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 | Introductory Comments by GRC Site Staff / Welcome by Mary M. Mader, Conference Chair |
7:45 pm - 9:30 pm | RULE-BREAKER COMPOUNDS: EXPANDING THE DEFINITION OF DRUG-LIKE MOLECULES |
| Discussion Leader: Mark Murcko (Vertex Pharmaceuticals) |
7:45 pm - 8:10 pm | Mark L. Peterson (Tranzyme Pharma Inc)
"Discovery and Optimization within a Macrocyclic Peptidomimetic Scaffold: Ghrelin Agonists" |
8:10 pm - 8:20 pm | Discussion |
8:20 pm - 8:45 pm | Muthiah Manoharan (Alnylam Pharmaceuticals)
"Making drugs out of siRNA's" |
8:45 pm - 8:55 pm | Discussion |
8:55 pm - 9:20 pm | Gregory L. Verdine (Harvard University)
"Synthetic Biologics to tackle 'Undruggable' Targets" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 10:45 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: Maria Blanco (Eli Lilly) |
MONDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | TOWARDS NOVEL AGENTS FOR THE TREATMENT OF DIABETES |
| Discussion Leader: Thomas Aicher (Array Biopharma) |
9:00 am - 9:30 am | Michael J. Waring (Astra Zeneca)
"Optimization of Neutral Glucokinase Activators - The Discovery of AZD1092" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Jeffrey A. Pfefferkorn (Pfizer Global Research and Development)
"Developing Partial Activators of Glucokinase for Treating Type 2 Diabetes: Identification of PF-04937319 as an Early Development Candidate" |
10:10 am - 10:20 am | Discussion |
10:20 am - 11:00 am | Coffee Break / Group Photo |
11:00 am - 11:30 am | James Scott (Astra Zeneca)
"Small Molecule Inhibitors of 11-bHSD1 containing Acidic Functionality: The Discovery of AZD4017" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Angel Guzman-Perez (Pfizer Global Research and Development)
"The Identification of PF-04923503, a Selective Dual Acetyl-CoA Carboxylase-1 and 2 Inhibitor, as an Early Development Candidate for Diabetes" |
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 | INFECTIOUS DISEASES |
| Discussion Leader: Christian Hubschwerlen (Actelion Pharmaceuticals) |
7:30 pm - 8:00 pm | Franz von Nussbaum (Bayer Schering Pharma)
"Chemical Postevolution of Antibacterial Antibiotics - Synthesis beyond Biogenesis" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Neil D. Pearson (GlaxoSmithKline)
"Structure-based Lead Optimization of Novel Bacterial Type II Topoisomerase Inhibition" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Suzanne Stokes (AstraZeneca Pharmaceuticals)
"Discovery and Optimization of Inhibitors of Bacterial DNA Ligase, Antibacterial Activity Through a New Target" |
9:20 pm - 9:30 pm | Discussion |
9:45 pm - 10:45 pm | Poster Session (Group B) / Social Hour |
| Discussion Leader: Maria Blanco (Eli Lilly) |
TUESDAY |
7:30 am - 8:30 am | Breakfast |
8:45 am - 9:00 am | Business Meeting, Part 1 |
| (Nominations for Chair of 2013 Meeting by Nominating Committee) |
9:00 am - 12:30 pm | TARGETING THE ENDOCANNABINOID SYSTEM |
| Discussion Leader: Rob Jones (Arena Pharmaceuticals) |
9:00 am - 9:30 am | Christopher Walpole (Astra Zeneca)
"Orally available, peripherally restricted CB1 agonists with potential as novel analgesics with reduced liabilities versus classical cannabinoids" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Doris Riether (Boehringer Ingelheim)
"Optimization of selective CB2 receptor agonists" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break |
11:00 am - 11:30 am | Kay Ahn (Pfizer)
"Discovery of Highly Selective Fatty Acid Amide Hydrolase (FAAH) Inhibitors for the Treatment of Inflammatory Pain" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Michael Dart (Abbott Laboratories)
"Identification of Potent, Selective, Orally Efficacious Cannabinoid CB2 Receptor Agonists for Pain Management" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Optional activities include Softball or Soccer) |
5:00 pm - 6:00 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: Maria Blanco (Eli Lilly) |
6:00 pm | Dinner |
7:15 pm - 7:30 pm | Business Meeting, Part 2 |
| (Speeches by candidates for Chair of 2013 meeting; Announcement of poster awards) |
7:30 pm - 9:30 pm | PROSTAGLANDIN RECEPTOR MODULATORS |
| Discussion Leader: David Sandham (Novartis) |
7:30 pm - 8:00 pm | Brian Stearns (Amira)
"The discovery and optimization of a novel series of DP2 antagonists with efficacy in mouse models of COPD and asthma" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Stefano Crosignani (Merck-Serono)
"Discovery of Potent, Selective and Orally Bioavailable DP2 Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Mark Healy (formerly GlaxoSmithKline)
"Discovery of GSK726701: An EP4 Agonist for the Treatment of Inflammatory Pain" |
9:20 pm - 9:30 pm | Discussion |
WEDNESDAY |
7:30 am - 8:30 am | Breakfast |
8:50 am - 9:00 am | Business Meeting, Part 3 |
| (Election of Chair of 2013 meeting) |
9:00 am - 12:30 pm | TARGETING INFLAMMATION AND IMMUNOLOGICAL DISEASES |
| Discussion Leader: Katerina Leftheris (Vitae Pharmaceuticals) |
9:00 am - 9:30 am | J. Robert Merritt (Ligand Pharmaceuticals)
"A Novel Series of CCR1 Antagonists: From Library Hit to Preclinical Candidate" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Jürgen Wagner (Novartis Institute for Biomedical Research)
"Sotrastaurin: Oral and Specific Inhibitor of T cell Activation for the Prevention of Graft Rejection and the Treatment of Autoimmune Diseases" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break |
10:50 am - 11:00 am | Poster Awards 1 & 2: Oral Summaries |
11:00 am - 11:30 am | Joseph Kozlowski (Merck Research)
"TACE Inhibitors" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Chunjian Liu (BMS Research and Development)
"Discovery of BMS-582949, a Clinical p38 MAPK Inhibitor for the Treatment of Inflammatory Diseases" |
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: Maria Blanco (Eli Lilly) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | THIRD WORLD DISEASES |
| Discussion Leader: Richard Elliott (Bill and Melinda Gates Foundation) |
7:30 pm - 8:00 pm | Robert T. Jacobs (Scynexis)
"Discovery and Pre-Clinical Development of SCYX-7158 (AN 5568), a Novel Oxaborole-6-Carboxamide with Potential for Treatment of Stage 2 Human African Trypanosomiasis" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Jeremy Burrows (MMV)
"Antimalarial Medicinal Chemistry: challenges & opportunities" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Clifton Barry III (NIH)
"Antitubercular nitroimidazoles: structure-based approaches to optimization of a prodrug" |
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 |
| (Fill out Conference Evaluation Forms; Discuss future Site & Scheduling preferences) |
9:00 am - 12:30 pm | SPECIAL TOPICS / LATE BREAKING DEVELOPMENTS |
| Discussion Leader: Janeta Popovici-Muller (Agios Pharmaceuticals) |
9:00 am - 9:30 am | David Powell (Merck Frosst)
"Design of Liver-Targeted Stearoyl Coenzyme-A Desaturase Inhibitors for the Treatment of Diabetes" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Sabina Pecchi (Novartis)
"The Discovery of BKM120, a Pan Class I PI3 Kinase Inhibitor in Phase I/II Clinical Trials" |
10:10 am - 10:20 am | Discussion |
10:20 am | Coffee Break |
10:55 am - 11:00 am | Poster Award 3: Oral Summary |
11:00 am - 11:30 am | David Claremon (Vitae Pharmaceuticals)
"VTP-27999, An Orally Bioavailable Renin Inhibitor" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Charles Mowbray (Pfizer)
"The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist" |
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 - 9:30 pm | CHAIR'S SPEAKER |
| Discussion Leader: Mary Mader (Eli Lilly) |
7:30 pm - 8:15 pm | Paul A. Bartlett (University of California) |
8:15 pm - 8:45 pm | Discussion |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |