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 - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | NUCLEAR HORMONE RECEPTORS |
| Discussion Leader: Katerina Leftheris (Vitae Pharmaceuticals) |
7:40 pm - 8:05 pm | Ingrid Buchler (Pfizer)
"Dissociated Agonist of the Glucocorticoid Receptor (DAGR) a Super Anti-inflammatory" |
8:05 pm - 8:15 pm | Discussion |
8:15 pm - 8:40 pm | David Weinstein (Bristol-Myers Squibb)
"Discovery and Pharmacologic Evaluation of a Novel Series of Selective Glucocorticoid Receptor Modulators" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:15 pm | David Piotrowski (Pfizer)
"Non-Steroidal Mineralocorticoid Receptor Antagonists" |
9:15 pm - 9:30 pm | Discussion |
9:45 pm - 10:45 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: James Merritt (Kean University) |
MONDAY |
7:30 am - 8:30 am | Breakfast |
8:30 am | Group Photo |
9:00 am - 12:30 pm | RECENT DEVELOPMENTS OF TRANSIENT RECEPTOR POTENTIAL (TRP) CHANNELS |
| Discussion Leader: Maria J. Blanco (Eli Lilly and Company) |
9:00 am - 9:30 am | David Clapham (Harvard Medical School)
"Introduction to TRP Channels" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Andrew Griffin (AstraZeneca-Montreal)
"Discovery of AZD1386 - A TRPV1 Antagonist for the Treatment of Pain" |
10:10 am - 10:20 am | Discussion |
10:20 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Michael Kort (Abbott Laboratories)
"Discovery of Pharmacologically Differentiated TRPV1 Antagonists for the Treatment of Pain" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Mark R. Player (Johnson & Johnson)
"Benzimidazole containing Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists" |
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 | ACADEMICS IN DRUG DISCOVERY |
| Discussion Leader David Nugiel (Camden County College) |
7:30 pm - 8:00 pm | Barry Potter (University of Bath)
"Sulfatase Inhibitors: From Concept to Clinic" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Richard Silverman (Northwestern University)
"Inhibition of Protein Aggregation and the Development of Amyotrophic Lateral Sclerosis Therapeutics" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:10 pm | Jeffrey Kelly (The Scripps Research Institute)
"The Tafamidis Story - From Concept to First-in-Class Drug" |
9:10 pm - 9:20 pm | Discussion |
9:45 pm - 10:45 pm | Poster Session (Group B) / Social Hour |
| Discussion Leader: James Merritt (Kean University) |
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 | MODULATING PROTEIN FOLDING |
| Discussion Leader: Shelli R. McAlpine (University of New South Wales) |
9:00 am - 9:30 am | Paul Workman (The Institute of Cancer Research, Sutton, UK)
"Progress and Challenges with Molecular Chaperone Inhibitors: From Natural Products to Chemical Probes to Drugs in the Clinic" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Kraig Yager (Myrexis, Inc)
"The Discovery of MPC-3100" |
10:10 am - 10:20 am | Discussion |
10:20 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Tim Machajewski (Novartis)
"Discovery of NVP-HSP990, A Potent Oral Inhibitor of Hsp90 in Phase I Clinical Trials" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Marco Biamonte (Drug Discovery for Tropical Diseases)
"The Discovery of BIIB028" |
12:10 pm - 12:20 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 5:00 pm | Free Time (Softball or Soccer activities available) |
5:00 pm - 6:00 pm | Poster Session (Group A) / Social Hour |
| Discussion Leader: James Merritt (Kean University) |
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 | IMAGING IN DRUG DISCOVERY AND DEVELOPMENT |
| Discussion Leader: Sue Stokes (AstraZeneca) |
7:30 pm - 8:00 pm | Tobias Ritter (Harvard University)
"Late-Stage Fluorination to Enable PET Imaging" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Sally-Ann Ricketts (AstraZeneca)
"Preclinical and Translational Imaging in Drug Discovery" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Mac Johnson (Vertex Pharmaceuticals)
"Hyperpolarized Noble Gas MRI: An Emerging Tool for Drug Trials" |
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 | PHOSPHATASES IN DRUG DISCOVERY |
| Discussion Leader: Lori Gavrin (Pfizer) |
9:00 am - 9:30 am | Michel Tremblay (McGill University)
"Targeting Protein Tyrosine Phosphatases (PTP): A diversity of biomedical applications" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Zhong-Yin Zhang (Indiana University School of Medicine)
"Drugging the Undruggable: Targeting Protein Tyrosine Phosphatases for Therapeutic Development" |
10:10 am - 10:20 am | Discussion |
10:20 am - 10:50 am | Coffee Break |
10:50 am - 11:00 am | Poster Award 1 and 2: oral summary |
11:00 am - 11:30 am | Andrew Combs (Incyte)
"PTP1B Inhibitors: New Leads for a Challenging Drug Target via Structure-Based Drug Design Methods" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | Samuel Gerritz (Bristol-Myers Squibb)
"PTPgamma Ligands that Inhibit Phosphatase Activity via Perturbation of the WPD-Loop" |
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: James Merritt (Kean University) |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | APPROACHES TOWARDS IMPROVING MEMORY AND COGNITION |
| Discussion Leader: Alan P. Kaplan (Helicon Therapeutics, Inc.) |
7:30 pm - 8:00 pm | Michele Heffernan (Sunovion Pharmaceuticals, Inc.)
"D-Amino Acid Oxidase Inhibitors: From Discovery to the Clinic" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Gerhard Koenig (EnVivo Pharmaceuticals)
"EVP-6124: An Alpha-7 Nicotinic Receptor Agonist for Treating the Cognitive Defects in Alzheimer's Disease and Schizophrenia" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Michael Brodney (Pfizer Global Research and Development)
"5HT4 Partial Agonists to Improve Cognitive Dysfunction in Alzheimer's Disease" |
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: David Rotella (Montclair University) |
9:00 am - 9:30 am | Christopher J. O'Donnell (Pfizer)
"PF-4958242: A Novel AMPA Positive Allosteric Modulator (PAM) for the Treatment of Cognitive Deficits Associated with Schizophrenia (CIAS)" |
9:30 am - 9:40 am | Discussion |
9:40 am - 10:10 am | Christian Harcken (Boehringer Ingelheim)
"Preclinical and Clinical Profile of a Selective Glucocorticoid Receptor Agonist" |
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 |
11:00 am - 11:30 am | Robert Chorvat (Jenrin Discovery)
"Synthesis, Structure Activity Relationships and Pharmacology of CB1 Receptor Blockers as Metabolic Disorder Therapeutics Devoid of CNS Liabilities" |
11:30 am - 11:40 am | Discussion |
11:40 am - 12:10 pm | John Link (Gilead)
"GS-5885: An NS5A Inhibitor with Potent Antiviral Activity in HCV Infected Patients" |
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: Francesco G. Salituro (Agios Pharmaceuticals) |
7:30 pm - 8:30 pm | Mark Levin (Third Rock Ventures) |
8:30 pm - 9:00 pm | Discussion |
FRIDAY |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |