Sunday |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | Kinase Targets for CNS Disorders |
| Discussion Leader: Brock Shireman (Janssen R&D, USA) |
7:40 pm - 8:10 pm | Carolyn Dzierba (Bristol-Myers Squibb Co., USA) "The Road from a Knock Out Mouse to a Novel Potential Treatment for Neuropathic Pain" |
8:10 pm - 8:20 pm | Discussion |
8:20 pm - 8:50 pm | Michael Siu (Genentech, USA) "Development of Potent, Selective, and Brain-Penetrant Dual Leucine Zipper Kinase (DLK) Small Molecule Inhibitors for the Treatment of Neurodegenerative Diseases" |
8:50 pm - 8:55 pm | Discussion |
8:55 pm - 9:25 pm | Travis Wager (Pfizer Pharmaceuticals, USA) "Treatment of Circadian Rhythm Disorders: Selective Casein Kinase (CK1δ/ε) Inhibitors" |
9:25 pm - 9:30 pm | Discussion |
9:30 pm |
Poster Session
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Monday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Challenges and Successes Targeting Rheumatoid Arthritis |
| Discussion Leader: Janeta Popovici-Muller (Agios Pharmaceuticals, USA) |
9:00 am - 9:30 am | Mark Sabat (Takeda Pharmaceuticals, USA) "Cinnoline Inhibitors of BTK" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Stefan Laufer (Eberhard-Karls University Tübingen, Germany) "Is Two Better than One? Dual p38 MAPK/PDE4 Inhibitors from Design to Serendipity to Phase I" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Brian Safina (Genentech, USA) "Discovery of Selective PI3Kδ Inhibitors Towards the Treatment of Rheumatoid Arthritis: Teasing Apart ON and OFF Target Toxicity In Vivo" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Alan Northrup (Merck & Co., Inc., USA) "Discovery of MK-8457: A Selective SYK/Zap70 Dual Inhibitor for Treatment of Rheumatoid Arthritis" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Advances in Oncology |
| Discussion Leader: Peter Dragovich (Genentech, USA) |
7:30 pm - 8:00 pm | Barry Toure (Novartis Institutes for BioMedical Research, USA) "MELK as a Valid Cancer Therapeutic Target? From Virtual Screening to Highly Selective Inhibitors Suitable for In Vivo Dosing" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Chris De Savi (AstraZeneca Pharmaceuticals, USA) "Discovery of AZD9496: An Oral, Selective Estrogen Receptor Down-Regulator (SERD)" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Alessandro Boezio (Amgen, USA) "Discovery of AMG 337, a Potent and Selective Inhibitor of c-Met with High Unbound Exposure and Robust, Extended In Vivo Antitumor Activity" |
9:20 pm - 9:30 pm | Discussion |
Tuesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Ion Channel Drug Discovery for Cardiovascular and Pain |
| Discussion Leader: Sharan Bagal (Pfizer Pharmaceuticals, United Kingdom) |
9:00 am - 9:30 am | Jeff Zablocki (Gilead Sciences, USA) "Discovery of GS-6615, a Potent, Selective Inhibitor of Cardiac Late Sodium Current for Cardiovascular Disease" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Alexander Pasternak (Merck & Co., Inc., USA) "Discovery and SAR Evolution of ROMK Inhibitor Sub-Classes Toward Identification of Our Clinical Development Compound" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Group Photo / Coffee Break |
11:00 am - 11:30 am | Patrick Stoy (GlaxoSmithKline, USA) "Discovery and Optimization of Spirocarbamate TRPV4 Antagonists" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Brian Marron (Pfizer Pharmaceuticals, USA) "Discovery of PF-05089771: The First in Class Selective Nav1.7 Inhibitor" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Advances in the Treatment of Schizophrenia |
| Discussion Leader: James Barrow (Johns Hopkins School of Medicine, USA) |
7:30 pm - 8:00 pm | Carol Tamminga (University of Texas Southwestern Medical Center, USA) "New Drug Treatments for Psychosis" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Matthew Volgraf (Genentech, USA) "Discovery of Highly Potent, Selective and Brain-Penetrant GluN2A NMDA Receptor Positive Allosteric Modulators (PAMs)" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Giles Brown (Heptares Therapeutics, United Kingdom) "Discovery and Optimization of Selective Muscarinic Agonists" |
9:20 pm - 9:30 pm | Discussion |
Wednesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Advances in Antibiotic Research: Porins, Natural Products and Boron Based Inhibitors |
| Discussion Leader: Blaise Lippa (Morphic Rock Therapeutic, USA) |
9:00 am - 9:30 am | Ruben Tommasi (Entasis Therapeutics, USA) "Addressing the Enigma of Antibacterial Drug Discovery" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | David Sherman (Life Sciences Institute, USA) "Engineering Biocatalysis for Creation of Novel Antibiotics" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Jef De Brabander (University of Texas Southwestern Medical Center, USA) "A Novel Antibiotic for Gram-Negative Pathogens" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Scott Hecker (Rempex Pharmaceuticals, Inc. / The Medicines Company, USA) "RPX7009 – A Novel Boronate β-Lactamase Inhibitor" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Ubiquitin Proteasome System: Untapped Source of New Therapeutic Opportunities |
| Discussion Leader: Shelli McAlpine (University of New South Wales, Australia) |
7:30 pm - 8:00 pm | Joseph Weinstock (Progenra Inc., USA) "Selective De-Ubiquitylase Inhibitors for Cancer Immunotherapy" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | David Wustrow (Cleave Biosciences, USA) "The Discovery of CB-5083: A First-in-Class Inhibitor of the AAA+ ATPase p97 for the Treatment of Cancer" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Jeff Ciavarri (Takeda Pharmaceuticals, USA) "Discovery of MLN7243: An Investigational First-in-Class Inhibitor of the Ubiquitin Activating Enzyme for the Treatment of Cancer" |
9:20 pm - 9:30 pm | Discussion |
Thursday |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting |
| Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair |
9:00 am - 12:30 pm | Late-Breaking Topics |
| Discussion Leader: Sabine Hadida (Vertex Pharmaceuticals, USA) |
9:00 am - 9:30 am | Jeremy Travins (Agios Pharmaceuticals, USA) "AG-221 – The First Clinical Inhibitor of IDH2 Mutant Enzymes in Acute Myelogenous Leukemia" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Tim Miles (GlaxoSmithKline, Spain) "A Fully Integrated Partnership Performing Drug Discovery Toward Visceral Leishmaniasis" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Alan Brown (Pfizer Neusentis, United Kingdom) "Discovery of Potent and Highly Selective NaV1.8 Inhibitors as Potential Pain Therapeutics" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Gerry Harriman (Nimbus Therapeutics, USA) "ND-630, an Allosteric Inhibitor of Acetyl Co-A Carboxylase for the Treatment of NASH" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Keynote Session: New Approaches in Discovery Science and New Challenges for the Biopharmaceutical Industry |
| Discussion Leader: Lori Gavrin (GlaxoSmithKline, United Kingdom) |
7:30 pm - 8:10 pm | John LaMattina (PureTech, USA) "New Approaches in Discovery Science and New Challenges for the Biopharmaceutical Industry" |
8:10 pm - 8:30 pm | Discussion |
8:30 pm - 9:20 pm | General Discussion |
9:20 pm - 9:30 pm | Closing Remarks |
Friday |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |