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Conference Program
 
Medicinal Chemistry
August 5-10, 2012
Colby-Sawyer College
New London, NH
Chair:
Amy Ripka

Vice Chair:
Mark A. Murcko

The 2012 Medicinal Chemistry Gordon Conference will feature talks on cutting edge drug discovery programs and new technologies which continue to advance the field. Mark Murcko of Disruptive Biomedical, LLC is putting together the 2012 scientific program; the 2011 program will provide examples of topics typically covered. We strongly encourage attendees to submit poster presentations as, historically, the poster sessions have been key to stimulating thoughtful discussion and interaction among the conferees. This year, the poster sessions will be organized by Simon Haydar. In addition to the general scientific sessions the conference will culminate with a Special Topics Session organized by J.C. Harmange. 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.

The 2012 Medicinal Chemistry GRC will continue a tradition of outstanding science presented in a relaxed atmosphere offering a variety of social activities. Vice-Chair Elect Dave Rotella of Montclair State University will organize social events for the week, including a hike of Mt. Kearsarge, softball, soccer, kayaking and the Vice-Chair Elect Golf Tournament. Please contact Dave with any questions regarding these activities.

As we look forward to another outstanding conference in 2012, 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 2012 Medicinal Chemistry GRC.

Amy Ripka
Chair, 2012 GRC on Medicinal Chemistry


Contributors

SUNDAY
2:00 pm - 9:00 pmArrival and Check-in (Office Closed 6:00 pm - 7:00 pm)
6:00 pmDinner
7:30 pm - 7:45 pmWelcome / Introductory Comments by GRC Site Staff
7:45 pm - 9:30 pmRule-Breaker Compounds
Discussion Leader: Carl Decicco (BMS)
7:45 pm - 8:15 pmPercy Carter (BMS)
"Millamolecular Chemistry"
8:15 pm - 8:20 pmDiscussion
8:20 pm - 8:50 pmHiroaki Suga (University of Tokyo)
"Non-Traditional Peptide Therapeutic Leads"
8:50 pm - 8:55 pmDiscussion
8:55 pm - 9:25 pmJulio Camararo (USC)
"Cyclotides"
9:25 pm - 9:30 pmDiscussion
9:30 pm - 11:00 pmPoster Session (Group A) / Social Hour
Discussion Leader: Simon Haydar (Eli Lilly)
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmCovalent Drugs
Discussion Leader: Mark Noe (Pfizer)
9:00 am - 9:30 amRussell Petter (Celgene)
"Specific Silencing of PI3K Alpha With a Targeted Covalent Inhibitor"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amJack Taunton (UCSF)
"Cysteine-Targeted Inhibitors of P90 Ribosomal S6 Kinase"
10:10 am - 10:20 amDiscussion
10:20 am - 10:50 amCoffee Break
10:50 am - 11:20 amWei Chen (Pharmacyclics)
"Discovery and Development of Irreversible BTK Inhibitors: Pharmacyclics' Approach"
11:20 am - 11:30 amDiscussion
11:30 am - 12:00 pmAmy Dounay (Pfizer)
"Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia"
12:00 pm - 12:10 pmDiscussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time (Organized Mt. Kearsarge hike available)
6:00 pmDinner
7:30 pm - 9:30 pmCardiovascular Drugs
Discussion Leader: Andrew Stamford (Merck)
7:30 pm - 8:00 pmJulien Papillon (Novartis)
"Therapeutic Inhibition of CYP450s: the Discovery of Orally Available Aldosterone Synthase Inhibitors"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmSven Ruf (Sanofi)
"Development of Cathepsin A Inhibitors for the Treatment of Heart Failure"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmScott Priestley (BMS)
"Discovery of Orally Bioavailable Macrocyclic FViia Inhibitors"
9:20 pm - 9:30 pmDiscussion
9:30 pm - 11:00 pmPoster Session (Group B) / Social Hour
Discussion Leader: Simon Haydar (Eli Lilly)
TUESDAY
7:30 am - 8:30 amBreakfast
8:45 am - 9:00 amBusiness Meeting (Part 1)
Nominations for Chair of the 2013 Meeting by the Nominating Committee
9:00 am - 12:30 pmMetabolic Cancer Targets
Discussion Leader: Janeta Popovici-Muller (Agios Pharmaceuticals)
9:00 am - 9:30 amMatthew Vander Heiden (Koch Institute, MIT)
"Understanding How Metabolism Impacts Cell Proliferation"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amScott Biller (Agios)
"Discovery of IDH Inhibitors"
