EFMC-ISMC 2012

Plenary Lecture
Umpolung and the Art of Innovation

Youssef BENNANI

VERTEX PHARMACEUTICALS, Laval (Quebec), Canada
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Youssef BENNANI

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Youssef L. Bennani is currently VP-R&D, Vertex Pharmaceuticals (Canada) Inc. He previously served as Vice-President of Drug Innovation (Integrated Discovery chemistry and DMPK) at Vertex Pharmaceuticals in Cambridge, MA, USA for 7 years. Over the past ~20 years, he successfully led several of research programs in therapeutic areas such as neurology, metabolism, immunology, infection [bacterial, viral and fungal], and oncology, delivering more than 25 new molecular entities reaching various stages of pre-clinical, human clinical development and market stages. To date he communicated over 125 publications and is an inventor on more than 50 patents. His education consists of a Doctorate degree (PhD) in chemistry from Universite de Montreal (S. Hanessian), and post-doctoral studies The Scripps Research Institute (K. B. Sharpless), in La Jolla; as well as a MBA from LFGSM, in Chicago.

Plenary Lecture
The Future of Medicinal Chemistry

Hans-Joachim BÖHM

HOFFMANN-LA ROCHE, Basel, Switzerland
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Hans-Joachim BÖHM

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Hans-Joachim Böhm is Global Head of Chemistry at Roche and Center Manager for the Roche Pharma Research and Early Development Site Basel. Prior to this, Hans-Joachim Böhm was President and Research Site Head of Roche Palo Alto from 2006 to 2008. Hans-Joachim Böhm also headed Non-clinical Development at Roche Basel from 2005 - 2006, the Discovery Chemistry Department from 2002 - 2004, the Discovery Technology Department from 2000 - 2001 and the Research Informatics Department in Basel. Before joining Roche in 1996, Hans-Joachim Böhm worked for BASF in Ludwigshafen as Computational Chemist from 1988 - 1996 and for Siemens in Munich in field of Microelectronics from 1985 - 1987. He obtained his Ph.D. in Theoretical Chemistry at the University of Karlsruhe in 1984.

Berlin: The Dynamic Science Metropole Responds to Challenges and Opportunities of the 21st Century

Günter STOCK

HEALTH CAPITAL BERLIN BRANDENBURG, Berlin, Germany
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Günter STOCK

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Prof. Dr. Dr. Günter Stock, President of the Berlin-Brandenburg Academy of Sciences and Humanities and of the Union of the German Academies of Sciences and Humanities. Trained in medicine, research at the University in Heidelberg on “The limbic system” especially nucleus amygdalae. From 1983 to 2005 responsible for research and development in the pharmaceutical industry, Schering AG, Berlin, from 1989 to 2005 as member of the board of directors. Member of various scientific and supervisory boards.

Opening Lecture
Can Structure Lead to Better Antibiotics?

Ada YONATH

WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel
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Ada YONATH

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Ada Yonath is a Weizmann Institute of Science (WIS) Kimmel Professor for Structural biology, who determined the ribosome three-dimensional structure and showed how antibiotics paralyze it. She graduated the Hebrew University, earned PhD at WIS, postdoced at Carnegie-Mellon University and MIT and spent a sabbatical year at the University of Chicago. She has been and still is directing the Kimmelman Center for Biomolecular Structure at WIS since 1988. In parallel, during 1980-1986 she has been a visiting scientist at the Max-Planck-Institute for Molecular Genetics in Berlin, and during 1986-2004 she also headed Max-Planck-Research-Unit in Hamburg, Germany.

The Prous Institute-Overton & Meyer Award for New Technologies in Drug Discovery Lecture
Fragment-Based Drug Discovery - a Decade of Thinking Small

Harren JHOTI

ASTEX THERAPEUTICS, Cambridge, United Kingdom
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Harren JHOTI

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Dr Harren Jhoti is President and co-Founder of Astex Pharmaceuticals, an integrated biotechnology company that has pioneered Fragment-Based Drug Discovery over the last decade. As the initial Founding Chief Scientific Officer of Astex, and in his subsequent roles as CEO and now President, Dr. Jhoti has been a key innovator in the development of this drug discovery technology. He has also received several awards including being named a ‘Technology Pioneer’ by the World Economic Forum in 2005 and as the ‘Chemistry World Entrepreneur of the Year’ by the Royal Society of Chemistry in 2007. This has resulted in Dr. Jhoti having been featured by TIME magazine and CNBC. Before setting-up Astex in 1999, Dr. Jhoti was previously Head of Structural Biology and Bioinformatics at GlaxoWellcome in the UK (1991-1999). He obtained his BSc and PhD Degrees from London University (1981-1989) and performed post-doctoral research at Oxford University (1989-1991).

The UCB-Ehrlich Award for Excellence in Medicinal Chemistry Lecture
New Derivatives and Stereoisomers of Fenoterol: a Versatile Tool to Stimulate The B2 Adrenergic Receptor with Novel Therapeutical Perspectives

Krzysztof JOZWIAK

MEDICAL UNIVERSITY OF LUBLIN, Lublin, Poland
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Krzysztof JOZWIAK

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Professor Krzysztof Jozwiak is Head of the Laboratory of Medicinal Chemistry and Neuroengineering of Medical University of Lublin, Lublin, Poland. Following graduation in 2000 he was a postdoctoral fellow in the Gerontology Research Center at National Institutes of Health USA, under the supervision of Irving W. Wainer. In 2005 he started his second postdoc in the International Institute of Molecular and Cell Biology in Warsaw in prof. Slawomir Filipek group. In late 2007 he assumed the Associate Professor position at the Medical University of Lublin. Prof. Jozwiak’s main research interests focus on elucidation of molecular mechanisms of interactions between medicinal molecules and their protein targets, development of new methods for both experimental and theoretical characterization of drug-receptor interactions and their applications in medicinal chemistry projects.

