SUNDAY |
2:00 PM - 9:00 PM | Arrival & Registration |
4:30 PM - 6:00 PM | Welcoming Mixer |
6:00 PM | Dinner |
7:15 PM - 7:30 PM | Introduction and Conference Welcome |
| Proteases |
| Discussion Leader: Amy Ripka (BMS) |
7:30 PM - 8:00 PM | Dan Veber (GSK) Molecular properties that influence the oral bioavailability of drug candidates |
8:00 PM - 8:10 PM | Discussion |
8:10 PM - 8:40 PM | Phil Stein (BMS) Inhibitors of Coagulation Factor Xa- How Low Can You Get |
8:40 PM - 8:50 PM | Discussion |
8:50 PM - 9:20 PM | Jeremy Levin (AHP) Novel TACE Inhibitors |
9:20 PM - 9:30 PM | Discussion |
9:30 PM | Continuation of Welcoming Mixer |
MONDAY |
7:30 AM - 8:30 AM | Breakfast |
8:45 AM - 9:00 AM | Greeting and Meeting Business |
| Metabolic Syndrome |
| Discussion Leader: Jeff Cobb (GSK) |
9:00 AM - 9:30 AM | Barbara Hansen (Univ. of Maryland) Metabolic syndrome: What is it and why would we want to treat it? |
9:30 AM - 9:40 AM | Discussion |
9:40 AM - 10:10 AM | John Bondo Hansen (Novo Nordisk) Beta cell rest, a new strategy for preservation of beta cell function. Synthesis and characterization of activators of the Katp channel |
10:10 AM - 10:20 AM | Discussion |
10:20 AM - 10:50 AM | Photograph and Break |
10:50 AM - 11:20 AM | Soumya Sahoo (Merck) Identification of potent, orally active PPARalpha/gamma dual agonists and beyond |
11:20 AM - 11:30 AM | Discussion |
11:30 AM - 12:00 PM | Dan Sternbach (GSK) New PPAR Ligands: Chemistry and Biology |
12:00 PM - 12:10 PM | Discussion |
12:30 PM | Lunch |
1:30 PM - 6:00 PM | FREE TIME (organized Mt. Kearsearge hike available) |
6:00 PM | Dinner |
| Antivirals |
| Discussion Leader: Ron Griffith (Genelabs) |
7:30 PM - 8:00 PM | Michael Bos (Boehringer-Ingelheim) NS3 Serine Protease Inhibitors for the Treatment of HCV Infection |
8:00 PM - 8:10 | Discussion |
8:10 PM - 8:40 PM | Nicholas Meanwell (BMS) Discovery and Characterization of a Novel Inhibitor of HIV Entry |
8:40 PM - 8:50 PM | Discussion |
8:50 PM - 9:20 PM | Steven D. Young (Merck) Discovery and Antiviral Activity of a New Class of HIV Integrase Inhibitors |
9:20 PM - 9:30 PM | Discussion |
TUESDAY |
7:30 AM - 8:30 AM | Breakfast |
| Orally Active GPCR Antagonists |
| Discussion Leader: Lihu Yang (Merck) |
9:00 AM - 9:30 AM | Paul E. Finke (Merck) Cyclopentane Based Antagonists of the Human CCR5 Receptor as Anti-HIV Agents |
9:30 AM - 9:40 AM | Discussion |
9:40 AM - 10:10 AM | Mitsuru Shiraishi (Takeda) Orally Active CCR5 Antagonists as Anti-HIV-1 Agents |
10:10 AM - 10:20 AM | Discussion |
10:20 AM - 10:50 AM | Break |
10:50 AM - 11:20 AM | Gaetan H. Ladouceur (Bayer) Discovery of 5-Hydroxyalkyl-4-phenylpyridines as a New Class of Glucagon Receptor Antagonists |
11:20 AM - 11:30 AM | Discussion |
11:30 AM - 12:00 PM | Jesper Lau (Novo Nordisk) Discovery of Human Glucagon Receptor Antagonists for Treatment of Type2 Diabetes |
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 #1 Discussion Leader: Celia Dominguez (Amgen) |
6:00 PM | Dinner |
| Kinases |
| Discussion Leader: Rima Al-awar (Eli Lilly) |
7:30 PM - 8:00 PM | Sajan Joseph (Eli Lilly) Synthesis and Evaluation of Cyclin D1/cdk4 Inhibitors |
