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Medicinal Chemistry

Gordon Research Conference

August 7 - 12, 2005
Chair S. David Kimball
Vice Chairs John A. Lowe and George D. Hartman
Colby-Sawyer College
541 Main Street
New London, New Hampshire, United States
 Venue and Travel Information

Conference Description

The 2005 Medicinal Chemistry Gordon Conference will be held August 7th through 12th at Colby-Sawyer College in New London, New Hampshire. Vice-Chair John Lowe has done an outstanding job putting together the cutting edge program below. 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 Mary Mader of Lilly. Finally, the conference will wrap up on Thursday evening with the traditional lobster dinner and Chair's Talk, which will be given by Roy Vagelos, formerly of Merck.

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 George Hartman of Merck 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.

Conference Program

SUNDAY
2:00 pm - 9:00 pm Arrival and check-in
5:00 pm - 6:00 pmWelcome Mixer (Dining Center)
6:00 pmDinner
Conference Chair: David Kimball (Lexicon) & Colby-Sawyer Site Manager
Opening Remarks
7:30 pm - 9:30 pm Kinase Inhibitors
Discussion Leader: Andrew Mortlock (Astra-Zeneca)
7:30 pm - 7:55 pmWalter Ward (Astra Zeneca)
"An alternative approach to inhibition of p38 MAP kinase: Implications for medicinal chemistry"
7:55 pm - 8:00 pmDiscussion
8:00 pm - 8:25 pmPaul Manley (Novartis)
"Medicinal Chemistry versus Bcr-Abl"
8:25 pm - 8:30 pmDiscussion
8:30 pm - 8:55 pmHaile Tecle (Pfizer)
"Non-ATP Competitive MEK Inhibitors: PD0325901"
8:55 pm - 9:00 pmDiscussion
9:00 pm - 9:25 pmBrian Werneberg (Boehringer Ingelheim)
"Pursuit of Selective p38alpha Inhibitors"
9:25 pm - 9:30 pmDiscussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pm The Hit-to-Lead Process
Discussion Leader: Amy Ripka (Daiamed)
9:00 am - 9:30 amSamuel Gerritz (BMS)
"Combinatorial Chemistry in the Context of Hit Identification and Lead Optimization"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amBrian Shoichet (U. Cal. San Francisco)
"A specific mechanism for non-specific inhibition of screening hits"
10:10 am - 10:20 amDiscussion
10:20 am - 11:00 amCoffee Break / Group Photo
11:00 am - 11:30 amBill Michne (Astra-Zeneca - retired)
"Hit to Lead: Historical Perspective, Current Outcomes, and Future Challenges"
11:30 am - 11:40 am Discussion
11:40 am - 12:10 pmDennis Underwood (Infinity)
"Drug Discovery... a game of twenty questions?"
12:10 pm - 12:20 pmDiscussion
12:30 pmLunch
1:30 pm - 6:00 pmFree Time (organized Mt. Kearsarge hike available)
6:00 pmDinner
7:30 pm - 9:30 pmBiomarkers and PET Imaging
Discussion Leader: Balu Balusubramanian (BMS)
7:30 pm - 8:00 pmChet Mathis (U. Pittsburgh)
"PET Imaging and Alzheimer Probes"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmDoug Dischino (BMS)
"Impact of PET Imaging in preclinical and development programs"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmRichard Hargreaves (Merck)
"CNS drug development using novel PET imaging"
9:20 pm - 9:30 pmDiscussion
9:45 pm - 10:45 pmPoster Session / Social Hour
Discussion Leader: Frank Salituro (Vertex)
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHCV Antivirals
Discussion Leader: Michael Bos (Boehringer-Ingelheim)
9:00 am - 9:30 amRalf Bartenschlager (U. Heidelberg)
"HCV molecular virology: targets for antiviral drugs and cell-based systems for their evaluation"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 amRobert Perni (Vertex)
"The Design and Profile of VX-950, an HCV NS3-4A Protease Inhibitor in Clinical Development"
10:10 am - 10:20 amDiscussion
10:20 am - 11:00 amCoffee Break
11:00 am - 11:30 amPierre Beaulieu (Boehringer-Ingelheim)
"The identification of HCV Polymerase inhibitors: A showcase of modern drug discovery"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmDick Storer (Idenix)
"Ribonucleoside Analogues as Agents for the Treatment of Hepatitis C Infection"
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: Frank Salituro (Vertex)
6:00 pmDinner
7:30 pm - 9:30 pmNew Directions in Antibiotics
Discussion Leader: John Primeau (Astra-Zeneca)
7:30 pm - 8:00 pmPaul Aristoff (Pfizer)
"Oxazolidinone Antibacterials"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmDean Stamos (Vertex)
"GyrB/ParE Inhibitors"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmZhengyu Yuan (Vicuron)
"PDF Inhibitors"
9:20 pm - 9:30 pmDiscussion
9:45 pm - 10:45 pmPoster Session / Social Hour
Discussion Leader: Frank Salituro (Vertex)
WEDNESDAY
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amConference Business meeting
9:00 am - 12:30 pmProtease Inhibitors for Treating Pulmonary Inflammatory Disorders
Discussion Leader: Bruce Maryanoff (J&J)
9:00 am - 9:30 amDomenico Spina (Kings College London)
"Pulmonary inflammatory diseases and their therapies"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amMichael Greco (J&J)
"Inhibitors of cathepsin G and chymase"
10:10 am - 10:20 amDiscussion
10:20 am - 11:00 amCoffee Break
11:00 am - 11:30 amZhongli Gao (Sanofi-Aventis)
"Inhibitors of tryptase"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmJohn Link (Celera)
"Inhibitors of cathepsin S"
12:10 pm - 12:20 pmDiscussion
12:30 pm Lunch
1:30 pm - 5:00 pmFree Time (organized annual Vice-Chair elect Golf Tournament)
5:00 pm - 6:00 pmPoster Session
Discussion Leader: Frank Salituro (Vertex)
7:30 pm - 9:30 pmNew Treatments for Ophthalmological Disorders
Discussion Leader: Peter Klimko (Alcon Research)
7:30 pm - 8:00 pmJun Inoue (Senju)
"Calpain Inhibitors for the Treatment of Retinopathy"
8:00 pm - 8:10 pmDiscussion
8:10 pm - 8:40 pmYongxin Han (Merck Frosst)
"Selective EP4 Agonists as Ocular Hypotensive Agents"
8:40 pm - 8:50 pmDiscussion
8:50 pm - 9:20 pmJesse May (Alcon Research)
"Ocular Hypotensive 5-HT2 Receptor Agonists"
9:20 pm - 9:30 pmDiscussion
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmLate Breaking Topics
Discussion Leader: Mary Mader (Lilly)
9:00 am - 9:30 amMark Bunnage (Pfizer)
"TAFIa Inhibitors for Treatment of Thrombosis - Discovery of UK 396,082"
9:30 am - 9:40 amDiscussion
9:40 am - 10:10 amJasbir Singh (Decode)
"EP3 Receptor Antagonists"
10:10 am - 10:20 amDiscussion
10:20 am - 11:00 amCoffee Break
11:00 am - 11:30 amSrikanth Venkatraman (Schering)
"Discovery of Sch 503034, a Selective, Potent HCV NS3 Protease Inhibitor with Oral Bioavailability"
11:30 am - 11:40 amDiscussion
11:40 am - 12:10 pmAndy Freeman (GSK)
"Discovery of a Novel Benzophenone as a Next Generation HIV-1 NNRTI Agent"
12:10 pm - 12:20 pmDiscussion
12:30 pm Lunch
1:30 pm - 6:00 pmFree Time
6:00 pmDinner
7:30 pm - 9:30 pmChair's Talk
Discussion Leader: David Kimball (Lexicon)
7:30 pm - 8:30 pmRoy Vagelos (Merck - retired)
"The Basis of Drug Discovery - Past and Future"
FRIDAY
7:30 am - 8:30 am Breakfast
9:00 amDeparture

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