RICT 2011 - Drug Discovery and Selection
06/07/2011
08:00Registration
09:15Welcome Session
Session 1: Case Studies
Session Chair
Prof. Pascal DUMY
(ECOLE NATIONALE SUPÉRIEURE DE CHIMIE DE MONTPELLIER (ENSCM), Montpellier, France)
09:30Discovery of Riociguat: A Potent, Oral Stimulator of Soluble Guanylate Cyclase for the Treatment of Pulmonary Hypertension
Prof. Joachim MITTENDORF
(BAYER SCHERING PHARMA, Wuppertal, Germany)
10:15Aleglitazar, a Potent and Balanced Dual PPARα/γ Agonist for the Reduction of Cardiovascular Mortality and Morbidity in Patients with Type 2 Diabetes
Dr Peter MOHR
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
11:00Coffee Break
Session Chair
Dr Edmond DIFFERDING
(DIFFERDING CONSULTING, Louvain-la-Neuve, Belgium)
11:30Discovery of Potent and Selective Smoothened Inhibitors for the Treatment of Hedgehog-dependent Tumors
Dr Stefan PEUKERT
(NOVARTIS, Cambridge MA, United States)
12:15Gut-Targeted Microsomal Triglyceride Transfer Protein Inhibitors to Treat Obesity: Design, Clinical Proof of Concept and Novel Chemical Leads
Dr Lieven MEERPOEL
(JANSSEN R&D, Beerse, Belgium)
13:00Lunch and Poster Session
Session 2: From Screening to Development
Session Chair
Prof. Pierre-Alain CARRUPT
(UNIVERSITÉ DE GENÈVE, Geneva 4, Switzerland)
14:30Discovery and Optimization of Kinase Inhibitors: Some Case Studies from GKS3β and IGF1R Inhibitors
Dr Dominique LESUISSE
(SANOFI AVENTIS, Chilly-Mazarin, France)
15:15Discovery and Lead Optimisation of a Novel Series of Highly Potent, Selective and Orally Bioavailable SYK Inhibitors
Dr Neil GARTON
(GLAXOSMITHKLINE, Stevenage, United Kingdom)
16:00Coffee Break and Poster Session
Session Chair
Dr Luc VAN HIJFTE
(JANSSEN RESEARCH & DEVELOPMENT, Nijmegen, The Netherlands)
16:30The Design, SAR and Synthesis of Novel ADAM-TS4 (Aggrecanase-1) Inhibitors for the Treatment of Osteoarthritis
Dr Chris DE SAVI
(ASTRAZENECA R&D, Boston, United States)
17:15Ehrlich Lecture - Title to be announced
Prof. Jean MARTINEZ
(UNIVERSITY OF MONTPELLIER, Montpellier, France)
18:00Final Announcements
18:30Welcome drink sponsored by BIOalternatives
07/07/2011
Session 3: Other Innovative Approaches
Session Chair
Prof. Jens HASSERODT
(ENS, Lyon, France)
09:00Tumor Targeting Using Shiga Toxin: Syntheses and Biological Evaluations of Some Conjugates
Dr Frédéric SCHMIDT
(INSTITUT CURIE, Paris, France)
09:45Folding Oligomers with Predictable Structures and Properties
Dr Ivan HUC
(IECB & CNRS - UNIVERSITÉ DE BORDEAUX, Bordeaux, France)
10:30Coffee Break and Poster Session
Session 3: Other Innovative Approaches (Fol.)Session 4: In Silico Approaches
Session Chair
Dr Pascal GEORGE
(SCT & INDEPENDENT SCIENTIFIC EXPERT & ADVISER, Longvilliers, France)
11:00Fragment-based Engineering of Protein-ligand Interactions Using NMR and Other Biophysical Methods : Towards Tailor-made Drugs
Prof. Jean-Marc LANCELIN
(CPE, VILLEURBANNE Cedex, France)
11:45Template Assembled Functional Biomolecules : Chemistry, Characterization and Validation as a Paradigm for Tailor Made Molecular Medicine
Prof. Pascal DUMY
(ECOLE NATIONALE SUPÉRIEURE DE CHIMIE DE MONTPELLIER (ENSCM), Montpellier, France)
Session Chair
Dr Solo GOLDSTEIN
(INSTITUT DE RECHERCHES SERVIER, Suresnes, France)
11:00How can Computers Support Drug Discovery? In Silico Approaches for Anticipating Bioactivity Spectra, Analysing Adverse Drug Reactions and Predicting Ligand Activity Against Particular Protein Mutants
Prof. Andreas BENDER
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
11:45A Journey in Data and Chemical Spaces: Application to Pharmaceutical Sciences
Dr Philippe VAYER
(LABORATOIRE SERVIER, Orléans, France)
12:30Lunch and Poster Session
Session 5: Hit to LeadSession 6: Fluorine in Medicinal Chemistry
Session Chair
Dr Olivier LAVERGNE
(., Les Ulis, France)
14:00The Mitotic Kinesin Eg5 as a Target for Drug Development in Cancer Chemotherapy: from Inhibitor Screening to in vivo Models
Prof. Frank KOZIELSKI
(BEATSON INSTITUTE FOR CANCER RESEARCH, Glasgow, United Kingdom)
14:45Proteomic Studies as a Guide in the Development of New Cyclin-dependent Kinase Inhibitors
Prof. Hervé GALONS
(SCT & PARIS DESCARTES UNIVERSITY, Paris, France)
Session Chair
Dr Frédéric DOLLE
(CEA, SERVICE HOSPITALIER FRÉDÉRIC JOLIOT, Orsay, France)
14:00A Brief Guide to Fluorine-Protein Interactions for the Medicinal Chemist
Dr Jérôme AMAUDRUT
(ABBOTT-LABORATOIRE FOURNIER, Daix, France)
14:45Difluoromethylbenzoxazole (DFMB)Pyrimidine Thioether Derivatives: A Novel Class of Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
Dr Maurice MEDEBIELLE
(UNIVERSITÉ CLAUDE BERNARD LYON 1, Villeurbanne, France)
15:30Coffee Break and Poster Session
Session 5: Hit to Lead (Fol.)Session 6: Fluorine in Medicinal Chemistry (Fol.)
Session Chair
Mr Jean-Claude FLORENT
(INSTITUT CURIE, Paris, France)
16:15KCC2 : a New Target for Epilepsy?
Dr Cécile PEGURIER
(UCB PHARMA, Braine-L'Alleud, Belgium)
17:00New Multivalent Glyco-vaccines: Molecular Engineering of the Regiospecificity of Transglucosidases for Chemo-enzymatic Oligosaccharide Synthesis
Prof. Pierre MONSAN
(INSA, Toulouse, France)
Session Chair
Dr Pascal GEORGE
(SCT & INDEPENDENT SCIENTIFIC EXPERT & ADVISER, Longvilliers, France)
16:15Synthesis of Radiolabelled Probes for Positron Emission Tomography: The Link Between Molecular Imaging and Medicinal Chemistry
Dr Frédéric DOLLE
(CEA, SERVICE HOSPITALIER FRÉDÉRIC JOLIOT, Orsay, France)
17:45Final Announcements
20:00Gala Dinner
08/07/2011
Session 7: New Strategies, Tools and Platforms
Session Chair
Prof. Peter GOEKJIAN
(UNIVERSITE DE LYON, Villeurbanne Cedex, France)
09:00Accessing Libraries of Highly Antitumor Active Ansamycin Antibiotics by Semi- and Mutasynthesis
Prof. Andreas KIRSCHNING
(LEIBNIZ UNIVERSITY, Hannover, Germany)
09:45Development of Enantiomers: the Example of Chiral Sulfoxides
Dr Philippe PITCHEN
(FOREST RESEARCH INSTITUTE, Hauppauge, United States)
10:30Coffee Break and Poster Session
11:00Poster Awards
Session 7: New Strategies, Tools and Platforms (fol)
Session Chair
Dr Michel PEREZ
(PIERRE FABRE, Toulouse, France)
11:30Non-Denaturing Chemical Proteomics for Protein Complex Isolation and Identification
Dr Alain WAGNER
(UNIVERSITÉ DE STRASBOURG, Illkirch, France)
12:15Mentzer Lecture - DNA-Encoded Chemical Libraries: a New Tool for Drug Discovery
Prof. Dario NERI
(ETH ZÜRICH, Zürich, Switzerland)
13:00Final Conclusions
13:15Lunch
<Previous page


Organised by

In association with

With the support of

Media partners