussion Leader: Rachael Hunter (Cephalon) |
| MONDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Kinases |
| Discussion Leader: Mary Mader (Eli Lilly) |
| 9:00 am - 9:30 am | Michal Vieth (Eli Lilly)
"Kinase Bioprints - Understanding, Modeling and Exploring Kinase Selectivity" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Mark Fraley (Merck)
"The Discovery of Potent Checkpoint Kinase I (Chk1) Inhibitors for the Treatment of Cancer" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am | Coffee Break / Group Photo |
| 11:00 am - 11:30 am | Paul Lyne (Astra-Zeneca)
"Application Of Lead And Target Hopping Approaches To The Discovery And Optimization Of Mutant B-Raf Inhibitors" |
| 11:30 am - 11:40 am | Discussion |
| 11:40 am - 12:10 pm | Mike Luzzio (Pfizer)
"The Discovery and Preclinical Development of Focal Adhesion Kinase Inhibitors" |
| 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 | New Approaches to Cardiovascular Diseases |
| Discussion Leader: Stéphane De Lombaert (Boehringer-Ingelheim) |
| 7:30 pm - 8:00 pm | Roger Ruggeri (Pfizer)
"CETP Inhibition: Promise and Peril in Drug Discovery and Development" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Robert Stavenger (GSK)
"Rho Kinase Inhibitors as Potential Therapeutic Agents for Cardiovascular Diseases" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Samuel Chackalamannil (Schering-Plough)
"Discovery of a Himbacine-based Thrombin Receptor (PAR-1) Antagonist as a Novel Antiplatelet Agent" |
| 9:20 pm - 9:30 pm | Discussion |
| 9:45 pm - 10:45 pm | Poster Session / Social Hour |
| Discussion Leader: Rachael Hunter (Cephalon) |
| TUESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:45 am - 9:00 am | Nominations for Chair of 2010 Meeting
Nominating Committee |
| 9:00 am - 12:30 pm | Approaches Toward Treatment of Sleep and Wake Disorders |
| Discussion Leader: Jim Barrow (Merck) |
| 9:00 am - 9:30 am | Dale Edgar (Hypnion)
"Principles and Practice of Sleep-Wake Drug Discovery" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Ling Hong Xie (Neurogen)
"Discovery of NG2-73, an α3-Preferring GABAa Partial Agonist for Insomnia" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am | Coffee Break |
| 11:00 am - 11:30 am | Christoph Boss (Actelion)
"Orexin Receptor Antagonists: A New Therapeutic Principle in Neurology and Psychiatry?" |
| 11:30 am - 11:40 am | Discussion |
| 11:40 am - 12:10 pm | Michael Letavic (Johnson & Johnson)
"Histamine H3 Antagonists: Potential Applications for the Treatment of Excessive Sleepiness, Narcolepsy and Attention Disorders" |
| 12:10 pm - 12:20 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: Rachael Hunter (Cephalon) |
| 6:00 pm | Dinner |
| 7:15 pm - 7:30 pm | Speeches by the Candidates for Chair of the 2010 Meeting
Nominating Committee |
| 7:30 pm - 9:30 pm | Disruptors of Protein-Protein Interactions |
| Discussion Leader: Mike Shultz (Novartis) |
| 7:30 pm - 8:00 pm | Jean Chmielewski (Purdue)
"Disrupting Protein-Protein Interactions" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Michael Wendt (Abbott)
"Discovery Of ABT-263, An Orally Bioavailable Bcl-2 Family Inhibitor" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Kurt Deshayes (Genentech)
"Inducing Programmed Cell Death in Cancer: A New Therapeutic Approach" |
| 9:20 pm - 9:30 pm | Discussion |
| 9:45 pm - 10:45 pm | Social Hour |
| WEDNESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:45 am - 9:00 am | Business Meeting |
| (Election of Chair for the 2010 Meeting; Discussion of GRC Medicinal Chemistry 2010 site; Meeting Evaluation Form) |
| 9:00 am - 12:30 pm | Structure-Based Drug Design |
| Discussion Leader: Mark Murko (Vertex) |
| 9:00 am - 9:30 am | Martin Drysdale (Vernalis)
"Discovery and Structure Guided Optimization of Hsp90 Inhibitors for the treatment of cancer" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Theresa Williams (Merck)
"The Design of 2nd Generation HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am | Coffee Break |
| 11:00 am - 11:30 am | John Mathias (Pfizer)
"Structure-Based Design of PDE4 Inhibitors as Potential Inhaled Anti-Inflammatories" |
| 11:30 am - 11:40 am | Discussion |
| 11:40 am - 12:10 pm | Patrick Lam (BMS)
"Molecular Recognition in Drug Design - Structure-based Discovery of Apixaban as Novel Factor Xa Inhibitor" |
| 12:10 pm - 12:20 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 |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Advancing Targets for Treating Pain |
| Discussion Leader: Mark Bilodeau (Merck) |
| 7:30 pm - 8:00 pm | Michael P. Dillon (Roche)
"Purinergic Receptor Antagonists: Novel Treatments For Pain And Overactive Bladder" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Christopher Burgey (Merck)
"Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists for the Treatment of Migraine" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Mark Suto (Icagen)
"Ion Channel Approaches for the Treatment of Pain" |
| 9:20 pm - 9:25 pm | Discussion |
| 9:25 pm - 9:30 pm | Presentation of Poster Awards |
| Rachael Hunter (Cephalon) |
| 9:45 pm - 10:45 pm | Social Hour |
| THURSDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Late Breaking Topics |
| Discussion Leader: Kateri Ahrendt (Array) |
| 9:00 am - 9:30 am | Louis N. Jungheim (Eli Lilly)
"The Discovery and Optimization of Triazole-Based NK-1 Antagonists" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Renata M. Oballa (Merck Frosst)
"The Discovery of MK-0822: A Selective Inhibitor of Cathepsin K for the Treatment of Osteoporosis" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am | Coffee Break |
| 10:40 am - 11:10 am | William N. Washburn (BMS)
"SGLT-2 Inhibition: A Promising New Approach for Type 2 Diabetes" |
| 11:10 am - 11:20 am | Discussion |
| 11:20 am - 11:50 am | Stephen J. Baker (Anacor)
"AN2690, A Topical Oxaborole for Onychomycosis. Discovery, Development And Mechanism Of Action Of This New Antifungal Agent" |
| 11:50 am - 12:00 pm | Discussion |
| 12:00 pm - 12:30 pm | Poster Award Winner Talks |
| Discussion Leader: Rachael Hunter (Cephalon) |
| 12:30 pm | Lunch |
| 1:30 pm - 5:00 pm | Free Time |
| 5:00 pm - 6:00 pm | Chair's Reception |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | Chair's Talk |
| Paul Anderson
"A Retrospective Look at Drug Discovery" |
| Discussion |
| 9:45 pm - 10:45 pm | Social Hour |
| FRIDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am | Depart |
