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Medicinal Chemistry
Gordon Research Conference

Dates

August 5-10, 2007

Location

Colby-Sawyer College
New London, NH

Organizers

Chair:
George D. Hartman

Vice Chair:
Les W. McQuire

Meeting Program

SUNDAY
2:00 pm - 11:00 pmArrival and Check-in
5:00 pm - 6:00 pmWelcome Mixer (Dining Center)
6:00 pmDinner
7:15 pm - 7:30 pmWelcome (George Hartman, Conference Chair) / Introductory Comments by GRC Site Staff
7:30 pm - 9:30 pmApplication Of Targeted Prodrugs To Improve Pharmacokinetic And Pharmacodynamic Parameters
Discussion Leader: Manoj C. Desai (Gilead Sciences)
7:30 pm - 8:00 pmDennis A. Smith (Pfizer)
"Do Prodrugs Deliver?"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmRichard Mackman (Gilead Sciences)
"Discovery of GS9131, An Amidate Prodrug of a Novel Nucleoside Phosphonate HIV Reverse Transcriptase Inhibitor"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmMark Gallop (XenoPort)
"Actively Transported Prodrugs of GABA Analogs: Chemistry, Biology and Clinical Efficacy"
9:20 pm - 9:30 pmDiscussion
9:45 pm - 10:45 pmPoster Session / Social Hour
Discussion Leader: Rachael Hunter (Cephalon)
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmKinases
Discussion Leader: Mary Mader (Eli Lilly)
9:00 am - 9:30 amMichal Vieth (Eli Lilly)
"Kinase Bioprints - Understanding, Modeling and Exploring Kinase Selectivity"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amMark Fraley (Merck)
"The Discovery of Potent Checkpoint Kinase I (Chk1) Inhibitors for the Treatment of Cancer"
10:10 am - 10:20 amDiscussion
10:20 am Coffee Break / Group Photo
11:00 am - 11:30 amPaul 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 amDiscussion
11:40 am - 12:10 pmMike Luzzio (Pfizer)
"The Discovery and Preclinical Development of Focal Adhesion Kinase Inhibitors"
12:10 pm - 12:20 pmDiscussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time (Organized Mt. Kearsarge Hike available)
6:00 pmDinner
7:30 pm - 9:30 pmNew Approaches to Cardiovascular Diseases
Discussion Leader: Stéphane De Lombaert (Boehringer-Ingelheim)
7:30 pm - 8:00 pmRoger Ruggeri (Pfizer)
"CETP Inhibition: Promise and Peril in Drug Discovery and Development"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmRobert Stavenger (GSK)
"Rho Kinase Inhibitors as Potential Therapeutic Agents for Cardiovascular Diseases"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmSamuel Chackalamannil (Schering-Plough)
"Discovery of a Himbacine-based Thrombin Receptor (PAR-1) Antagonist as a Novel Antiplatelet Agent"
9:20 pm - 9:30 pmDiscussion
9:45 pm - 10:45 pmPoster Session / Social Hour
Discussion Leader: Rachael Hunter (Cephalon)
TUESDAY
7:30 am - 8:30 amBreakfast
8:45 am - 9:00 amNominations for Chair of 2010 Meeting
Nominating Committee
9:00 am - 12:30 pmApproaches Toward Treatment of Sleep and Wake Disorders
Discussion Leader: Jim Barrow (Merck)
9:00 am - 9:30 amDale Edgar (Hypnion)
"Principles and Practice of Sleep-Wake Drug Discovery"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amLing Hong Xie (Neurogen)
"Discovery of NG2-73, an α3-Preferring GABAa Partial Agonist for Insomnia"
10:10 am - 10:20 amDiscussion
10:20 amCoffee Break
11:00 am - 11:30 amChristoph Boss (Actelion)
"Orexin Receptor Antagonists: A New Therapeutic Principle in Neurology and Psychiatry?"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmMichael Letavic (Johnson & Johnson)
"Histamine H3 Antagonists: Potential Applications for the Treatment of Excessive Sleepiness, Narcolepsy and Attention Disorders"
12:10 pm - 12:20 pmDiscussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time (Organized Annual East-West Softball Game)
5:00 pm - 6:00 pmPoster Session
Discussion Leader: Rachael Hunter (Cephalon)
6:00 pmDinner
7:15 pm - 7:30 pmSpeeches by the Candidates for Chair of the 2010 Meeting
Nominating Committee
7:30 pm - 9:30 pmDisruptors of Protein-Protein Interactions
Discussion Leader: Mike Shultz (Novartis)
7:30 pm - 8:00 pmJean Chmielewski (Purdue)
"Disrupting Protein-Protein Interactions"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmMichael Wendt (Abbott)
"Discovery Of ABT-263, An Orally Bioavailable Bcl-2 Family Inhibitor"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmKurt Deshayes (Genentech)
"Inducing Programmed Cell Death in Cancer: A New Therapeutic Approach"
9:20 pm - 9:30 pmDiscussion
9:45 pm - 10:45 pmSocial Hour
WEDNESDAY
7:30 am - 8:30 amBreakfast
8:45 am - 9:00 amBusiness Meeting
(Election of Chair for the 2010 Meeting; Discussion of GRC Medicinal Chemistry 2010 site; Meeting Evaluation Form)
9:00 am - 12:30 pmStructure-Based Drug Design
Discussion Leader: Mark Murko (Vertex)
9:00 am - 9:30 amMartin Drysdale (Vernalis)
"Discovery and Structure Guided Optimization of Hsp90 Inhibitors for the treatment of cancer"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amTheresa Williams (Merck)
"The Design of 2nd Generation HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors"
10:10 am - 10:20 amDiscussion
10:20 amCoffee Break
11:00 am - 11:30 amJohn Mathias (Pfizer)
"Structure-Based Design of PDE4 Inhibitors as Potential Inhaled Anti-Inflammatories"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmPatrick Lam (BMS)
"Molecular Recognition in Drug Design - Structure-based Discovery of Apixaban as Novel Factor Xa Inhibitor"
12:10 pm - 12:20 pmDiscussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time (Organized Annual Vice-Chair Elect Golf Tournament)
5:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmAdvancing Targets for Treating Pain
Discussion Leader: Mark Bilodeau (Merck)
7:30 pm - 8:00 pmMichael P. Dillon (Roche)
"Purinergic Receptor Antagonists: Novel Treatments For Pain And Overactive Bladder"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmChristopher Burgey (Merck)
"Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists for the Treatment of Migraine"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmMark Suto (Icagen)
"Ion Channel Approaches for the Treatment of Pain"
9:20 pm - 9:25 pmDiscussion
9:25 pm - 9:30 pmPresentation of Poster Awards
Rachael Hunter (Cephalon)
9:45 pm - 10:45 pmSocial Hour
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmLate Breaking Topics
Discussion Leader: Kateri Ahrendt (Array)
9:00 am - 9:30 amLouis N. Jungheim (Eli Lilly)
"The Discovery and Optimization of Triazole-Based NK-1 Antagonists"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amRenata 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 amDiscussion
10:20 am Coffee Break
10:40 am - 11:10 amWilliam 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 pmDiscussion
12:00 pm - 12:30 pmPoster Award Winner Talks
Discussion Leader: Rachael Hunter (Cephalon)
12:30 pmLunch
1:30 pm - 5:00 pmFree Time
5:00 pm - 6:00 pmChair's Reception
6:00 pmDinner
7:30 pm - 9:30 pmChair's Talk
Paul Anderson
"A Retrospective Look at Drug Discovery"
Discussion
9:45 pm - 10:45 pmSocial Hour
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart
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