RICT 2008 - Drug Discovery and Selection
01/07/2009
08:00Registration
09:15Welcome Session
Prof. André TARTAR (UNIVERSITY LILLE 2, Lille, France)
Prof. Gérald GUILLAUMET (UNIVERSITÉ D'ORLÉANS, Orléans, France)
First Session: In Silico Selection
Session Chair:
Prof Luc MORIN-ALLORY
(UNIVERSITY OF ORLEANS, Orléans, France)
09:30Navigation in Chemistry Universe Towards Biological Activity
Dr Peter ERTL
(NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
10:15Structure-Based in Silico Screening: Free Tools and Applications
Dr. Bruno VILLOUTREIX
(INSERM - UNIVERSITY PARIS DIDEROT, Paris, France)
Second Session: From Target Identification to Development
Session Chair:
Dr Philippe PITCHEN
(FOREST RESEARCH INSTITUTE, Hauppauge, United States)
11:00The Therapeutic Potential of Pharmacological Inhibitors of Cyclin-Dependent Kinases
Dr Laurent MEIJER
(CNRS - ROSCOFF, Roscoff, France)
11:45Targeted Small Molecule Anti-Cancer Drugs: an Asian Perspective from Discovery to Clinical
Dr. Stéphanie BLANCHARD
(S*BIO, Singapore, Singapore)
12:30Lunch and Poster Session
12:30Career Session in parallel From 12:30 till 16:00
Second Session: From Target Identification to Development (Fol.)
Session Chair:
Dr Luc VAN HIJFTE
(JANSSEN CILAG, Val de Reuil, France)
14:30Selective Inhibitors of MMP-12 : from Chemistry to Therapeutic Applications
Dr. Vincent DIVE
(CEA, Gif-sur-Yvette, France)
15:15Discovery of the Macrocyclic HCV Protease Inhibitor TMC435350
Dr Pierre RABOISSON
(JANSSEN INFECTIOUS DISEASES, Beerse, Belgium)
16:00Coffee Break and Poster Session
Session Chair:
Dr Solo GOLDSTEIN
(INSTITUT DE RECHERCHES SERVIER, Suresnes, France)
16:30Irreversible Serine Protease Inhibitors: Useful Tools in Drug Discovery
Prof. Koen AUGUSTYNS
(UNIVERSITY OF ANTWERP, Antwerp, Belgium)
17:15« Paul Ehrlich» Lecture: Discovery of Xarelto, a Novel, Oral Antithrombotic Agent
Dr. Susanne ROEHRIG
(BAYER SCHERING PHARMA, Wuppertal, Germany)
18:00« Paul Ehrlich» Lecture Award
Prof. Gérald GUILLAUMET (UNIVERSITÉ D'ORLÉANS, Orléans, France)
Prof. André TARTAR (UNIVERSITY LILLE 2, Lille, France)
19:30Welcome Cocktail at Hôtel Groslot (Offered by Mr. Serge Grouard, the Mayor of Orléans)
02/07/2009
Third Session: Interfacing Chembio and MedchemFifth Session: Imaging
Session Chair:
Dr. Grégoire PREVOST
(GROUP IPSEN, Les Ulis, France)
08:30GLP-1 Analog Taspoglutide: Design, Synthesis and Biological Activity
Dr. Jesse DONG
(IPSEN, Milford, United States)
09:15Experiences in Fragment Based Lead Discovery
Prof. Rod HUBBARD
(UNIVERSITY OF YORK / VERNALIS, York, United Kingdom)
10:00Coffee Break and Poster Session
Session Chair:
Prof. Gerard DELERIS
(UNIVERSITY BORDEAUX SEGALEN, Bordeaux, France)
10:30Using Knowledge from NBEs to Inform Drug Design
Dr. Alastair LAWSON
(UCB CELLTECH, Slough, United Kingdom)
11:15Diversity Oriented Synthesis of Natural Product Motifs
Prof. Nicolas WINSSINGER
(UNIVERSITY OF STRASBOURG, Strasbourg, France)
12:00Lunch and Poster Session
Session Chair:
Dr Jean-Philippe ROCHER
(ADDEX THERAPEUTICS, Plan-les-Ouates, Switzerland)
08:30Facilitating Drug Development with PET Imaging
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
09:15Targeting G-Protein Coupled Receptors with Radiolabeled Peptides for the Molecular Imaging and Targeted Therapy of Cancer
Dr. Helmut MAECKE
(UNIVERSITY HOSPITAL, Basel, Switzerland)
10:00Coffee Break and Poster Session
Session Chair:
Dr. Jean Claude BELOEIL
(CNRS UPR 4301, Orléans, France)
10:30PET Imaging in Drug Discovery and Development of CNS Drugs
Dr. Jose Ignacio ANDRES
(JOHNSON & JOHNSON PHARMACEUTICAL R & D, Toledo, Spain)
11:15Modified Selective Integrin Ligands for Cancer Therapy, Molecular Imaging and for Improvement of Biomaterials
Dr Horst KESSLER
(TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany)
12:00Lunch and Poster Session
Fourth Session: Synthesis and Lead OptimizationSixth Session: High Throughput Screening and Lead Identification
Session Chair:
Prof. Christiane GARBAY
(UNIVERSITÉ PARIS 5, Paris, France)
14:00Discovery of Potent, Selective and Orally Bioavailable DP2 Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases
Dr. Stefano CROSIGNANI
(MERCK-SERONO PHARMACEUTICAL RESEARCH INSTITUTE, Plan-les-Ouates, Switzerland)
14:45Dynamic Combinatorial Chemistry in Chemical Biology and Drug Discovery
Prof. Jean-Marie BEAU
(UNIVERSITÉ PARIS SUD 11, Orsay, France)
15:30Development of Marine Anticancer Drugs
Dr. Andrès FRANCESCH
(PHARMAMAR, Colmenar Viejo, Spain)
16:15Coffee Break and Poster Session
Session Chair:
Ing Michel CALDERINI
(MERCK, Darmstadt, Germany)
17:00A Chemistry-Driven Approach to the Discovery of New Calcium-Sensing Receptor Ligands and Antimitotic Agents
Dr. Robert H. DODD
(ICSN CNRS, Gif-Sur-Yvette, France)
17:45Knowledge management, prospective design and chemical enablement as strategies for lead optimization: The PDE-9 inhibitor and opiate antagonist case studies.
