08:00
09:00
Session 1: Case Studies (Kinase)
Session Chairman
Dr Pascal GEORGE
SCT & INDEPENDENT SCIENTIFIC EXPERT & ADVISER, Longvilliers, France
09:15
Translating Structural-biology & Preclinical Activity of Nilotinib into Efficacy in Leukemia Patients
Dr Paul W. MANLEY
NOVARTIS PHARMA, Basel, Switzerland
Executive Director / Novartis Leading Scientist. Dr. Paul W. Manley received his Ph.D. in Organic Chemistry from Liverpool University. He has over 30 years of medicinal chemistry experience in the pharmaceutical industry, across several therapeutic areas. Since year 2000, he has been engaged in the discovery and development of drugs to treat haematological malignancies, with the invention of nilotinib (Tasigna®), marketed worldwide for the treatment of chronic myelogenous leukemia, being a significant achievement.
He has published over 110 scientific papers on leukaemia and oncology drugs, medicinal and organic chemistry, and is co-inventor of over 60 patents.
10:00
Matched Triplicate Design Sets in the Optimisation of a New Series of Glucokinase Activators
Prof. Mike WARING
ASTRAZENECA, Newcastle upon Tyne, United Kingdom
Mike is a medicinal chemist working for AstraZeneca in CVGI at Alderley Park. Mike received his degree (chemistry, 1996) and PhD (organic chemistry, 2000) from The University of Manchester working with Tim Donohoe then carried out post doctoral work at The University of Texas at Austin with Prof Phil Magnus working on The Total Synthesis of Guanacastepene. Mike then joined AstraZeneca at Alderley Park in 2001 and has worked in both cancer and CVGI, delivering 11 compounds into development including the glucokinase activator AZD1656. He is the winner of the 2010 Royal Society of Chemistry Capps-Green-Zomaya medal for outstanding contributions to medicinal chemistry and the 2010 runner up of the European Federation for Medicinal Chemistry award for an outstanding young medicinal chemist in industry. Mike is the author of 18 published papers, 21 patents and one book, he is also a member of the scientific advisory board for Medicinal Chemistry Communications (Royal Society of Chemistry). Mike is currently a Principal Scientist in CVGI Medicinal Chemistry at Alderley Park.
10:45
Session 2: Non Classical Drugs
Session Chairman
Dr Samir JEGHAM
SANOFI R&D, MONTPELLIER, France
11:15
Synthetic Carbohydrates in the Search for Tailor-made Antibacterial Vaccines: Shigellosis as a Challenge
Dr Laurence MULARD
PASTEUR INSTITUTE, Paris, France
Laurence A. Mulard graduated as an engineer from the Ecole Supérieure de Physique et Chimie Industrielles (ESPCI, Paris, France) and completed her MSc at the Université Pierre et Marie Curie (Paris, France) in 1988. She received her PhD in chemistry from the same University (1991) working under the supervision of Prof. Czernecki. After three postdoctoral years at the National Institutes of Health (NIH, Bethesda, MD, USA) studying glycochemistry in the group of Dr Glaudemans, she joined the Institut Pasteur (Paris, France) as research assistant. Involved in the field of glycosciences, she received her “Habilitation” in 2003 and was promoted Senior Scientist in 2007, while acting as Head of the Unité de Chimie Organique. In 2008, she was appointed Head of the Unit “Chemistry of Biomolecules” at the Institut Pasteur. Her research interests are in the area of chemical biology with focus on carbohydrates and glycoconjugates in relation to diseases and biological recognition. Major investigations are on polysaccharide antigen/antibody interactions by use of synthetic chemistry in combination with structural, physicochemical and immunochemical analysis. Current focus is on the identification and synthesis of well-defined mimics of selected bacterial polysaccharides – and conjugates thereof – for the development of novel carbohydrate-based vaccines.
12:00
Bicyclic Peptide Antagonists Isolated From Phage Display Libraries
Prof. Christian HEINIS
ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE (EPFL), Lausanne, Switzerland
Christian Heinis is a Tenure-track Assistant Professor at the Institute of Chemical Sciences and Engineering (ISIC) of the Ecole Polytechnique Fédérale de Lausanne (EPFL) in Switzerland.
The research goal of Christian Heinis is the development of novel and innovative therapeutic strategies. A main focus is the engineering of bicyclic peptides binding to disease targets using phage display and the testing of their therapeutic potential in vitro and in vivo.
Christian Heinis had studied biochemistry at the Swiss Federal Institute of Technology in Zurich (ETHZ) where he also did a PhD in the research group of Prof. Dr. Dario Neri. He was a postdoctoral fellow in the group of Prof. Dr. Kai Johnsson at the EPFL and in the group of Sir Gregory Winter at the Laboratory of Molecular Biology (LMB) in Cambridge, UK. In 2008 he was appointed Assistant Professor with tenure track for Bioorganic Chemistry at EPFL and since 2009 he is holding a professorship of the Swiss National Science Foundation. Christian is a scientific founder of the start-up company Bicycle Therapeutics.