8:00 PM - 8:10 PM | Discussion |
8:10 PM - 8:40 PM | George Hartman (Merck) Novel KDR Kinase Inhibitors for Cancer- Potency, Pharmacokinetic, Pharmacodynamic, and Tumor Growth Inhibitory Considerations |
8:40 PM - 8:50 PM | Discussion |
8:50 PM - 9:20 PM | Philip Jewsbury (AstraZeneca) The exploitation of structural surrogates in molecular design: a CDK4 case study |
9:20 PM - 9:30 PM | Discussion |
WEDNESDAY |
7:30 AM - 8:30 AM | Breakfast |
| Histone Deacetylase Inhibitors: From Chromatin Remodeling To Experimental Therapeutics |
| Discussion Leader: Kristof Van Emelen (Johnson&Johnson) |
9:00 AM - 9:30 AM | Eric Verdin (The Gladstone Institute) Biology Of Histone Deacetylases: New Targets For Cancer Therapy |
9:30 AM - 9:40 AM | Discussion |
9:40 AM - 10:10 AM | Ronald Breslow (University of Columbia) HDAC inhibitors |
10:10 AM - 10:20 AM | Discussion |
10:20 AM - 10:50 AM | Election of Vice-Chair Elect and Break |
10:50 AM -11:20 AM | Daniel Delorme (Methylgene) Sulfonamide Hydroxamic Acids, A Novel Class Of Histone Deacetylase Inhibitors, Are Antiproliferative Against Human Cancer Cells |
11:20 AM - 11:30 AM | Discussion |
11:30 AM - 12:00 PM | Stacy Remiszewski (Novartis) Discovery of NVP-LAQ824, a Novel Histone Deacetylase Inhibitor with In Vitro and In Vivo Antitumor Activity |
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 #2 Discussion Leader: Celia Dominguez (Amgen) |
6:00 PM | Dinner |
| Soluble Receptors |
| Discussion Leader: Brad Morgan (Pfizer) |
7:30 PM - 8:00 PM | Tim Willson (GSK) Chemical and Structural Genomics of Orphan Nuclear Receptors |
8:00 PM - 8:10 PM | Discussion |
8:10 PM - 8:40 PM | Phil Kym (Abbott) Discovery of a Novel Class of Nonsteroidal, Selective Glucocorticoid Receptor Modulators |
8:40 PM - 8:50 PM | Discussion |
8:50 PM - 9:20 PM | Richard Chesworth (Pfizer) The Discovery of Novel Estrogen Receptor-beta Selective Agonists |
9:20 PM - 9:30 PM | Discussion |
THURSDAY |
7:30 AM - 8:30 AM | Breakfast |
| Special Topics |
| Discussion Leader: Paul Ornstein (Lilly) |
9:00 AM - 9:30 AM | Natesan Murugesan (BMS) Discovery of Potent Dual angiotensin II and Endothelin A Receptor Antagonists |
9:30 AM - 9:40 AM | Discussion |
9:40 AM - 10:10 AM | Klaus Rudolf (Boehringer Ingelheim) The Discovery of BIBN4096, a Novel CGRP Antagonist for the Treatment of Migraine |
10:10 AM - 10:20 AM | Discussion |
10:20 AM - 10:50 AM | Break |
10:50 AM -11:20 AM | Dennis Zimmerman (Lilly) The discovery and development of arylalkylsulfonamides AMPA receptor potentiators for the treatment of cognition and other major CNS disorders |
11:20 AM - 11:30 AM | Discussion |
11:30 AM - 12:00 PM | Alan Stobie (Pfizer) Glycine site NMDA receptor antagonists in the treatment of Stroke - idea to proof of concept |
12:00 PM - 12:10 PM | Discussion |
12:30 PM | Lunch |
5:00 PM - 6:00 PM | Chairman's Social/Mixer |
6:00 PM | Dinner |
| Chair's Talk |
| Discussion Leader: John Macor, Chair (BMS) |
7:30 PM - 9:30 PM | Barry Werth, author of "The Billion-Dollar Molecule" |
9:20 PM - 9:30 PM | Discussion |
FRIDAY |
7:30 AM - 8:30 AM | Breakfast |
9:00 AM | Bus Departs for Logan Airport |