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Medicinal Chemistry
Gordon Research Conference

Innovations in Small Molecule Drug Discovery in Oncology, Neglected Diseases, Immunology, Parkinson's Disease, Fibrosis, First Disclosure Clinical Candidates, and New Drug Discovery Technologies

Dates

August 7-12, 2016

Location

Colby-Sawyer College
New London, NH

Organizers

Chair:
Bradley Tait

Vice Chair:
Matthew Marx

Meeting Description

The 2016 Medicinal Chemistry Gordon Research Conference will feature talks on the cutting edge of the discipline that include the first disclosure of clinical compounds, targets and technologies that advance the science. Matthew Marx of Mirati Therapeutics is putting together the scientific program; please see below the sessions that are currently being developed and contact Matt if you have any suggestions as these sessions evolve toward the publication of the preliminary program in December. The scientific program will culminate with a "Late-Breaking Topics" session organized by Brock Shireman of Janssen. 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 as 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 Jim Barrow of Johns Hopkins University.

The 2016 Medicinal Chemistry GRC will continue a tradition of outstanding science presented in a relaxed interactive atmosphere offering a variety of social activities. Vice-Chair Elect Carolyn Dzierba of Bristol-Myers Squibb will organize social events for the week, including hiking, softball, soccer, yoga, biking, running, frisbee golf, and a golf tournament. Please contact Carolyn with any questions regarding these activities.

As we look forward to another outstanding conference in 2016, 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 2016 Medicinal Chemistry GRC.

Brad Tait
Brad Tait Enterprise LLC
Chair, 2016 GRC on Medicinal Chemistry

Related Meeting

This GRC was held in conjunction with the "Medicinal Chemistry" Gordon Research Seminar (GRS). Refer to the associated GRS program page for more information.

Contributors

Final 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 pmSmall Molecule Anti-Fibrotics
Discussion Leader: Jehrod Brenneman (Boehringer-Ingelheim Pharmaceuticals Inc., USA)
7:40 pm - 8:10 pmLara Kallander (GlaxoSmithKline, USA)
"BMP1/TLL1/TLL2 Inhibitors for Treating Fibrotic Disease"
8:10 pm - 8:15 pmDiscussion
8:15 pm - 8:45 pmTom Heightman (Astex Pharmaceuticals, United Kingdom)
"Highly Potent Cell-Penetrant Inhibitors of the KEAP1-NRF2 Protein-Protein Interaction via X-Ray Fragment Screening"
8:45 pm - 8:55 pmDiscussion
8:55 pm - 9:25 pmSabine Hadida (Vertex Pharmaceuticals, Inc., USA)
"The Discovery of CFTR Modulators for the Treatment of Cystic Fibrosis"
9:25 pm - 9:30 pmDiscussion
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmNeglected Tropical Diseases
Discussion Leader: Cindy Parrish (GlaxoSmithKline, USA)
9:00 am - 9:30 amChristopher B. Cooper (TB Alliance, USA)
"Antitubercular 3-(4-Aminophenyl)Oxazolidin-2-Ones: Progress Towards Better, Safer TB Agents"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amIsabel Castellote Alvaro (GlaxoSmithKline, Spain)
"Antimalarial Pyrazines: A Long and Winding Road from a Phenotypic Hit to a Pre-Clinical Candidate"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amStacie S. Canan (Celgene Global Health, USA)
"Design of Compounds for Animal African Trypanosomosis (AAT): From Parasite Screen to Target Animal Model"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmValentina Molteni (Genomics Institute of the Novartis Research Foundation, USA)
"Pan-Kinetoplastid Growth Inhibitors: Towards One Treatment for Multiple Diseases"
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 pmEnabling New Technologies in Medicinal Chemistry
Discussion Leader: Matthew Bourbeau (Amgen, USA)
7:30 pm - 8:00 pmJeffrey Dodge (Eli Lilly and Company, USA)
"HDX: Structure-Based Drug Design Without Crystallography"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmWoody Sherman (Schrodinger, USA)
"Next Generation Free Energy Calculations in Drug Discovery"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmIan Churcher (GlaxoSmithKline Medicines Research Centre, United Kingdom)
"Medicinal Chemistry Beyond Small Molecule Inhibition: New Possibilities Through Induced Intracellular Protein Degradation"
9:20 pm - 9:30 pmDiscussion
Tuesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmExciting Advances Toward New Treatments for Autoimmune Disorders
Discussion Leader: Dustin Mergott (Eli Lilly and Company, USA)
9:00 am - 9:30 amMichelle Machacek (Merck & Co., USA)
"Strategies for the Design of Inhaled Kinase Inhibitors: Discovery of MK-8351, an Inhaled Spleen Tyrosine Kinase (SYK) Inhibitor for the Treatment of Asthma"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amSteve Staben (Genentech, Inc., USA)
"Inhibition of NF-κB-Inducing Kinase (NIK)"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amGroup Photo / Coffee Break
11:00 am - 11:30 amPeter Toogood (Lycera, USA)
"Modulation of the Mitochondrial ATPase for the Treatment of Inflammatory Bowel Disease"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmAtli Thorarensen (Pfizer, USA)
"Design of a JAK3-Specific Inhibitor Allowing for the Interrogation of JAK3 Signaling in Humans"
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 pmAdvances in Lead Generation
Discussion Leader: Joerg Holenz (AstraZeneca, USA)
7:30 pm - 8:00 pmFranz Von Nussbaum (Bayer SAS, France)
"Driving Tumors into a Mitotic Catastrophe - Lead Generation of Mps1 Inhibitors Leading to Two Clinical Candidates: BAY1161909 and BAY1217389"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmErin DiMauro (Amgen, USA)
"Discovery of Efficient, Selective, CNS-Penetrant Leads for Glycine Receptor Potentiation"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmKatherine Lee (Pfizer, USA)
"Lead Generation Strategies: Discovery of a Potent, Selective and Lipophilic Efficient IRAK4 Inhibitor, a Clinical Candidate from Fragment-Based Drug Design"
9:20 pm - 9:30 pmDiscussion
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmApproaches to the Treatment of Parkinson's Disease
Discussion Leader: Michael Ellis (Merck Research Laboratories, USA)
9:00 am - 9:30 amMarco Baptista (The Michael J. Fox Foundation for Parkinson's Research, USA)
"LRRK2 Kinase Inhibitors: The Path to the Clinic"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amYeon-Hee Lim (Merck Research Laboratories, USA)
"Discovery, SAR Evolution, and Clinical Evaluation of Adenosine A2A Antagonists for the Treatment of Parkinson's Disease"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amHolger Monenschein (Takeda California, USA)
"The Discovery of GPR6 as a Novel Target for the Treatment of Parkinson's Disease"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmJoerg Holenz (AstraZeneca, USA)
"Discovery of the Selective and Brain-Penetrant Irreversible Myeloperoxidase (MPO) Inhibitor AZD3241"
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 pmKinase Inhibitors in Oncology - Success Stories
Discussion Leader: Eugene Chekler (EMD Serono, USA)
7:30 pm - 8:00 pmKurt Pike (AstraZeneca, United Kingdom)
"Identifying High Quality, Potent and Selective Inhibitors of ATM Kinase: Discovery of AZD0156"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmJustin Ernst (eFFECTOR Therapeutics, USA)
"Identification of eFT508, an Oral, Potent and Highly Selective Inhibitor of Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 via a Disciplined, Iterative Structure-Based Drug Design Strategy"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmBayard Huck (EMD Serono, Germany)
"Identification of the Potent, Brain-Penetrant p70S6K/Akt Inhibitor M2698, a Novel Dual Inhibitor of the PI3K/Akt/mTOR Pathway"
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: Disclosures of Clinical Candidates
Discussion Leader: Brock Shireman (Janssen R&D, USA)
9:00 am - 9:30 amGregory Notte (Gilead Sciences, USA)
"Discovery of GS-4997, a Highly Selective Inhibitor of Apoptosis Signal-Regulating Kinase 1 (ASK1)"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amBrad Savall (Janssen Research & Development, USA)
"JNJ-54175446: A P2X7 Receptor Antagonist that Reduces IL-1β Levels for Major Depressive Disorders"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amDavid Weinstein (Bristol-Myers Squibb, USA)
"Discovery and Pre-Clinical Evaluation of a Novel Allosteric Inhibitor of TYK2"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmPhilip Harris (GlaxoSmithKline, USA)
"Identification of a First-in-Class RIP1 Kinase Inhibitor in Clinical Trials for Immuno-Inflammatory Diseases"
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: Embracing and Anticipating Change in a Dynamic Industry - View from One Medicinal Chemist
Discussion Leader: Bradley Tait (Brad Tait Enterprise LLC, USA)
7:30 pm - 8:30 pmKazumi Shiosaki (MPM Capital, USA)
"Embracing and Anticipating Change in a Dynamic Industry - View from One Medicinal Chemist"
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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