Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Advances in Small
Molecule Immunomodulators
Discussion Leader: David Weinstein (Vividion Therapeutics, USA)
7:40 pm - 8:05 pm
Alex Cortez (Genomics Institute of the Novartis Research Foundation, USA)
"Cancer Immunotherapy with a TLR7 Selective Agonist"
8:05 pm - 8:15 pm
Discussion
8:15 pm - 8:40 pm
Lynn Hawkins (Eisai Andover Innovative Medicines (AiM) Institute, USA)
"E6742: A First in Class TLR7/8 Antagonist for the Treatment of SLE"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Alec Lebsack (Janssen R&D, USA)
"Efforts Toward Small Molecule Modulators of Tumor Necrosis Factor-Alpha (TNFα)"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
New
Directions in Oncology
Discussion Leader: Cindy Parrish (GlaxoSmithKline, USA)
9:00 am - 9:30 am
Christopher O'Donnell (Pfizer Inc, USA)
"Medicinal Chemistry Approaches to the Discovery of Clinically Active Antibody Drug Conjugates"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Frederick Goldberg (AstraZeneca, United Kingdom)
"Pump Up the Volume: Optimisation of Acidic Monocarboxylate Transporter 4 (MCT4) Inhibitors for Oncology"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Thomas D. Aicher (Lycera Corp., USA)
"Targeting the RORγ Nuclear Receptor"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Emily Hanan (Genentech, Inc., USA)
"Discovery of GDC-0077, a Highly Isoform Selective Inhibitor of PI3Kα that Promotes Selective Degradation of Mutant-p110α"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Challenges and Novel Approaches to the Treatment of Epilepsy
Discussion Leader: Graeme Freestone (Dart NeuroScience, USA)
7:30 pm - 8:00 pm
H. Steve White (University of Washington, USA)
"Treatment Refractory Epilepsy and the Need for More Efficacious Therapies"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Jamison Tuttle (Pfizer, USA)
"Identifying Brain Penetrant JAK Inhibitors to Attenuate Neuroinflammation Associated with Epilepsy"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Olivier Bezencon (Idorsia Pharmaceuticals Ltd., Switzerland)
"T-Type Calcium Channel Blockers for the Treatment of Generalized Epilepsies"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Rare Diseases / Genetically-Driven Diseases
Discussion Leader: Joshi Ramanjulu (GlaxoSmithKline, USA)
9:00 am - 9:30 am
Brian Hodous (Blueprint Medicines, USA)
"Discovery and Development of BLU-285: A Potent, Highly Selective Inhibitor of KIT and PDGFRa Activation Loop Mutants"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Pamela Haile (GlaxoSmithKline, USA)
"Targeting an Ultra-Rare Disease: Discovery of RIP2 Kinase Inhibitors for Blau Syndrome and Beyond"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
Florence Wagner (Broad Institute of MIT and Harvard, USA)
"Dissecting the Kinome One Carbon at a Time: Rational Design of Exquisitely Selective Inhibitors of the GSK3 Kinase Paralogs"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Johan Oslob (MyoKardia, USA)
"Discovery of Sarcomere Modulator MYK-461 for Hypertrophic Cardiomyopathy"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Recent Developments
in Covalent Drug Design
Discussion Leader: Matthew Volgraf (Genentech, Inc., USA)
7:30 pm - 8:00 pm
Jack Taunton (University of California, San Francisco, USA)
"Chemical Biology of Lysine-Targeted Covalent Probes"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Christopher Butler (Pfizer Global R&D, USA)
"Identification of Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Chandra Miduturu (Blueprint Medicines, USA)
"Discovery of BLU-554: A Potent and Highly Selective Covalent Inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4) for the Targeted Treatment of Advanced Hepatocellular Carcinoma (HCC)"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Targeted Drug Delivery
Discussion Leader: Valentina Molteni (Genomics Institute of the Novartis Research Foundation, USA)
9:00 am - 9:30 am
Philip Low (Purdue University, USA)
"Principles in the Design of Ligand-Targeted Drugs: Examples from Targeted Small Drugs and Immunotherapies"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
Muthiah Manoharan (Alnylam Pharmaceuticals, USA)
"Targeted Delivery of RNAi Therapeutics"
10:10 am - 10:25 am
Discussion
10:25 am - 10:45 am
Coffee Break
10:45 am - 11:15 am
Dawn George (AbbVie, USA)
"Colon-Restricted Delivery of Colony Stimulating Factor 1 Receptor (CSF1R) Inhibitors"
11:15 am - 11:30 am
Discussion
11:30 am - 12:00 pm
Kim Huard (Pfizer, USA)
"Improving the Safety Profile of ACC Inhibitors Through Liver Targeting"
12:00 pm - 12:15 pm
Discussion
12:15 pm - 12:30 pm
Poster Previews
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Organic Synthesis: Strategic Role in Accelerating Project Advancement
Discussion Leader: Christopher Helal (Pfizer, USA)
7:30 pm - 8:00 pm
Paul Dransfield (Amgen, USA)
"Synthetic Strategies and Developments that Expedited Discovery of APJ Agonists for the Treatment of Heart Disease"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Aaron Wrobleski (Eli Lilly and Company, USA)
"Targeting Notch for Cancer Therapy: A Chemistry Perspective"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Alex Hird (AstraZeneca, USA)
"Discovery and Synthesis of a Series of Potent Macrocyclic Inhibitors of MCL1 for 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: Matthew Bourbeau (Amgen, USA)
9:00 am - 9:30 am
Paul Scola (Bristol-Myers Squibb, USA)
"Discovery of a Macrocyclic Peptide Inhibitor of Programmed Death-Ligand 1 (PD-L1)"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Lesley Liu-Bujalski (EMD Serono Research & Development Institute, USA)
"Discovery of M2951, a Selective, Covalent Inhibitor of BTK for the Treatment of Autoimmune Diseases"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Young Shin Cho (Novartis, USA)
"Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
James Taylor (Gilead Sciences, USA)
"Discovery of Voxilaprevir, a Pangenotypic HCV Protease Inhibitor with Improved Coverage of Resistance Associated Variants"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: A Perspective on Synthetic and Medicinal Chemistry
Discussion Leader: Matthew Marx (Mirati Therapeutics, USA)
7:30 pm - 8:30 pm
Phil Baran (The Scripps Research Institute, USA)
"A Perspective on Synthetic and Medicinal Chemistry"
8:30 pm - 8:55 pm
Discussion
8:55 pm - 9:15 pm
General Discussion
9:15 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure