SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in (Office Closed 6:00 pm - 7:00 pm) |
6:00 pm | Dinner |
7:30 pm - 7:45 pm | Welcome / Introductory Comments by GRC Site Staff |
7:45 pm - 9:30 pm | Rule-Breaker Compounds |
| Discussion Leader: Carl Decicco (BMS) |
7:45 pm - 8:15 pm | Percy Carter (BMS)
"Millamolecular Chemistry"
|
8:15 pm - 8:20 pm | Discussion |
8:20 pm - 8:50 pm | Hiroaki Suga (University of Tokyo)
"Non-Traditional Peptide Therapeutic Leads"
|
8:50 pm - 8:55 pm | Discussion |
8:55 pm - 9:25 pm | Julio Camararo (USC)
"Cyclotides"
|
9:25 pm - 9:30 pm | Discussion |
9:30 pm - 11:00 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: Simon Haydar (Eli Lilly)
|
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Covalent Drugs |
| Discussion Leader: Mark Noe (Pfizer) |
9:00 am - 9:30 am | Russell Petter (Celgene)
"Specific Silencing of PI3K Alpha With a Targeted Covalent Inhibitor"
|
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Jack Taunton (UCSF)
"Cysteine-Targeted Inhibitors of P90 Ribosomal S6 Kinase"
|
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:20 am | Wei Chen (Pharmacyclics)
"Discovery and Development of Irreversible BTK Inhibitors: Pharmacyclics' Approach"
|
11:20 am - 11:30 am | Discussion |
11:30 am - 12:00 pm | Amy Dounay (Pfizer)
"Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia"
|
12:00 pm - 12:10 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 | Cardiovascular Drugs |
| Discussion Leader: Andrew Stamford (Merck) |
7:30 pm - 8:00 pm | Julien Papillon (Novartis)
"Therapeutic Inhibition of CYP450s: the Discovery of Orally Available Aldosterone Synthase Inhibitors"
|
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Sven Ruf (Sanofi)
"Development of Cathepsin A Inhibitors for the Treatment of Heart Failure"
|
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Scott Priestley (BMS)
"Discovery of Orally Bioavailable Macrocyclic FViia Inhibitors"
|
9:20 pm - 9:30 pm | Discussion |
9:30 pm - 11:00 pm | Poster Session (Group B) / Social Hour |
| Discussion Leader: Simon Haydar (Eli Lilly) |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
8:45 am - 9:00 am | Business Meeting (Part 1) |
| Nominations for Chair of the 2013 Meeting by the Nominating Committee
|
9:00 am - 12:30 pm | Metabolic Cancer Targets |
| Discussion Leader: Janeta Popovici-Muller (Agios Pharmaceuticals) |
9:00 am - 9:30 am | Matthew Vander Heiden (Koch Institute, MIT)
"Understanding How Metabolism Impacts Cell Proliferation"
|
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Scott Biller (Agios)
"Discovery of IDH Inhibitors"
|
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Group Photo / Coffee Break |
10:50 am - 11:20 am | Cindy Parrish (GSK)
"Pulling a FAS One on Cancer: Discovery and Characterization of Fatty Acid Synthase Inhibitors"
|
11:20 am - 11:30 am | Discussion |
11:30 am - 12:00 pm | Richard Ward (AstraZeneca)
"Discovery of Novel LDHA Inhibitors Using Fragment-Based Lead Generation"
|
12:00 pm - 12:10 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (softball, soccer, and hiking activities available) |
5:00 pm - 6:00 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: Simon Haydar (Eli Lilly) |
6:00 pm | Dinner |
7:15 pm - 7:30 pm | Business Meeting (Part 2) |
| Candidate speeches; Announcement of Poster Awards |
7:30 pm - 9:30 pm | Challenges and Successes in Diabetes Discovery |
| Discussion Leader: Scott Edmondson (Merck) |
7:30 pm - 8:00 pm | William Hagmann (Merck)
"Somatostatin Antagonists: A Potential Treatment for Type 2 Diabetes"
|
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Phil Hipskind (Eli Lilly)
"Glucagon Receptor Antagonists: From the Laboratory to the Patient"
|
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Benjamin Stevens (Pfizer)
"Approaching a Rule-of-Five Compliant Small Molecule Glucagon Receptor Antagonist: A Year From Discovery to FIH"
|
9:20 pm - 9:30 pm | Discussion |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
8:45 am - 9:00 am | Business Meeting (Part 3) |
| Election of Chair for the 2015 Meeting
|
9:00 am - 12:30 pm | Epigenetics |
| Discussion Leader: Silvana Leit (Galenea) |
9:00 am - 9:30 am | Manfred Jung (Albert-Ludwigs-Universität)
"Chemical Epigenetics - Editing the Bookmarks in the Book of Life"
|
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Brian Albrecht (Constellation Pharmaceuticals)
"Inhibition of BET Bromodomains for the Treatment of Cancer" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:00 am | Poster Awards 1 & 2: Oral Summaries |
11:00 am - 11:30 am | John Tatlock (Pfizer)
"Discovery and Optimization of Novel SETD7 Inhibitors"
|
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Chun-wa Chung (GSK)
"First in Class BET Inhibitors"
|
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Organized Vice-Chair Elect Golf Scramble available) |
5:00 pm - 6:00 pm | Poster Session (Group B) / Social Hour |
| Discussion Leader: Simon Haydar (Eli Lilly) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Allosteric Drugs |
| Discussion Leader: Peter Bernstein (PhaRmaB, LLC) |
7:30 pm - 8:00 pm | Jeffrey Conn (Vanderbilt)
"Allosteric Modulators of GPCRs for Treatment of CNS Disorders"
|
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Chantal Alcouffe (Sanofi)
"SSR128129, an Allosteric Modulator of FGF-Rs"
|
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Scott Kuduk (Merck)
"Evolution of Quinolizidinone M1 Receptor Selective Positive Allosteric Modulators"
|
9:20 pm - 9:30 pm | Discussion |
THURSDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting (Part 4) |
| Evaluation Forms; Site Selection & Scheduling For Future Conferences |
9:00 am - 12:30 pm | Late - Breaker Session |
| Discussion Leader: Jean-Christophe Harmange (Constellation Pharmaceuticals) |
9:00 am - 9:30 am | Dustin Mergott (Lilly)
"Central Inhibition of Beta-Secretase in Humans with LY2811376 and LY2886721"
|
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Kim Cameron (Pfizer)
"Design and Development of Ghrelin Inverse Agonists for the Treatment of Diabetes"
|
10:10 am - 10:20 am | Discussion |
10:20 am - 10:55 am | Coffee Break |
10:55 am - 11:00 am | Poster Award #3: Oral Summary |
10:50 am - 11:30 am | John Hynes (BMS)
"Discovery of a CCR1 Antagonist for the Treatment of Rheumatoid Arthritis"
|
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Tesfaye Biftu (Merck)
"MK-3102: A Novel Once-Weekly DPP-4 Inhibitor for Type 2 Diabetes"
|
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 6:00 pm | Free Time |
6:00 pm | Dinner |
7:30 pm - 9:00 pm | Chair's Speaker |
| Discussion Leader: Amy Ripka (SAR Consulting) |
7:30 pm - 8:30 pm | John Martin (Gilead)
"Twenty-Five Years of Advances in Nucleotide Antiviral Research"
|
8:30 pm - 9:00 pm | Discussion |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |