Conference Program
 
Combinatorial Chemistry

July 6-11, 2003
Tilton School
Tilton, NH

Chair:
Thomas J. Sowin

Vice Chair:
A Ganesan

SUNDAY
2:00 pm - 9:00 pmArrival and Check-in
6:00 pmDinner
7:30 pm - 9:30 pmSynthetic Methodologies - Part 1
Discussion Leader: Greg Roth (Boehringer-Ingelheim-USA)
7:30 pm - 8:10 pmPeter Wipf (University of Pittsburgh)
"Peptide Mimetics- Pharma's Worst Nightmare?"
8:10 pm - 8:50 pmMike Organ (York University-Ontario)
"Recent Advances in High Throughput Synthesis and Screening"
8:50 pm - 9:30 pmKay Brummond (University of Pittsburgh)
"Allenes and Transistion Metals: A Diverging Strategy for Assembling Multiple Architecturally Unique Compounds"
MONDAY
7:30 am - 8:30 amBreakfast
8:30 amGroup Photo
9:00 am - 12:30 pmSynthetic Methodologies - Part 2
Discussion Leader: Phil Kumler (SUNY-Fredonia)
9:00 am - 9:10 amChair's Welcome and Announcements
9:10 am - 9:50 amShelli McAlpine (San Diego State University)
"Synthesis of Antibiotics: Synergimycin Derivatives and Holliday Junction binders"
9:50 am - 10:30 amNina Kann (Chalmers University of Technology - Sweden)
"Solid Phase Synthesis Using Cobalt Carbonyl Complexes"
10:30 am - 11:00 amCoffee Break
11:00 am - 11:45 amRodolfo Lavilla (University of Barcelona - Spain)
"New Tricks for an Old Co-factor: MCR's based on NADH Analogs"
11:45 am - 12:30 pmBruce Hamper (Pharmacia - St. Louis)
"Parallel Synthesis of Targeted Heterocycles for Drug Discovery"
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #1
6:00 pmDinner
7:30 pm - 9:30 pmNatural Product-Like Libraries
Discussion Leader: Tom Sowin (Abbott Laboratories-USA)
7:30 pm - 8:00 pmSheo Sing (Merck-Rahway)
"The Role of Natural Products in Drug Discovery"
8:00 pm - 8:50 pmBrian Warrington (GlaxoSmithKline-UK)
Part 1 - "Do Natural Products have a Role in Drug Discovery?"
Part 2 - "Why Microchemistry?"
8:50 pm - 9:30 pmJohn Porco (Boston University)
"Expanded Chemical Diversity Using Stereocontrolled Synthesis"
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmComputer Techniques In Combinatorial Chemistry
Discussion Leader: Daryl Sauer (Abbott Laboratories-USA)
9:00 am - 9:45 amTudor Oprea (University of New Mexico)
"Understanding the Leadlike Space: An Analysis of Leads, Drugs, and Leads that are Drugs"
9:45 am - 10:30 amDavid Nunn (Wyeth-USA)
"Compound Library Design Tools Using Multivariate Analysis"
10:30 amCoffee Break
11:00 am - 11:45 amDick Cramer (Tripos-USA)
"Topomers: Discovering and Optimizing Leads Using 3D Shape for Library Design"
11:45 am - 12:30 pmJun Xu (Discovery Partners -USA)
"Combinatorial Library Design Based upon Dynamic Classification and Multiple Propertities Optimization"
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #1
6:00 pmDinner
7:30 pm - 9:30 pmLead Optimization Using Combinatorial Chemistry - Case Studies
Discussion Leader: Bruce Hamper (Pharmacia)
7:30 pm - 8:10 pmAndrew Baxter (AstraZeneca -UK)
"Hit to Lead Case Studies"
8:10 pm - 8:50 pmAdam Gilbert (Wyeth -USA)
"Statistical Molecular Design and Multivariate Analysis of acyl Carrier Protein Synthase (AcpS) Inhibitors"
8:50 pm - 9:30 pmJohn Josey (Array BioPharma -USA)
"Target-based Libraries for Lead Identification and Optimization"
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmLarge Libraries and High Throughput Methods
Discussion Leader: Shelli McAlpine (San Diego State University)
9:00 am - 9:45 amDaryl Sauer (Abbott Laboratories- USA)
"Design and Implementation of a High Throughput Organic Synthesis Service for Drug Discovery"
9:45 am - 10:30 amChris Cooper (Bristol-Myers Squibb- USA)
"High Throughput Target Class Library Development and Production: Recent Applications of the IRORI NanoKanTM Combinatorial Chemistry System"
10:30 amCoffee Break
11:00 am - 11:45 amNicolas Winssinger (University Louis Pasteur - France)
"From Split-Pool Libraries to Microarrays and Functional Profiling"
11:45 am - 12:30 pmJacqueline Sharon (Boston University -School of Medicine)
"Polyclonal Antibody Libraries for Cancer and Infectious Diseases"
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #2
6:00 pmDinner
7:30 pm - 9:30 pmPurification and QC of Compound Libraries
Discussion Leader: Sam Gerritz (Bristol-Myers Squibb -USA)
7:30 pm - 8:10 pmMarc Towle (ArQule -USA)
"High Throughtput Purification Approaches to Support a Parallel Synthesis Platform"
8:10 pm - 8:50 pmNathan Collins (ChemRx -USA)
"High Throughput Purification as a Commercial Process: The Accelerated Retention Window (ARW) Method as a Library Production Tool"
8:50 pm - 9:30 pmLarry Truesdale (Pfizer- San Diego)
"High Throughput Supercritical Fluid Chromatography for Combinatorial Libraries"
THURSDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmTarget Directed Libraries
Discussion Leader: Kay Brummond (University of Pittsburgh)
9:00 am - 9:45 amBarry Bunin (Libraria -USA)
"The Identification of Novel Abl Kinase Inhibitors in Small Targeted Libraries Designed from Gene-Family Wide Public-Domain SAR and Predictive e-Screens"
9:45 am - 10:30 amSam Gerritz (Bristol-Myers Squibb -USA)
"Target Class Libraries for the Discovery of New Leads"
10:30 amCoffee Break
11:00 am - 11:45 amPeter Brown (GlaxoSmithKline -USA)
"Design of Nuclear Receptors Targeted Arrays"
11:45 am - 12:30 pmBusiness Meeting: "Election of 2004 Vice-chair / Conference Surveys"
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session #2
6:00 pmDinner
7:30 pm - 9:30 pmKeynote Session: Chemistry and Chemical Genomics at Harvard's ICCB
Discussion Leader: A. Ganesan (University of Southampton-UK)
7:30 pm - 9:30 pmStuart Schreiber, Eric Brauner, Paul Clemons, John Tallarico (Harvard University)
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart

INDUSTRIAL SUPPORTERS

Abbott Laboratories
Albany Molecular Research
Amgen
Array BioPharma
Aventis
Boehringer Ingelheim
Bristol-Myers Squibb
Eli Lilly
Gilead Sciences
Pfizer
Polymer Laboratories
Roche Bioscience
Wyeth Research


Last Updated: May 4, 2006