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Medicinal Chemistry
Gordon Research Conference

Highlighting Innovations and Technologies: First Disclosures of Programs and Approaches for Therapeutic Discovery

Dates

August 6-11, 2017

Location

Colby-Sawyer College
New London, NH Site Information

Organizers

Chair:
Matthew Marx

Vice Chair:
Carolyn D. Dzierba

Application Deadline

This meeting is currently oversubscribed (full). You may still submit an application. However, it will only be considered by the Conference Chair if more seats become available due to cancellations.

Meeting Description

The 2017 Medicinal Chemistry Gordon Research Conference will feature talks on the cutting edge of the discipline that include new innovations, technologies and compounds that advance the science. Carolyn Dzierba of Bristol-Myers Squibb is responsible for the scientific program; please see the planned topic areas below and contact the Chairs if you would like to submit a talk proposal. The program of speakers will be developed between August and November, 2016.

In addition to the general scientific sessions the conference will culminate with a Special Topics Session organized by Matt Bourbeau of Amgen. This session comprises late-breaking results on important clinical candidates across therapeutic areas. Finally, the conference will wrap up on Thursday evening with the Keynote address organized by the Chair.

We strongly encourage attendees to submit poster presentations on any aspect of Medicinal Chemistry as, historically, the poster sessions have been an essential outlet for thoughtful discussion and interaction among the conferees. This year, the poster sessions will be organized by Darby Schmidt of Quartet Medicine.

This conference is typically full by early May. We encourage application by April 1st and the submission of any poster abstracts by April 15th to facilitate the admissions process.

The 2017 Medicinal Chemistry GRC will continue a tradition of outstanding science presented in a relaxed atmosphere offering a variety of social activities. Vice-Chair Elect Robert Marquis of GSK will organize social events for the week, including a hike of Mt. Kearsarge, softball, soccer, kayaking and a golf tournament.

As we look forward to another outstanding conference in 2017, on behalf of myself, the Vice Chair and the Vice-Chair elect, we welcome your application and particularly encourage the application from those of diverse scientific backgrounds.

Thank you for your interest in the Medicinal Chemistry GRC.

Matt Marx
Mirati Therapeutics
Chair, 2017 Medicinal Chemistry GRC

Related Meeting

This GRC will be held in conjunction with the "Medicinal Chemistry" Gordon Research Seminar (GRS). Those interested in attending both meetings must submit an application for the GRS in addition to an application for the GRC. Refer to the associated GRS program page for more information.

Contributors

Meeting Program

Sunday
2:00 pm - 9:00 pmArrival and Check-in
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmAdvances in Small Molecule Immunomodulators
Discussion Leader: David Weinstein (Vividion Therapeutics, USA)
7:40 pm - 8:05 pmAlex Cortez (Genomics Institute of the Novartis Research Foundation, USA)
"Cancer Immunotherapy with a TLR7 Selective Agonist"
8:05 pm - 8:15 pmDiscussion
8:15 pm - 8:40 pmLynn 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 pmDiscussion
8:50 pm - 9:20 pmAlec Lebsack (Janssen R&D, USA)
"Efforts Toward Small Molecule Modulators of Tumor Necrosis Factor-Alpha (TNFα)"
9:20 pm - 9:30 pmDiscussion
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmNew Directions in Oncology
Discussion Leader: Cindy Parrish (GlaxoSmithKline, USA)
9:00 am - 9:30 amChristopher O'Donnell (Pfizer Inc, USA)
"Medicinal Chemistry Approaches to the Discovery of Clinically Active Antibody Drug Conjugates"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amFrederick Goldberg (AstraZeneca, United Kingdom)
"Pump Up the Volume: Optimisation of Acidic Monocarboxylate Transporter 4 (MCT4) Inhibitors for Oncology"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amThomas D. Aicher (Lycera Corp., USA)
"Targeting the RORγ Nuclear Receptor"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmEmily 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 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmChallenges and Novel Approaches to the Treatment of Epilepsy
Discussion Leader: Graeme Freestone (Dart NeuroScience, USA)
7:30 pm - 8:00 pmH. Steve White (University of Washington, USA)
"Treatment Refractory Epilepsy and the Need for More Efficacious Therapies"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmJamison Tuttle (Pfizer, USA)
"Identifying Brain Penetrant JAK Inhibitors to Attenuate Neuroinflammation Associated with Epilepsy"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmOlivier Bezencon (Idorsia Pharmaceuticals Ltd., Switzerland)
"T-Type Calcium Channel Blockers for the Treatment of Generalized Epilepsies"
9:20 pm - 9:30 pmDiscussion
Tuesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmRare Diseases / Genetically-Driven Diseases
Discussion Leader: Joshi Ramanjulu (GlaxoSmithKline, USA)
9:00 am - 9:30 amBrian 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 amDiscussion
9:45 am - 10:15 amPamela Haile (GlaxoSmithKline, USA)
"Targeting an Ultra-Rare Disease: Discovery of RIP2 Kinase Inhibitors for Blau Syndrome and Beyond"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amGroup Photo / Coffee Break
11:00 am - 11:30 amFlorence 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 amDiscussion
11:45 am - 12:15 pmJohan Oslob (MyoKardia, USA)
"Discovery of Sarcomere Modulator MYK-461 for Hypertrophic Cardiomyopathy"
12:15 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmRecent Developments in Covalent Drug Design
Discussion Leader: Matthew Volgraf (Genentech, Inc., USA)
7:30 pm - 8:00 pmJack Taunton (University of California, San Francisco, USA)
"Chemical Biology of Lysine-Targeted Covalent Probes"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmChristopher 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 pmDiscussion
8:50 pm - 9:20 pmChandra 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 pmDiscussion
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmTargeted Drug Delivery
Discussion Leader: Valentina Molteni (Genomics Institute of the Novartis Research Foundation, USA)
9:00 am - 9:30 amPhilip Low (Purdue University, USA)
"Principles in the Design of Ligand-Targeted Drugs: Examples from Drugs that Treat the Tumor Micro-Environment"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amMuthiah Manoharan (Alnylam Pharmaceuticals, USA)
"Targeted Delivery of RNAi Therapeutics"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amDawn George (AbbVie, USA)
"Colon-Restricted Delivery of Colony Stimulating Factor 1 Receptor (CSF1R) Inhibitors"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmKim Huard (Pfizer, USA)
"Improving the Safety Profile of ACC Inhibitors Through Liver Targeting"
12:15 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmOrganic Synthesis: Strategic Role in Accelerating Project Advancement
Discussion Leader: Christopher Helal (Pfizer, USA)
7:30 pm - 8:00 pmPaul Dransfield (Amgen, USA)
"Synthetic Strategies and Developments that Expedited Discovery of APJ Agonists for the Treatment of Heart Disease"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmAaron Wrobleski (Eli Lilly and Company, USA)
"Targeting Notch for Cancer Therapy: A Chemistry Perspective"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmAlex Hird (AstraZeneca, USA)
"Discovery and Synthesis of a Series of Potent Macrocyclic Inhibitors of MCL1 for Treatment of Cancer"
9:20 pm - 9:30 pmDiscussion
Thursday
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness 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 pmLate-Breaking Topics
Discussion Leader: Matthew Bourbeau (Amgen, USA)
9:00 am - 9:30 amPaul Scola (Bristol-Myers Squibb, USA)
"Discovery of a Macrocyclic Peptide Inhibitor of Programmed Death-Ligand 1 (PD-L1)"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amLesley 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 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amYoung Shin Cho (Novartis, USA)
"Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmJames Taylor (Gilead Sciences, USA)
"Discovery of Voxilaprevir, a Pangenotypic HCV Protease Inhibitor with Improved Coverage of Resistance Associated Variants"
12:15 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session
6:00 pmDinner
7:30 pm - 9:30 pmKeynote Session: A Perspective on Synthetic and Medicinal Chemistry
Discussion Leader: Matthew Marx (Mirati Therapeutics, USA)
7:30 pm - 8:30 pmPhil Baran (The Scripps Research Institute, USA)
"A Perspective on Synthetic and Medicinal Chemistry"
8:30 pm - 8:55 pmDiscussion
8:55 pm - 9:15 pmGeneral Discussion
9:15 pm - 9:30 pmClosing Remarks
Friday
7:30 am - 8:30 amBreakfast
9:00 amDeparture
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