RICT 2007 - Drug Discovery and Selection RICT 07 First Announcement (10/10/2006 - 1255 KB)
04/07/2007
09:40 Successful RNAi-Based Target Discovery Programs in a Wide Range of Human Diseases
Dr. Richard JANSSEN (BIOFOCUS, Leiden, The Netherlands)
Session 1: Target Identification Validation
10:15 Polypharmacology
Dr. Andrew L. HOPKINS (PFIZER GLOBAL R&D, Sandwich, United Kingdom)
10:50 Opening the Gate to Novel Ion Channel Modulators and Innovative Anti-arrhythmics
Dr. Petra BLOM (DEVGEN, Zwijnaarde, Belgium)
11:25 From Compound to Targets to Compounds: The Example of the PPARs
Prof. Bart STAELS (INSTITUT PASTEUR DE LILLE, Lille, France)
12:15 Lunch & poster installation
14:30 Fragment-based Drug Discovery – From Crystal to Clinic
Dr Steve WOODHEAD (TAKEDA CALIFORNIA, San Diego, United States)
Session 2: Hit Generation
15:05 Discovery and Optimisation of Pyrazole Inhibitors of HSP90
Dr. Ted MCDONALD (INSTITUTE FOR CANCER RESEARCH, Sutton, United Kingdom)
15:40 AstraZeneca Compound Collection Enhancement: The Synthesis of ‘Lead-Like’ Libraries
Dr. Jeff STONEHOUSE (ASTRAZENECA R&D CHARNWOOD, Loughborough, United Kingdom)
16:15 Coffee break
16:45 Synthesis and Structure-Activity Relationships of Oral Venous Antithrombotic Thioglycosylated Derivatives
Dr. Véronique BARBEROUSSE (ABBOTT - LABORATOIRE FOURNIER, France)
17:35 Posters and wine
19:05 Closing
20:00 Speakers' reception
05/07/2007
Session 3: Hit-2-Lead; Lead Generation and Selection
08:30 The Synthesis and Activity of New Inhibitors of CDK4 Based on Fascaplysin
Dr. Paul R. JENKINS (UNIVERSITY OF LEICESTER, Leicester, United Kingdom)
09:05 Natural Product Inspired Isoform Selective Histone Deacetylase Inhibitors
Dr. A. GANESAN (UNIVERSITY OF SOUTHAMPTON, Southampton, United Kingdom)
09:40 The Evolution of a Series of Small Molecule Inhibitors of Neutral Endopeptidase
Dr David PRYDE (PFIZER GLOBAL R&D, Sandwich, United Kingdom)
10:15 Coffee break
10:45 The Discovery of AZD0530: A Novel, Oral, Highly Selective SRC Inhibitor with BCR-ABL Activity
Dr Laurent HENNEQUIN (ASTRAZENECA, Reims, France)
11:35 "Paul Ehrlich" lecture
Medicinal Chemistry: a Support to Chemical Biology and a Necessity for Drug Discovery
Dr. Jean-Pierre MAFFRAND (SANOFI-AVENTIS, Toulouse, France)
12:10 Lunch & posters
13:30 Sigma-Aldrich Workshop:
New services for Drug Discovery by Sigma-Aldrich
Dr Scott BATCHELLER (SIGMA-ALDRICH CORPORATION, Milwaukee, United States)
Career Session
This event, with presentations and discussion will run in parallel to the scientific programme
14:10 Early ADMET Tools in Drug Discovery
Mr Marc BERTRAND (TECHNOLOGIE SERVIER, Orleans Cedex, France)
Session 4: Discovery ADMET
14:45 Biotransformation Studies in Drug Discovery Setting - Strategy, Approach and Impact
Dr. Yue-Zhong SHU (BRISTOL-MYERS SQUIBB, Wallingford, United States)
15:20 Coffee break
15:50 The Discovery and Development of a Green Process for Radafaxine
Dr. Trevor J. GRINTER (GLAXO SMITH KLINE, Tonbridge, United Kingdom)
Session 5: Synthetic Chemistry New Frontiers Impacting Drug Discovery
16:25 Ghrelin Ligands: from Design and Synthesis to Clinical Studies
Prof. Jean MARTINEZ (UNIVERSITY OF MONTPELLIER, Montpellier, France)
17:00 Metathesis and Synthesis of Anticancer Agents
Prof. Janine COSSY (ESPCI PARISTECH, Paris, France)
17:35 Posters and wine
19:15 Cocktail
20:30 Gala dinner
06/07/2007
08:30 In Silico / Biological Fingerprinting: the Challenge of Experimental Data to Concepts of Structural and Activity Similarity and Risk Management
Dr. Jonathan MASON (HEPTARES THERAPEUTICS, Welwyn Garden City, United Kingdom)
Session 6: In Silico Tools
09:05 In Silico Predicitions of Cardiovascular Safety - Beyond hERG
Dr. Luca FENU (JOHNSON & JOHNSON PRD, Beerse, Belgium)
09:40 Predicting Metabolic Stability for Xenobiotics
Prof. Gabriele CRUCIANI (UNIVERSITY OF PERUGIA, Perugia, Italy)
10:15 Coffee break
10:45 Long Duration of Action by Design: Discovery of Degarelix, a Self-Depoting GnRH Blocker
Dr. Claudio SCHTEINGART (FERRING RESEARCH INSTITUTE, San Diego, CA, United States)
Session 7: Non Classical Drug Discovery: Breaking the Rules
11:35 Concept and Development of Chimeric Molecules: Somatostatin –Dopamine Chimeras
Dr. Christophe THURIEAU (GROUP IPSEN, Les Ulis, France)
12:15 Therapeutic proteins : Role of Post-Translational Modifications in Structure-Function Relationships. Application to Monoclonal Antibodies and Coagulation Factors
Dr. Laurent SIRET (LFB, Courtabœuf, France)
12:55 Lunch
13:55 From Medicinal Chemistry to New Targets and New Drugs. Discovery of New Antiepileptic Drug Candidates.
Dr Benoit KENDA (UCB, Braine-l'Alleud, Belgium)
Session 8: Non Classical Drug Discovery: Breaking the Rules
14:35 Diarylquinoline, a New Antibiotic, Shuts Mycobacterial Energy Supply
Dr. Anil KOUL (JOHNSON & JOHNSON PHARMACEUTICAL RESEARCH & DEVELOPMENT, Beerse, Belgium)
15:15 Discovery of Eltrombopag, a Small-Molecule Oral Thrombopoietin Receptor Agonist: a Modulator of a Protein-Protein Interaction
Dr. Juan LUENGO (GLAXO SMITH KLINE, Collegeville, United States)
16:05 Closing
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