12:45
Lunch and Poster Presentation
Session Chairman
Prof. Vincent LISOWSKI
UNIVERSITÉ DE MONTPELLIER 1, Montpellier, France
14:15
A Look at Some Innovative Chemical Aspects in Medicinal Chemistry, about Heterocycles, Microwaves, Chemical Libraries, Boronics and Garlands
Paul Ehrlich Prize Lecture
Prof. Sylvain RAULT
UNIVERSITÉ DE CAEN, Caen Cedex, France
Sylvain RAULT- Pharmacist 1975, Docteur d’Etat es Sciences ( Organic chemistry) 1982
Professor of Medicinal Chemistry –Faculty of Pharmacy- University of Caen -1986 ….
Director of CERMN - Centre d’Etudes et de Recherche sur le Médicament de Normandie - 1998- 2011
Assistant Director of the French Chemical librairy - 2003 …
Current area of research in organic chemistry: Synthesis of heterocyclic compounds oriented by diversity and drugability, organization of chemical librairies, exploration of new areas of the chemical field. Synthesis of boronic species and their use for the preparation of garlands as new foldamers. Main domains of application in medicinal chemistry: cancerology ( PPI’s) and neurosciences ( 5-HT)
Other position: French Ministry of Environment: President of the “ Commission des produits chimiques et biocides, CPCB ” 2003….
Session 3: Targeted Therapies
Session Chairman
Prof. Jean-Pierre GESSON
UNIVERSITÉ DE POITIERS, Poitiers, France
15:00
Squalenoyl Nanomedicines as Potential Therapeutics
Dr Didier DESMAËLE
UNIVERSITÉ PARIS SUD, Châtenay-Malabry, France
Didier Desmaële earned his PhD at the University P&M Curie (Paris, France) in 1984, working on the total synthesis of cholecalciferol. After a post-doctoral research position at Yale University in the group of Professor S. L. Schreiber, he was appointed scientist at the CNRSand he moved to the Ecole de Chimie & Physique de la Ville de Paris, where he developed new asymmetric synthesis methodologies. In 1992, he moved to the school of Pharmacy of Université Paris-Sud and took the position of head of team within the CNRS research unit BIOCIS. His main interests were total synthesis of natural products, asymmetric synthesis and medicinal chemistry. Since 1998 he is highly involved in in the design of new drug delivery systems. In January 2011, he joined the CNRS research unit UMR 8612 “Physico-chimie, Pharmacotechnie et Biopharmacie” at the University Paris Sud. His current research activities focus on the design and the synthesis of bioconjugates for nanoparticular drug delivery.
15:45
Coffee Break and Poster Session
Session Chairman
Prof. Jean-Pierre GESSON
UNIVERSITÉ DE POITIERS, Poitiers, France
16:15
Protein-binding Prodrugs and Drug Conjugates in Oncology: From Design, Applications to Combination Therapy
Prof. Felix KRATZ
TUMOR BIOLOGY CENTER, Freiburg, Germany
The Division Macromolecular Prodrugs was founded in 1994 by Dr. Felix Kratz in the Clinical Research Department at the Tumor Biology Center, Freiburg, Germany. Felix Kratz graduated in Chemistry from the University of Heidelberg in 1991. The primary goal of his research team is the development of novel drug delivery concepts for improving the efficacy and toxicity of anticancer agents. He has 20 years of experience in the preclinical development of anticancer drugs and profound knowledge of translational research from the laboratory to the clinic and has successfully transferred a first albumin-binding doxorubicin prodrug (INNO-206) into the clinic which is currently undergoing phase II trials. His research areas are drug targeting, drug delivery systems, prodrugs, receptor targeting, bioconjugate chemistry, polymer therapeutics and nanocarriers. He has authored approximately 240 scientific publications, book articles and proceedings and is the inventor or co-inventor of 28 patents and patent applications.
17:00
Potent Antibody Drug Conjugates for Cancer Therapy: From the Lab to a Clinically Approved Drug
Dr Peter SENTER
SEATTLE GENETICS, Bothell, United States
Peter Senter is the Vice President of Chemistry at Seattle Genetics. He has been with the company for 13 years, shortly after it was founded. Dr. Senter initiated and led the antibody drug conjugate (ADC) program that resulted in the recent approval of ADCETRIS, an ADC that recognizes the CD30 antigen on Hodgkin lymphoma and anaplastic large cell lymphoma. His group has focused attention on all aspects of ADC technology, starting with the development of highly potent cytotoxic drugs, conditionally labile linkers, conjugation technologies, antibody engineering, and ADC biology. Dr. Senter also serves as the Senior Editor for Bioconjugate Chemistry and is an Adjunct Professor in the Department of Bioengineering at the University of Washington in Seattle. He received an A.B. degree in Biochemistry from the University of California at Berkeley, a PhD in Chemistry from the University of Illinois in Urbana, and did postdoctoral research at the Max Planck Institute for Experimental Medicine in Göttingen, Germany. Prior to joining Seattle Genetics, Dr. Senter held various positions at the Dana Farber Cancer Institute, Bristol Myers Squibb Pharmaceutical Research Institute, and Cytokine Networks. His research interests include targeted drug delivery, protein chemistry, and the design of novel chemotherapeutic agents.
17:45
18:00
Booster Presentations Exhibitors