Gordon Research Conferences
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Conference Program
 
Medicinal Chemistry
August 3-8, 2008
Colby-Sawyer College
New London, NH
Chair:
Les W. McQuire

Vice Chair:
Albert J. Robichaud

Dear Colleagues,

The 2008 Medicinal Chemistry Gordon Conference will be held August 3rd through 8th at Colby-Sawyer College in New London, New Hampshire. Vice-Chair Al Robichaud 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 2007 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 Young Shin Cho at Novartis. 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 Lori Krim Gavrin of Wyeth. 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 Mary Mader of Lilly 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. Please contact Mary with any questions or suggestions for activities.

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. I am looking forward to an outstanding conference in 2008 and thank you for your interest in the Medicinal Chemistry GRC.

Les McQuire
Chair, 2008 GRC on Medicinal Chemistry
Novartis Institutes for BioMedical Research


SUNDAY
2:00 pm - 11:00 pmArrival and Check-in
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 Les McQuire, Conference Chair
7:45 pm - 9:30 pmNovel Approaches to Neurodegenerative Diseases
Discussion Leader: Stephen Hitchcock (Amgen)
7:45 pm - 8:10 pm Peter Lansbury (Harvard)
"Approaches to a Disease-Modifying Drug for Parkinson's Disease"
8:10 pm - 8:20 pm Discussion
8:20 pm - 8:45 pm Ellen Baxter (Johnson & Johnson)
"Aminoheterocycles as BACE-1 Inhibitors for the Potential Treatment of Alzheimer's Disease"
8:45 pm - 8:55 pm Discussion
8:55 pm - 9:20 pm Mark Layton (Merck)
"NR2B Selective NMDA Receptor Antagonists"
9:20 pm - 9:30 pm Discussion
9:45 pm - 10:45 pm Poster Session / Social Hour
Discussion Leader: Young Shin Cho (Novartis)
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmApproaches to Treating Cognition and Schizophrenia
Discussion Leader: Robert Hudkins (Cephalon)
9:00 am - 9:30 am Joseph T. Coyle (Harvard Medical School)
"Glutamate and the Emerging Pathologic Circuit in Schizophrenia"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Jonathan Gross (Wyeth)
"The Design and Synthesis of Novel, Potent and Selective H3 Antagonists for use in CNS Disorders"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break / Group Photo
11:00 am - 11:30 am Klaus Bæk Simonsen (H. Lundbeck A/S)
"Novel NK3 Receptor Antagonists for the Treatment of Schizophrenia. Lead Optimization and Preclinical Pharmacology"
11:30 am - 11:40 am Discussion
11:40 am - 12:10 pm Neil D. Miller (GlaxoSmithKline)
"5-HT6 Receptor Antagonists for Symptomatic Treatment of Alzheimers Disease, from Discovery to Clinic"
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 pmAllosteric Modulation of G-Protein Coupled Receptors
Discussion Leader: Scott Kuduk (Merck)
7:30 pm - 8:00 pm Craig W. Lindsley (Vanderbilt University)
"In Vitro and In Vivo Characterization of Highly Subtype-Selective Allosteric Modulators of the M1 and M4 Muscarinic Receptors"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Jesper Lau (Novo Nordisk A/S)
"Discovery of Peptide and Non-peptide GLP-1 Agonists"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Jean-Phillipe Rocher (Addex Pharma SA)
"Discovery and Structure Activity Relationships of a New Series of mGluR5 Negative Allosteric Modulators"
9:20 pm - 9:30 pm Discussion
9:45 pm - 10:45 pm Poster Session / Social Hour
Discussion Leader: Young Shin Cho (Novartis)
TUESDAY
7:30 am - 8:30 amBreakfast
8:45 am - 9:00 amNominations for Chair of the 2011 meeting
Nominating Committee
9:00 am - 12:30 pmFoundation Funded Drug Discovery and Development
Discussion Leader: Celia Dominguez (CHDI)
9:00 am - 9:30 amRobert Pacific (CHDI)
"Disease Foundation Driven Research: A New Paradigm for Translational Drug Discovery"
9:20 am - 9:40 amDiscussion
9:40 am - 10:10 amAlex Kiselyov (Decode)
"Novel Small Molecule SMN2 Promoter Activators for the Potential Treatment of Spinal Muscular Atrophy"
10:10 am - 10:20 amDiscussion
10:20 am Coffee Break
11:00 am - 11:30 amSteve Courtney (Evotec)
"Optimization of Novel, Potent Inhibitors of Kynurenine Mono-oxygenase (KMO) for the Treatment of Huntington's Disease"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmKeith Barnes (AMRI/NINDS)
"Optimization of Indoprofen for the Treatment of Spinal Muscular Atrophy: A New NIH Driven Translational Research Model for Therapy Development"
12:10 pm - 12:20 pmDiscussion
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: Young Shin Cho (Novartis)
6:00 pmDinner
7:15 pm - 7:30 pmSpeeches by the candidates for Chair of the 2011 meeting
Nominating Committee
7:30 pm - 9:30 pmNew Advances in Inflammation Therapy
Discussion Leader: Francesco Salituro (Wyeth)
7:30 pm - 8:00 pmLiping Pettus (Amgen)
"The Discovery of Potent, Selective and Orally Efficacious p38 MAP Kinase Inhibitors Based on a Phthalazine Scaffold"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmWei Li (Wyeth)
"Selective MMP-12 Inhibitors as Potential Treatment for Respiratory Inflammatory Diseases"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmDavid Goldstein (Roche)
"The Discovery of Pamapimod, a Potent and Selective Inhibitor of P38 MAP Kinase"
9:20 pm - 9:30 pmDiscussion
9:45 pm - 10:45 pm Social Hour
WEDNESDAY
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting
(Election of Chair for the 2011 meeting; Discussion of 2011 meeting site; Fill out Conference Evaluation Forms)
9:00 am - 12:30 pmApplications of New Technologies
Discussion Leader: Bradley Morgan (Cytokinetics)
9:00 am - 9:30 am William Goddard III (California Institute of Technology)
"Methods for Predicting Structures of and Ligand Bonding to Membrane Proteins: Application to Receptors for Epinephrine, Dopamine, Serotonin, GLP1, Urotensin, and Tastants"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Nicholas Cosford (Burnham Institute for Medical Research)
"Chemical Genomics: A New Wave of HTS and Medicinal Chemistry in Academia"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break
11:00 am - 11:30 am X. Shawn Qian (Cytokinetics)
"Application of Electrostatic Potential Maps in the Discovery of Novel Inhibitors of Kinesin Spindle Protein"
11:30 am - 11:40 am Discussion
11:40 am - 12:10 pm Roger Ruggeri (Pfizer)
"Integration of Statistical Models in Drug Discovery and Design"
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: Young Shin Cho (Novartis)
6:00 pmDinner
7:45 pm - 9:30 pmFrom A Natural Product To A Clinical Candidate
Discussion Leader: Michael Luzzio (Novartis)
7:30 pm - 8:00 pm Kun Liu (Merck)
"Synthesis and Antibacterial Activity of Thiazomycin Analogs"
8:00 pm - 8:10 pm Discussion
8:10 pm - 8:40 pm Soong-Hoon (Andres) Kim (BMS)
"Synthesis and Biological Effects of BMS-753493: an Epothilone-folate Conjugate Designed to Selectively Target FR-α Expressing Tumor Cells"
8:40 pm - 8:50 pm Discussion
8:50 pm - 9:20 pm Frank Fang (Eisai Research)
"Chemical Evolution of Natural Products in Drug Discovery and Development"
9:20 pm - 9:25 pm Discussion
9:25 pm - 9:30 pm Presentation of Poster Awards
Presenter: Young Shin Cho (Novartis)
9:45 pm - 10:45 pm Social Hour
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:00 pmLate Breaking Topics
Discussion Leader: Lori Krim Gavrin (Wyeth)
9:00 am - 9:30 am Lihu Yang (Merck)
"Discovery of GPR40 Agonists for the Treatment of Diabetes"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Robert Marquis (GlaxoSmithKline)
"Discovery of Ronacaleret an Orally Bioavailable PTH Secretagogue for the Treatment of Osteoporosis"
10:10 am - 10:20 am Discussion
10:20 am Coffee Break
10:40 am - 11:10 am Graham Johnson (Rib-X Pharmaceuticals)
"Discovery and Clinical Development of RX-1741, a Designer Oxazolidinon"
11:10 am - 11:20 am Discussion
11:20 am - 11:50 am Heather Finlay (BMS)
"The discovery of Pyrazolodihydropyrimidine KV1.5 Blockers"
11:50 am - 12:00 pm Discussion
12:00 pm - 12:30 pmPoster Award Winner Talks
Discussion Leader: Young Shin Cho (Novartis)
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 Talk
7:30 pm - 8:30 pmPaul J. Reider (Princeton University)
8:30 pm - 9:30 pmGeneral Discussion
9:45 pm - 10:45 pmSocial Hour
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart

 
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