The Gordon Research Seminar on Medicinal Chemistry is a unique forum for graduate students, post-docs, and other scientists with comparable levels of experience and education to present and exchange new data and cutting edge ideas in modern drug
Topics will include discussion of concepts of
lead-likeness and also on the impact of chemical structure on physicochemical properties,
pharmacology, pharmacokinetic and toxicology outcomes. The application of
cutting edge technologies to drug discovery programs will also be discussed.
The focus of this meeting is to explore fundamental principles
of contemporary medicinal chemistry coupled with poster presentations
representing the various therapeutic areas and target classes of current
interest in the biotech and pharmaceutical industries. The principles will be
presented in a workshop format, allowing for close interaction between
practicing medicinal chemists and participating attendees. Case studies of drug
discovery projects will highlight successful approaches taken to deliver
clinical candidates. Registration support will be available for
participants; please contact the chair for details.
This GRS was held in conjunction with the "Medicinal Chemistry" Gordon Research Conference (GRC)
. Refer to the associated GRC program page
for more information.
Final Meeting Program
|2:00 pm - 5:00 pm||Arrival and Check-in|
|3:30 pm - 3:45 pm||Introductory Comments by GRC Site Staff / Welcome by the GRS Conference Chair|
|3:45 pm - 5:45 pm||Understanding Drug-Likeness and Medicinal Chemistry Strategies|
|Discussion Leader: Amy Dounay (Colorado College, USA)|
|3:45 pm - 3:55 pm||Introduction by Discussion Leader|
|3:55 pm - 4:25 pm||Thomas Simpson (Boehringer Ingelheim Pharmaceuticals, USA)|
"What Makes a Good Lead?"
|4:25 pm - 4:40 pm||Discussion|
|4:40 pm - 5:10 pm||Mark Tichenor (Janssen Research & Development LLC, USA)|
"Strategies for Lead Optimization"
|5:10 pm - 5:25 pm||Discussion|
|5:25 pm - 5:45 pm||General Discussion|
|7:30 pm - 9:30 pm||Absorption, Distribution, Metabolism, Excretion, and Toxicity|
|Discussion Leader: Srinivasa Karra (EMD Serono Research & Development Institute, USA)|
|7:30 pm - 7:40 pm||Introduction by Discussion Leader|
|7:40 pm - 8:10 pm||Kimberly Cameron (Pfizer, USA)|
"Medicinal Chemistry Lead Optimization: The Use of In Vitro Assays to Solve ADME and Safety Issues"
|8:10 pm - 8:25 pm||Discussion|
|8:25 pm - 8:55 pm||Christopher Smith (COI Pharmaceuticals, USA)|
"Addressing Issues Identified by Second-Tier ADMET Assays"
|8:55 pm - 9:10 pm||Discussion|
|9:10 pm - 9:30 pm||General Discussion|
|9:45 pm - 11:00 pm||Poster Session|
|7:30 am - 8:30 am||Breakfast|
|9:00 am - 11:00 am||Translation into Animal Models|
|Discussion Leader: David Kummer (Janssen, Johnson & Johnson, USA)|
|9:00 am - 9:10 am||Introduction by Discussion Leader|
|9:10 am - 9:40 am||Margaret Chu-Moyer (Amgen, USA)|
"A Medicinal Chemist's Primer on Pharmacokinetics"
|9:40 am - 9:55 am||Discussion|
|9:55 am - 10:25 am||David Price (Pfizer Inc., USA)|
"In Vivo Models and PKPD, First Principles"
|10:25 am - 10:40 am||Discussion|
|10:40 am - 11:00 am||General Discussion|
|11:00 am - 12:30 pm||Poster Session|
|Coffee will be served in the poster area from 11:00 am - 11:30 am|
|1:30 pm - 2:30 pm||Case Studies in Medicinal Chemistry|
|Discussion Leader: Christoph Boss (Actelion Pharmaceuticals Ltd., Switzerland)|
|1:30 pm - 1:50 pm||Kim Huard (Pfizer, USA)|
"Sodium-Coupled Citrate Transporter (NaCT or SLC13A5) Inhibitors for the Treatment of Metabolic Diseases"
|1:50 pm - 1:55 pm||Discussion|
|1:55 pm - 2:15 pm||Patrick Stoy (GlaxoSmithKline, USA)|
"TRPV4 Antagonists: A Case Study in Managing Lipophilicity"
|2:15 pm - 2:20 pm||Discussion|
|2:20 pm - 2:30 pm||Closing Remarks|
|2:30 pm - 3:00 pm||Evaluation Period|
|Fill in GRS Evaluation Forms|
|3:00 pm||Seminar Concludes|