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Medicinal Chemistry
Gordon Research Conference

Recent Advances in Drug Discovery: Pathways, Targets and Molecules

Dates

August 2-7, 2015

Location

Colby-Sawyer College
New London, NH

Organizers

Chair:
Lori K. Gavrin

Vice Chair:
Bradley Tait

Meeting Description

The 2015 Medicinal Chemistry Gordon Research Conference will feature talks on the cutting edge of the discipline that include new compounds, targets and technologies that advance the science. Bradley Tait of Proteostasis is putting together the scientific program; please review the 2014 program to see examples of the kinds of topics typically covered at this conference. In addition to the general scientific sessions the conference will culminate with a Special Topics Session organized by Sabine Hadida of Vertex. This session is comprised of 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, 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 Carolyn Dzierba of Bristol Myers Squibb.

The 2015 Medicinal Chemistry GRC will continue a tradition of outstanding science presented in a relaxed atmosphere offering a variety of social activities. Vice-Chair Elect Matthew Marx of Marx Pharma Consulting will organize social events for the week, including a hike of Mt. Kearsarge, softball, soccer, kayaking and a golf tournament. Please contact Matt with any questions regarding these activities.

As we look forward to another outstanding conference in 2015, 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 2015 Medicinal Chemistry GRC.

Lori Gavrin
GlaxoSmithKline
Chair, 2015 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 pmKinase Targets for CNS Disorders
Discussion Leader: Brock Shireman (Janssen R&D, USA)
7:40 pm - 8:10 pmCarolyn 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 pmDiscussion
8:20 pm - 8:50 pmMichael 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 pmDiscussion
8:55 pm - 9:25 pmTravis Wager (Pfizer Pharmaceuticals, USA)
"Treatment of Circadian Rhythm Disorders: Selective Casein Kinase (CK1δ/ε) Inhibitors"
9:25 pm - 9:30 pmDiscussion
9:30 pm Poster Session
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmChallenges and Successes Targeting Rheumatoid Arthritis
Discussion Leader: Janeta Popovici-Muller (Agios Pharmaceuticals, USA)
9:00 am - 9:30 amMark Sabat (Takeda Pharmaceuticals, USA)
"Cinnoline Inhibitors of BTK"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amStefan 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 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amBrian 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 amDiscussion
11:45 am - 12:15 pmAlan 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 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 Oncology
Discussion Leader: Peter Dragovich (Genentech, USA)
7:30 pm - 8:00 pmBarry 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 pmDiscussion
8:10 pm - 8:40 pmChris De Savi (AstraZeneca Pharmaceuticals, USA)
"Discovery of AZD9496: An Oral, Selective Estrogen Receptor Down-Regulator (SERD)"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmAlessandro 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 pmDiscussion
Tuesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmIon Channel Drug Discovery for Cardiovascular and Pain
Discussion Leader: Sharan Bagal (Pfizer Pharmaceuticals, United Kingdom)
9:00 am - 9:30 amJeff 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 amDiscussion
9:45 am - 10:15 amAlexander 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 amDiscussion
10:30 am - 11:00 amGroup Photo / Coffee Break
11:00 am - 11:30 amPatrick Stoy (GlaxoSmithKline, USA)
"Discovery and Optimization of Spirocarbamate TRPV4 Antagonists"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmBrian Marron (Pfizer Pharmaceuticals, USA)
"Discovery of PF-05089771: The First in Class Selective Nav1.7 Inhibitor"
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 the Treatment of Schizophrenia
Discussion Leader: James Barrow (Johns Hopkins School of Medicine, USA)
7:30 pm - 8:00 pmCarol Tamminga (University of Texas Southwestern Medical Center, USA)
"New Drug Treatments for Psychosis"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmMatthew Volgraf (Genentech, USA)
"Discovery of Highly Potent, Selective and Brain-Penetrant GluN2A NMDA Receptor Positive Allosteric Modulators (PAMs)"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmGiles Brown (Heptares Therapeutics, United Kingdom)
"Discovery and Optimization of Selective Muscarinic Agonists"
9:20 pm - 9:30 pmDiscussion
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmAdvances in Antibiotic Research: Porins, Natural Products and Boron Based Inhibitors
Discussion Leader: Blaise Lippa (Morphic Rock Therapeutic, USA)
9:00 am - 9:30 amRuben Tommasi (Entasis Therapeutics, USA)
"Addressing the Enigma of Antibacterial Drug Discovery"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amDavid Sherman (Life Sciences Institute, USA)
"Engineering Biocatalysis for Creation of Novel Antibiotics"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amJef De Brabander (University of Texas Southwestern Medical Center, USA)
"A Novel Antibiotic for Gram-Negative Pathogens"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmScott Hecker (Rempex Pharmaceuticals, Inc. / The Medicines Company, USA)
"RPX7009 – A Novel Boronate β-Lactamase Inhibitor"
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 pmUbiquitin Proteasome System: Untapped Source of New Therapeutic Opportunities
Discussion Leader: Shelli McAlpine (University of New South Wales, Australia)
7:30 pm - 8:00 pmJoseph Weinstock (Progenra Inc., USA)
"Selective De-Ubiquitylase Inhibitors for Cancer Immunotherapy"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmDavid 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 pmDiscussion
8:50 pm - 9:20 pmJeff 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 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: Sabine Hadida (Vertex Pharmaceuticals, USA)
9:00 am - 9:30 amJeremy Travins (Agios Pharmaceuticals, USA)
"AG-221 – The First Clinical Inhibitor of IDH2 Mutant Enzymes in Acute Myelogenous Leukemia"
9:30 am - 9:45 amDiscussion
9:45 am - 10:15 amTim Miles (GlaxoSmithKline, Spain)
"A Fully Integrated Partnership Performing Drug Discovery Toward Visceral Leishmaniasis"
10:15 am - 10:30 amDiscussion
10:30 am - 11:00 amCoffee Break
11:00 am - 11:30 amAlan Brown (Pfizer Neusentis, United Kingdom)
"Discovery of Potent and Highly Selective NaV1.8 Inhibitors as Potential Pain Therapeutics"
11:30 am - 11:45 amDiscussion
11:45 am - 12:15 pmGerry Harriman (Nimbus Therapeutics, USA)
"ND-630, an Allosteric Inhibitor of Acetyl Co-A Carboxylase for the Treatment of NASH"
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: New Approaches in Discovery Science and New Challenges for the Biopharmaceutical Industry
Discussion Leader: Lori Gavrin (GlaxoSmithKline, United Kingdom)
7:30 pm - 8:10 pmJohn LaMattina (PureTech, USA)
"New Approaches in Discovery Science and New Challenges for the Biopharmaceutical Industry"
8:10 pm - 8:30 pmDiscussion
8:30 pm - 9:20 pmGeneral Discussion
9:20 pm - 9:30 pmClosing Remarks
Friday
7:30 am - 8:30 amBreakfast
9:00 amDeparture
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