10:10 am - 10:20 amDiscussion
10:20 am - 10:50 amGroup Photo / Coffee Break
10:50 am - 11:20 amCindy Parrish (GSK)
"Pulling a FAS One on Cancer: Discovery and Characterization of Fatty Acid Synthase Inhibitors"
11:20 am - 11:30 amDiscussion
11:30 am - 12:00 pmRichard Ward (AstraZeneca)
"Discovery of Novel LDHA Inhibitors Using Fragment-Based Lead Generation"
12:00 pm - 12:10 pmDiscussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time (softball, soccer, and hiking activities available)
5:00 pm - 6:00 pmPoster Session (Group A) / Social Hour
Discussion Leader: Simon Haydar (Eli Lilly)
6:00 pmDinner
7:15 pm - 7:30 pmBusiness Meeting (Part 2)
Candidate speeches; Announcement of Poster Awards
7:30 pm - 9:30 pmChallenges and Successes in Diabetes Discovery
Discussion Leader: Scott Edmondson (Merck)
7:30 pm - 8:00 pmWilliam Hagmann (Merck)
"Somatostatin Antagonists: A Potential Treatment for Type 2 Diabetes"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmPhil Hipskind (Eli Lilly)
"Glucagon Receptor Antagonists: From the Laboratory to the Patient"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmBenjamin Stevens (Pfizer)
"Approaching a Rule-of-Five Compliant Small Molecule Glucagon Receptor Antagonist: A Year From Discovery to FIH"
9:20 pm - 9:30 pmDiscussion
WEDNESDAY
7:30 am - 8:30 amBreakfast
8:45 am - 9:00 amBusiness Meeting (Part 3)
Election of Chair for the 2015 Meeting
9:00 am - 12:30 pmEpigenetics
Discussion Leader: Silvana Leit (Galenea)
9:00 am - 9:30 amManfred Jung (Albert-Ludwigs-Universität)
"Chemical Epigenetics - Editing the Bookmarks in the Book of Life"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amBrian Albrecht (Constellation Pharmaceuticals)
"Inhibition of BET Bromodomains for the Treatment of Cancer"
10:10 am - 10:20 amDiscussion
10:20 am - 10:50 amCoffee Break
10:50 am - 11:00 amPoster Awards 1 & 2: Oral Summaries
11:00 am - 11:30 amJohn Tatlock (Pfizer)
"Discovery and Optimization of Novel SETD7 Inhibitors"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmChun-wa Chung (GSK)
"First in Class BET Inhibitors"
12:10 pm - 12:20 pmDiscussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time (Organized Vice-Chair Elect Golf Scramble available)
5:00 pm - 6:00 pmPoster Session (Group B) / Social Hour
Discussion Leader: Simon Haydar (Eli Lilly)
6:00 pmDinner
7:30 pm - 9:30 pmAllosteric Drugs
Discussion Leader: Peter Bernstein (PhaRmaB, LLC)
7:30 pm - 8:00 pmJeffrey Conn (Vanderbilt)
"Allosteric Modulators of GPCRs for Treatment of CNS Disorders"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmChantal Alcouffe (Sanofi)
"SSR128129, an Allosteric Modulator of FGF-Rs"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmScott Kuduk (Merck)
"Evolution of Quinolizidinone M1 Receptor Selective Positive Allosteric Modulators"
9:20 pm - 9:30 pmDiscussion
THURSDAY
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting (Part 4)
Evaluation Forms; Site Selection & Scheduling For Future Conferences
9:00 am - 12:30 pmLate - Breaker Session
Discussion Leader: Jean-Christophe Harmange (Constellation Pharmaceuticals)
9:00 am - 9:30 amDustin Mergott (Lilly)
"Central Inhibition of Beta-Secretase in Humans with LY2811376 and LY2886721"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amKim Cameron (Pfizer)
"Design and Development of Ghrelin Inverse Agonists for the Treatment of Diabetes"
10:10 am - 10:20 amDiscussion
10:20 am - 10:55 amCoffee Break
10:55 am - 11:00 amPoster Award #3: Oral Summary
10:50 am - 11:30 amJohn Hynes (BMS)
"Discovery of a CCR1 Antagonist for the Treatment of Rheumatoid Arthritis"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmTesfaye Biftu (Merck)
"MK-3102: A Novel Once-Weekly DPP-4 Inhibitor for Type 2 Diabetes"
12:10 pm - 12:20 pmDiscussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time
6:00 pmDinner
7:30 pm - 9:00 pmChair's Speaker
Discussion Leader: Amy Ripka (SAR Consulting)
7:30 pm - 8:30 pmJohn Martin (Gilead)
"Twenty-Five Years of Advances in Nucleotide Antiviral Research"
8:30 pm - 9:00 pmDiscussion
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDeparture

 
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