SUNDAY |
2:00 pm - 9:00 pm | Arrival and Check-in (Office Closed 6:00 pm - 7:00 pm) |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | Frontiers 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 am | Breakfast |
9:00 am - 12:30 pm | Hit 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 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session I |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Drug 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 am | Breakfast |
9:00 am - 12:30 pm | High 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 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session I |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Chemical 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 am | Breakfast |
9:00 am - 12:30 pm | Chemical 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 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session II |
6:00 pm | Dinner |
7:00 pm - 7:30 pm | Business Meeting (Part I) |
| (Nominations for the next Vice Chair; Fill out Conference Evaluation Forms) |
7:30 pm - 9:30 pm | Drug 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 am | Breakfast |
8:30 am - 9:00 am | Business Meeting (Part II) |
| (Vice Chair nominee talks) |
9:00 am - 12:30 pm | High 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 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session II |
6:00 pm | Dinner |
7:00 pm - 7:30 pm | Business Meeting (Part III) |
| (Election of the next Vice Chair; Discuss future Site & Scheduling preferences) |
7:30 pm - 9:30 pm | Frontiers 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 am | Breakfast |
9:00 am | Depart |