Dr. Spiros LIRAS
(PFIZER GLOBAL RESEARCH, Groton, United States)
Session Chair:
Prof. Sylvain RAULT
(CERMN, Caen, France)
14:00Generation of New Active Compounds in an Industrial-Academic Screening Organization
Dr. Frederic AUSSEIL
(INSTITUT DE RECHERCHE PIERRE FABRE, Toulouse, France)
14:45New Strategies in Chemical Biology : Scientific and Therapeutic Outcome
Prof. Marcel HIBERT
(UNIVERSITÉ DE STRASBOURG, Illkirch, France)
15:30The Crystal Structure of the Adenosine A2A Receptor - Implications for GPCR Drug Design
Prof. Ad P. IJZERMAN
(UNIVERSITY OF LEIDEN, Leiden, The Netherlands)
16:15Coffee Break and Poster Session
Session Chair:
Dr Pascal GEORGE
(SANOFI-AVENTIS R&D, Longvilliers, France)
17:00Aptamers: Oligonucleotides that Rival Antibodies for Therapeutics and Diagnostics.
Prof. Jean-Jacques TOULME
(IECB & INSERM - UNIVERSITÉ BORDEAUX II, Bordeaux, France)
17:45Recent Developments in Structural Biology: Applying Crystallographic and NMR Approaches in Lead Finding and Optimization
Dr Vincent MIKOL
(SANOFI AVENTIS, Vitry-sur-Seine, France)
18:30End of Conference
18:45Departure to Gala Dinner
03/07/2009
Fourth Session: Synthesis and Lead Optimization (fol.)
Session Chair:
Dr Françoise GUERITTE
(INSERM - CNRS, Gif-sur-Yvette, France)
09:00Taking up the Adme Challenge
Prof. Benoit DEPREZ
(UNIVERSITY OF LILLE 2, Lille, France)
09:45Discovery of Novel Potent, Selective and Orally Efficacious A2B Adenosine Receptor Antagonists.
Dr. Bernat VIDAL
(LABORATORIOS ALMIRALL, Barcelona, Spain)
10:30Coffee Break and Poster Session
Session Chair:
Prof Chris KRUSE
(ABBOTT, Weesp, The Netherlands)
11:00New Synthetic Methods and their Application to the Preparation of Biologically Active Molecules
Prof. Mike SHIPMAN
(UNIVERSITY OF WARWICK, Coventry, United Kingdom)
11:45« Prix Charles Mentzer »: From Heparin to New Anticoagulants with Unprecedented Pharmacological Profile
Dr. Maurice PETITOU
(ENDOTIS PHARMA, Romainville, France)
12:30« Prix Charles Mentzer » Award
Prof. Gérald GUILLAUMET (UNIVERSITÉ D'ORLÉANS, Orléans, France)
Prof. André TARTAR (UNIVERSITY LILLE 2, Lille, France)
12:35Lunch and Poster Session
Seventh Session: Biophysics Tools and ADME Tox
Session Chair:
Dr Bruno FIGADERE
(UNIVERSITÉ PARIS-SUD, Chatenay-Malabry, France)
14:00Biophysical Approaches in the Hit-to-Lead Optimisation Strategy
Dr. Jean BOUTIN
(INSTITUT DE RECHERCHES SERVIER, Croissy-sur-Seine, France)
14:45ADME-PK Optimization Strategies in Drug Discovery and Selection
Dr. Sonia POLI
(ADDEX PHARMA, Plan-les-Ouates, Switzerland)
15:30Poster Prizes
16:00Conclusions
Prof. Gérald GUILLAUMET (UNIVERSITÉ D'ORLÉANS, Orléans, France)

Prof. André TARTAR (UNIVERSITY LILLE 2, Lille, France)
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