Gordon Research Conferences
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Conference Program
 
Medicinal Chemistry
August 2-7, 2009
Colby-Sawyer College
New London, NH
Chair:
Albert J. Robichaud

Vice Chair:
Mary M. Mader

Dear Colleagues,

The 2009 Medicinal Chemistry Gordon Conference will be held August 2nd through 7th at Colby-Sawyer College in New London, New Hampshire. Vice-Chair Mary Mader is putting together the program, which will feature talks on cutting edge applications of medicinal chemistry to drug discovery programs as well as new technology that will play a role in advancing the field. The 2008 program will give you an idea of the topics typically covered. We encourage attendees to bring poster presentations, this is a great way to introduce your work to colleagues and solicit their feedback. The poster sessions will be organized by Janeta Popovici-Muller of Schering Plough. The conference scientific sessions will end with a Special Topics Session, comprised of late-breaking results from recent clinical compounds. This session will be organized by Sandra Filla of Lilly. Please contact her with any suggested contributions for Special Topics. Finally, the conference will wrap up on Thursday evening with the traditional lobster dinner and Chair's Talk, which will feature a talk on general aspects of the medicinal chemistry discipline.

The Medicinal Chemistry GRC will continue the tradition of outstanding science presented in a relaxed atmosphere. Social events for the week will be organized by Vice-Chair Elect Frank Salituro of Wyeth Research and will feature the Monday Hike to the peak of Mt. Kearsarge, the Tuesday East/West Softball Game (Krantz Cup) and the Wednesday Vice-Chair Elect Golf Tournament. In addition, we will be having our 3rd wine tasting and plan to continue our recently added Vice-Chair Fundraising event on Thursday evening. Please contact Frank with any questions or suggestions for activities.

On behalf of myself, the Vice Chair and the Vice-Chair elect, I would like to specifically encourage the application and attendance of scientists from a diversity of backgrounds and experience. In particular, women, minorities and younger scientists in the early stages of their careers as medicinal chemists should consider application. We are looking forward to an outstanding conference in 2009 and thank you for your interest in the Medicinal Chemistry GRC.

Al Robichaud
Chair, 2009 GRC on Medicinal Chemistry
Wyeth Research, Princeton NJ


SUNDAY
2:00 pm - 9:00 pmArrival and Check-in (Office Closed 6:00 pm - 7:00 pm)
5:00 pm - 6:00 pmWelcome Mixer (Dining Center)
6:00 pmDinner
7:30 pm - 7:45 pmIntroductory Comments by GRC Site Staff / Welcome by Albert J. Robichaud, Conference Chair
7:45 pm - 9:30 pmPathway and Phenotypic Screening in Target and Drug Discovery
Discussion Leader: Young Shin Cho (Novartis)
7:45 pm - 8:10 pm Sergey Kozmin (Univ of Chicago)
"Identification of the cellular target of leucascandrolide A and neopeltolide, Glycolysis inhbitors"
8:10 pm - 8:20 pm Discussion
8:20 pm - 8:45 pm Mike Foley (MIT)
"Small Molecule Microarray and Target ID Facilitate Probe Discovery"
8:45 pm - 8:55 pm Discussion
8:55 pm - 9:20 pm John Tallarico (Novartis)
"Chemistry-centric Discovery of New Targets"
9:20 pm - 9:30 pm Discussion
9:45 pm - 10:45 pm Poster Session / Social Hour
Discussion Leader: Janeta Popovici-Muller (Schering Plough)
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmNew Prospects for the Treatment of Type 2 Diabetes
Discussion Leader: Scott J. Hecker (Metabasis Therapeutics)
9:00 am - 9:30 am Mark Erion (Metabasis Therapeutics)
"Design of Fructose 1,6-Bisphosphatase Inhibitors and Evaluation of their Safety, Tolerability and Glucose-Lowering Potential in Patients with Poorly-Controlled Type 2 Diabetes"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Ramakanth Sarabu (Roche)
"Glucokinase Activators - Discovery to POC"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break / Group Photo
11:00 am - 11:30 am Rob Jones (Arena Pharma)
"Discovery of JNJ-28630355, a Potent & Selective Tri-substituted Pyrimidine GPR119 Agonist"
11:30 am - 11:40 am Discussion
11:40 am - 12:10 pm Bob Dow (Pfizer Global R&D)
"Discovery and Preclinical Pharmacology of PF-4620110: A Selective Inhibitor of DGAT-1 for the Treatment of Type-2 Diabetes"
12:10 pm - 12:20 pm Discussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time (Organized Mt. Kearsarge Hike available)
6:00 pmDinner
7:30 pm - 9:30 pmAntivirals
Discussion Leader: Manoj Desai (Gilead Sciences)
7:30 pm - 8:00 pm Paul M. Scola (Bristol-Myers Squibb)
"Inhibition of HCV"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm John McCauley (Merck)
"Discovery of MK-7009: A Novel Macrocyclic HCV NS3/4a Protease Inhibitor"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Mike Peel (Scynexis)
"Cyclophilin Inhibition: Targeting HCV Replication via Host-Protein Modulation"
9:20 pm - 9:30 pm Discussion
9:45 pm - 10:45 pm Poster Session / Social Hour
Discussion Leader: Janeta Popovici-Muller (Schering Plough)
TUESDAY
7:30 am - 8:30 amBreakfast
8:45 am - 9:00 amBusiness Meeting (Part I)
(Nominations for Chair of the 2012 Meeting by Nominating Committee)
9:00 am - 12:30 pmTargeting the PI3K/AKT pathway for oncology: Recent advances in drug discovery
Discussion Leader: Jean-Cristophe Harmange (Constellation Pharma)
9:00 am - 9:30 am John Allen (Amgen)
"Azole-Based Inhibitors of AKT"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Kevin Freeman-Cook (Pfizer Global R&D)
"Discovery of a Selective Akt Inhibitor for the Treatment of Human Tumors"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break
11:00 am - 11:30 am Mark Layton (Merck)
"MK-2206: Discovery of the First Oral Allosteric Akt Kinase Inhibitor"
11:30 am - 11:40 am Discussion
11:40 am - 12:10 pm Carlos Garcia-Echeverria (Novartis)
"Imidazo[4,5-c]quinoline derivatives - structure-based design and optimization of dual PI3K/mTOR inhibitors"
12:10 pm - 12:20 pm Discussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time (Organized Annual East-West Softball Game)
5:00 pm - 6:00 pmPoster Session
Discussion Leader: Janeta Popovici-Muller (Schering Plough)
6:00 pmDinner
7:15 pm - 7:30 pmBusiness Meeting (Part II)
(Speeches by the candidates for Chair of the 2012 meeting)
7:30 pm - 9:30 pmSphingosine-1-phosphate signalling and immunomodulation
Discussion Leader: Zoran Rankovic (Schering-Plough)
7:30 pm - 8:00 pm Hugh Rosen (Scripps Institute)
"Chemical modulators of the S1P receptor system: the integrated biology underlying therapeutics"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Kevin Cusack (Abbott)
"S1P receptor agonist: MedChem hit to DC and pre-clinical PoC"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Nigel Cooke (Novartis)
"Discovery and optimisation of novel S1P-1 receptor modulators"
9:20 pm - 9:25 pm Discussion
9:25 pm - 9:30 pm Presentation of Poster Awards
Presenter: Janeta Popovici-Muller (Schering Plough)
9:45 pm - 10:45 pm Social Hour
WEDNESDAY
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting (Part III)
(Election of Chair for the 2012 meeting; Discussion of 2012 meeting site; Fill out Conference Evaluation Forms)
9:00 am - 12:30 pmPreclinical Screening and Design Principles for Improved Drug Safety
Discussion Leader: Mark Noe (Pfizer Global R&D)
9:00 am - 9:30 am Tom Baillie (Univ of Washington)
"The Role of DMPK in Optimizing Drug Candidates for Safety"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am David Goldstein (Roche)
"Using In-Vitro Assays, including KinaseSelectivity Profiles, to Predict Toxicity In-Vivo"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break
10:55 am - 11:00 am Poster Award 1: Oral Overview
11:00 am - 11:30 am Jim Empfield (Astra Zeneca)
"Physicochemical and pharmacological properties as predictors of drug safety and success"
11:30 am - 11:40 am Discussion
11:40 am - 12:10 pm Martin Edwards (Pfizer Global R&D)
"Drug Safety - Can we usefully separate structurally specific risks from physical property risks?"
12:10 pm - 12:20 pm Discussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time (Organized Annual Vice-Chair Elect Golf Tournament)
5:00 pm - 6:00 pmPoster Session
Discussion Leader: Janeta Popovici-Muller (Schering Plough)
6:00 pmDinner
7:30 pm - 9:30 pmNew Targets in Oncology
Discussion Leader: Matthew Marx (Pfizer Global R&D)
7:30 pm - 7:35 pmPoster Award 2: Oral Overview
7:35 pm - 8:00 pm Shawn Qian (Cytokinetics)
"CENP-E motor protein, Clinical candidate first disclosure, SAR and in vivo biology"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Mike Koehler (Genentech)
"The Discovery of the Hedgehog Antagonist GDC-0449 for the Treatment of Solid Tumors"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Ashvin Gavai (Bristol-Myers Squibb)
"Novel Androgen Receptor Antagonists: Lead Optimization & Preclinical Pharmacology"
9:20 pm - 9:30 pm Discussion
9:45 pm - 10:45 pm Social Hour
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmLate Breaking Topics
Discussion Leader: Sandra Filla (Eli Lilly)
9:00 am - 9:30 am Patrick Verhoest (Pfizer Global Research & Development)
"Identification of a PDE9 Clinical Candidate for the Treatment of Alzheimer's Disease Utilizing Prospective Design and Novel Protocol Development"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Lianhong Xu (Gilead)
"GS-9350: A Potent and Selective Pharmacoenhancer"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break
10:50 am - 10:55 amPoster Award 3: Oral Overview
10:55 am - 11:25 am Philip A. Hipskind (Research Fellow, Lilly Research Laboratories)
"Novel CRH1 Antagonists for Anxiety Depression Alcohol Abuse"
11:25 am - 11:35 am Discussion
11:35 am - 12:05 pm Mark Bunnage (Pfizer Global Research & Development)
"Discovery of PF-610,355: An inhaled once-daily Beta-2 adrenoceptor agonist for treatment of asthma & COPD"
12:05 pm - 12:15 pm Discussion
12:30 pmLunch
1:30 pm - 5:00 pmFree Time
5:00 pm - 6:00 pmChair's Reception
6:00 pmDinner
7:30 pm - 9:30 pmChair's Speaker
7:30 pm - 8:30 pm Paul J. Reider (Princeton University)
8:30 pm - 9:30 pm General Discussion
9:45 pm - 10:45 pm Social Hour
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart

 
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