Conference Program
 
Combinatorial Chemistry
High Throughput Chemistry & Chemical Biology
(This meeting is currently known as "High Throughput Chemistry & Chemical Biology")
June 7-12, 2009
Colby-Sawyer College
New London, NH
Chair:
Joseph M. Salvino

Vice Chair:
Michael A. Foley

Related Meeting Information
The Combinatorial Chemistry Gordon Research Conference was held in conjunction with the Combinatorial Chemistry Gordon-Kenan Research Seminar. Please refer to the Combinatorial Chemistry GKRS web page for more information.

Dear Colleagues,

The 2009 Combinatorial Chemistry; High Throughput Chemistry and Chemical Biology Gordon Research Conference will be held June 7-12 at Colby Sawyer College, New London, NH. This year we will hold the first Gordon Research Seminar for our conference the weekend prior to the GRC, June 6-7. This year’s vice chair is Dr. Michael Foley, of the Broad Institute, and the two co-chairs for the GRS are Dr. Alan Rolfe and Thiwanka B. Samarakoon, both students in the chemistry department at the University of Kansas. Combinatorial chemistry is a dynamic, rapidly evolving field and has different meaning to various scientists. The combinatorial chemistry community has contributed significantly towards the evolution of the drug discovery process with the major emphasis in the field evolving towards methods to accelerate lead generation / lead optimization, focused parallel synthesis, high throughput technology, and chemical biology. This year’s program will feature cutting edge talks bridging the disciplines of organic synthesis, medicinal chemistry, and chemical biology applied towards high speed synthesis, parallel chemistry approaches, rapid generation of structure activity relationships to accelerate drug discovery, and the discovery of small molecule probes to discover and elucidate molecular pathways. Feedback based on reports of monitors and attendee self-evaluation has given this meeting an excellent rating. A review of the 2008 program will give you an idea of the range of topics typically covered. Participants are encouraged to present posters. 2008 poster winners; Benjamin L. Miller, University of Rochester; Marco Schmidt, Leibniz-Institute for Molecular-Pharmacology Berlin; and Ann Kelly; Broad Institute, will be presenting talks this year.

The GRC and accompanying GRS Combinatorial Chemistry High throughput Chemistry and Chemical Biology will continue the tradition of excellent science in a relaxed atmosphere. I would like to encourage the application and attendance of scientists from diverse backgrounds and experiences, including women, minorities, graduate students, post docs, academic, and industrial researchers to the Conference. Continued corporate support in terms of leading edge talks, conference attendance, and financial backing is essential to insure that combinatorial chemistry continues to meet the needs of the drug discovery and probe development community in the future. I look forward to an outstanding conference in 2009 and thank you for your support and interest.

Joseph M. Salvino, PhD
Chair, 2009 GRC on Combinatorial Chemistry
Cephalon, Inc.


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 - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmFrontiers in Drug Discovery
Discussion Leader: Oliver Reiser (University of Regensberg)
7:40 pm - 8:20 pm Mikel Moyer (Broad Institute)
"Medicinal chemists are people too, and that is a problem"
8:20 pm - 8:30 pm Discussion
8:30 pm - 9:20 pm Stuart Schreiber (Harvard University)
"The Gap between Scientists' Aspirations and Society's Expectations"
9:20 pm - 9:30 pm Discussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHit to Lead / Medicinal Chemistry
Discussion Leader: Roland E. Dolle (Adolor)
9:00 am - 9:25 am Karin Worm (Adolor)
"Library Approach to Non-Psychotropic Biaryl Cannabinoid Receptor Agonists"
9:25 am - 9:35 am Discussion
9:35 am - 10:00 am Horst Hemmerle (Lilly, Inc.)
"Learning from Data-Driven Iterative Library Design in Major Biological Target Families"
10:00 am - 10:10 am Discussion
10:10 am - 10:40 am Coffee Break / Group Photo
10:40 am - 11:05 am Scott Wolkenberg (Merck)
"GlyT1 Inhibitors for the Treatment of Schizophrenia"
11:05 am - 11:15 am Discussion
11:15 am - 11:40 am Mario Rottländer (H. Lundbeck A/S)
"High Throughput Medicinal Chemistry for CNS Drug Targets"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pm Tony W.J. Cooper (GlaxoSmithKline)
"The Use of Arrays (Small Focused Libraries) in Medicinal Chemistry - Our Experiences and Practice"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session I
6:00 pmDinner
7:30 pm - 9:30 pmDrug Discovery and New Directions in Medicinal Chemistry
Discussion Leader: Scott Wolkenberg (Merck)
7:30 pm - 8:20 pm Amos Smith III (University of Pennsylvania)
"Anion Relay Chemistry (ARC): A New Tactic for Diversity Oriented Synthesis"
8:20 pm - 8:30 pm Discussion
8:30 pm - 9:20 pm Paul Anderson (Consultant)
"Where We Have Been, Where We Might Be Going"
9:20 pm - 9:30 pm Discussion
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHigh Throughput Technologies
Discussion Leader: Greg Roth (Burnham Institute for Medical Research)
9:00 am - 9:30 am David Spring (Cambridge University)
"Search for New Antibacterials Using Diversity­Oriented Synthesis"
9:30 am - 9:40 am Discussion
9:40 am - 10:10 am Annaliese Franz (UC Davis)
"Catalytic Enantioselective Synthesis of Substituted Oxindole Heterocycles"
10:10 am - 10:20 am Discussion
10:20 am - 10:40 am Coffee Break
10:40 am - 11:05 am Ann Kelly (Broad Institute)
"Accessing Skeletal Diversity Using Catalyst Control: Formation of n and n + 1 Macrocyclic Triazole Rings"
11:05 am - 11:15 am Discussion
11:15 am - 11:40 am Marco Schmidt (Leibniz Institute)
"Dynamic Ligation Screening: A Novel Tool in Drug Discovery"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pm Benjamin Miller (Univ Rochester)
"A Dynamic Combinatorial Approach to RNA Recognition"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session I
6:00 pmDinner
7:30 pm - 9:30 pmChemical Methodologies and Library Development
Discussion Leader: Padmakumar R. Kaimal (SUVEN)
7:30 pm - 7:55 pm Anthony W. Czarnik (Deuteria Pharmaceuticals, LLC)
"SAR of Combinatorially-Deuterated Atorvastatins"
7:55 pm - 8:05 pm Discussion
8:05 pm - 8:30 pm Richard Hartley (University of Glasgow)
"Chameleon Catches for the Synthesis of Privileged Structures"
8:30 pm - 8:40 pm Discussion
8:40 pm - 9:20 pm John Porco (CMLD Boston University)
"Reaction Discovery Approaches to Chemical Diversity"
9:20 pm - 9:30 pm Discussion
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmChemical Methodologies and Library Development
Discussion Leader: Michael Lawrence (BMS)
9:00 am - 9:25 am Scott A. Snyder (Columbia University)
"Strategies for the Controlled Synthesis of Oligomeric Polyphenols"
9:25 am - 9:35 am Discussion
9:35 am - 10:00 am Greg Roth (Burnham Institute for Medical Research)
"Surf and Turf: Approaches towards Natural Product Inspired Libraries"
10:00 am - 10:10 am Discussion
10:10 am - 10:30 am Coffee Break
10:30 am - 10:55 am Aaron Beeler (CMLD Boston University)
"Discovery of Chemical Reactions through Multidimensional Screening"
10:55 am - 11:05 am Discussion
11:05 am - 11:35 am Anna Mapp (University of Michigan)
"Small Molecule Transcriptional Switches"
11:35 am - 11:45 am Discussion
11:45 am - 12:20 pm Paul Floreancig (CMLD University of Pittsburgh)
"Nitriles as Versatile Building Blocks in Reaction Development"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session II
6:00 pmDinner
7:00 pm - 7:30 pmBusiness Meeting (Part I)
(Nominations for the next Vice Chair; Fill out Conference Evaluation Forms)
7:30 pm - 9:30 pmDrug Discovery and Synthesis
Discussion Leader: Scott A. Snyder (Columbia University)
7:30 pm - 8:20 pm Kevin Burgess (Texas A&M)
"Minimalist Peptidomimetics"
8:20 pm - 8:30 pm Discussion
8:30 pm - 9:20 pm M. Christina White (University of Illinois)
"C-H: A New Functional Group for Streamlining Synthesis"
9:20 pm - 9:30 pm Discussion
THURSDAY
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting (Part II)
(Vice Chair nominee talks)
9:00 am - 12:30 pmHigh Throughput Technologies / Hit to Lead
Discussion Leader: Richard Hartley (University of Glasgow)
9:00 am - 9:25 am Hong Liu (Novartis)
"Discovery of Novel Cannabinoid-1 Receptor Antagonists and Their Anti-Obesity Efficacy"
9:25 am - 9:35 am Discussion
9:35 am - 10:05 am Craig Thomas (NIH Chemical Genomics Center)
"From Screen to Lead: Technologies, Profiles and Case Studies to Consider"
10:05 am - 10:15 am Discussion
10:15 am - 10:30 am Coffee Break
10:30 am - 10:55 am Michael Lawrence (BMS)
"From Screening Hits to In Vivo Actives - a Cardiovascular HTL Case Study"
10:55 am - 11:05 am Discussion
11:05 am - 11:35 am Paul Fleming (AstraZeneca)
"Applications of Parallel Synthesis for the Discovery of Novel Antibacterials"
11:35 am - 11:45 am Discussion
11:45 am - 12:20 pm Alex Kiselyov (Decode)
"A Tandem of Structural Biology and Chemistry: Application of Fragment-Based Screening to Unravel Bacterial Genome"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 6:00 pmPoster Session II
6:00 pmDinner
7:00 pm - 7:30 pmBusiness Meeting (Part III)
(Election of the next Vice Chair; Discuss future Site & Scheduling preferences)
7:30 pm - 9:30 pmFrontiers in Drug Discovery
Discussion Leader: Anna Mapp (University of Michigan)
7:30 pm - 8:15 pm Alexis Borisy (CombinatoRx)
"Combinatorial Drug Targets"
8:15 pm - 8:25 pm Discussion
8:25 pm - 9:20 pm Edward Scolnick (Broad Institute)
"The Genomics of Psychotic Illness: A Revolution in Psychiatry"
9:20 pm - 9:30 pm Discussion
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart