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Medicinal Chemistry (GRS)
Gordon Research Seminar

Lead Optimization Strategies for Medicinal Chemists

Dates

August 5-6, 2017

Location

Colby-Sawyer College
New London, NH Site Information

Organizers

Chair:
Benjamin A. Pratt

Application Deadline

The application deadline for this meeting was July 8, 2017. You may still submit an application, which may be considered by the conference chair if there is still room available.

Meeting Description

Overview

The Gordon Research Seminar on Medicinal Chemistry is a unique forum for graduate students, post-docs, and other early career scientists with comparable levels of experience and education to learn from experienced medicinal chemists, present and exchange new data and cutting edge ideas.

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.

Application Instructions

The meeting will feature approximately 10 talks and 2 poster sessions. All attendees are expected to actively participate in the GRS either by giving an oral presentation or presenting a poster. Therefore, all applications must include an abstract.

The Chairs will select speakers from abstracts submitted by May 5, 2017. Those applicants who are not chosen for talks and those who apply after the deadline to be considered for an oral presentation will be expected to present a poster. In order to participate, you must submit an application by the date indicated in the Application Deadline section above.

Related Meeting

This GRS will be held in conjunction with the "Medicinal Chemistry" Gordon Research Conference (GRC). Those interested in attending both meetings must submit an application for the GRC in addition to an application for the GRS. Refer to the associated GRC program page for more information.

Contributors

Meeting Program

Saturday
2:00 pm - 5:00 pmArrival and Check-in
3:30 pm - 3:45 pmIntroductory Comments by GRC Site Staff / Welcome by the GRS Conference Chair
3:45 pm - 5:45 pmThe Role of the Medicinal Chemist in Drug Discovery
Discussion Leader: Amy Dounay (Colorado College, USA)
3:45 pm - 3:55 pmIntroduction by Discussion Leader
3:55 pm - 4:25 pmChristopher Smith (COI Pharmaceuticals, USA)
"Introduction to Medicinal Chemistry"
4:25 pm - 4:40 pmDiscussion
4:40 pm - 5:10 pmMark Tichenor (Janssen Research & Development LLC, USA)
"Strategies for Lead Optimization"
5:10 pm - 5:25 pmDiscussion
5:25 pm - 5:45 pmGeneral Discussion
6:00 pmDinner
7:30 pm - 9:30 pmOptimizing for ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity)
Discussion Leader: Mark Mitton-Fry (Ohio State University, USA)
7:30 pm - 7:40 pmIntroduction by Discussion Leader
7:40 pm - 8:10 pmDeidre Johns (Oregon State University, USA)
"Principles of ADMET - Part 1"
8:10 pm - 8:25 pmDiscussion
8:25 pm - 8:55 pmGraeme Freestone (Dart NeuroScience, USA)
"Principles of ADMET - Part 2"
8:55 pm - 9:10 pmDiscussion
9:10 pm - 9:30 pmGeneral Discussion
9:45 pm - 11:00 pmPoster Session
Sunday
7:30 am - 8:30 amBreakfast
9:00 am - 11:00 amAnimal Models for Safety and Efficacy
Discussion Leader: Dustin Mergott (Eli Lilly, USA)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:40 amMichael Ellis (Merck Research Laboratories, USA)
"Pharmacokinetics"
9:40 am - 9:55 amDiscussion
9:55 am - 10:25 amTom Simpson (West Chester University, USA)
"Pharmacodynamics"
10:25 am - 10:40 amDiscussion
10:40 am - 11:00 amGeneral Discussion
11:00 am - 12:30 pmPoster Session

Coffee will be served in the poster area from 11:00 am - 11:30 am
12:30 pmLunch
1:30 pm - 2:30 pmCase Studies in Drug Discovery
Discussion Leader: Amy Ripka (WuXi AppTec, USA)
1:30 pm - 1:55 pmKatherine Lee (Pfizer, USA)
"Lead Generation Strategies for IRAK4"
1:55 pm - 2:00 pmDiscussion
2:00 pm - 2:25 pmErin DiMauro (Merck & Co., USA)
"Discovery of High Quality TNKS Inhibitors via Multidimensional Lead Generation and Optimization"
2:25 pm - 2:30 pmDiscussion
2:30 pm - 3:00 pmEvaluation Period
Fill in GRS Evaluation Forms
3:00 pmSeminar Concludes
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