Nauta Award for Pharmacochemistry Lecture
Targeting IRS1/2 and Targeting the Immune System to Eradicate Metastatic Tumors as New Modalities of Cancer Therapy

Alexander LEVITZKI

HEBREW UNIVERSITY OF JERUSALEM, Jerusalem, Israel
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Alexander LEVITZKI

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Levitzki started with Cu(II) polyhistidine as a model oxidase and the validation of the induced fit hypothesis, on Concanavalin A. Later he worked on negative cooperativity and allosteric regulation of enzymes. In the 1970s Levitzki switched to signal transduction, pioneering the radiorecptor assay for beta-adrenergic receptors (1974) and the identification of the beta-adrenergic protein by affinity labeling (1978), the mode of coupling of receptors with adenylyl cyclase (1978) and the receonstitution of the beta-adrenergic receptor dependent adenylyl cyclase from purified components. In 1988 he pioneerd the field of signal transduction therapy, using selective tyrosine phosphorylation inhibitors (tyrphostins/TKIs) against EGFR, Her2,PDGFR,Jak2 followed by the development of targeted delivery of long chain dsRNA to cancer (2002 onwards).He is currently Professor of Biochemistry at the Hebrew University, heading the Unit of Cellular Signaling, continuing his research on signal transduction in cancer.

EFMC Prize for a Young Medicinal Chemist in Industry
Minimising CNS Side Effects: DMPK Considerations in the design of Drugs with Limited Brain Penetration

Sharan BAGAL

PFIZER NEUSENTIS, Cambridge, United Kingdom
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Sharan BAGAL

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Sharan K. Bagal received her MChem in 2001 from the University of Oxford, where she subsequently completed her DPhil in chemistry in 2004 under the supervision of Professor Sir Jack Baldwin and Dr. Robert Adlington in the field of biomimetic natural product synthesis. Sharan then moved to Professor Samir Zard’s group at the École Polytechnique in France as a postdoctoral researcher studying xanthate-based radical chemistry. In 2006 she joined Pfizer Global Research and Development, Sandwich, UK as a medicinal chemist and is now a Senior Principal Medicinal Chemist at Pfizer Neusentis in Cambridge, UK. Her research interests encompass all aspects of medicinal chemistry, related in particular to protein kinases and ion channels where she has been directly involved in the invention of two compounds currently undergoing clinical trials. She also has a particular interest in the design of compounds that penetrate, or are restricted from, the central nervous system and has delivered several reviews and presentations in this area. Sharan has co-authored more than 15 papers and patents.

EFMC Prize for a Young Medicinal Chemist in Academia
Developing Inhibitors of the Bromodomain-acetyl-lysine Interaction

Stuart CONWAY

UNIVERSITY OF OXFORD, Los Angeles, United States
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Stuart CONWAY

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Stuart Conway is a Lecturer in Chemistry at the University of Oxford and the Fellow in Organic Chemistry at St Hugh’s College, Oxford. He studied Chemistry with Medicinal Chemistry at the University of Warwick before undertaking PhD studies with Prof. David Jane at the University of Bristol. Stuart completed post-doctoral studies with Prof. Andrew Holmes FRS at the University of Cambridge working on the synthesis of inositol polyphosphates. In 2003, Stuart was appointed as a Lecturer in Bioorganic Chemistry at the University of St Andrews and in 2008 he took up his current position. Stuart’s research focuses on the development of molecular tools to enable the study of biological systems. Recently this has included the synthesis of molecules to aid the study intracellular calcium signaling, wavelength-orthogonally caged neurotransmitters and the development of bromodomain inhibitors.

IUPAC Richter Prize Lecture
Design and Synthesis of Drug Prototypes Inspired by Natural Products

Stephen HANESSIAN

UNIVERSITY OF MONTREAL, MONTREAL, QC, Canada
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Stephen HANESSIAN

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http://osiris.corg.umontreal.ca

Stephen Hanessian obtained his Ph.D. degree at the Ohio State University. After seven years at the Parke-Davis Research Laboratories in Ann Arbor, Michigan, he accepted a faculty position at the University of Montreal where he has held the McConnell and NSERC Medicinal Chemistry chairs. His research interests are in organic, bioorganic, and medicinal chemistry. He has published over 500 papers and 45 patents on aspects of total synthesis of natural products, asymmetric synthesis, design and synthesis of medicinally important compounds, supramolecular assemblies, carbohydrates, reagent design and methodology, and computer assisted organic synthesis. He is the recipient of numerous awards including the A.C. Cope Scholar (1996), C. S. Hudson (1982), and M. L. Wolfrom (1993) awards from the American Chemical Society, the Gold Medal from the National Science and Engineering Council of Canada (1996), and the Killam Memorial Prize for natural sciences (1997). He is the first recipient of the Alfred Bader (Aldrich) award (1988), and the Bernard Belleau Award in Medicinal Chemistry (2001) from the Canadian Society for Chemistry. He received the Chemical Institute of Canada Palladium medal in 1988. In 1998 he was elected as Officer of the Order of Canada. He is one of the 2002 recipients of the Queen Elisabeth Golden Jubilee medal. In 2008, he was elected Foreign Member of the National Academy of the National Academy of Sciences of the Republic of Armenia. In February 2011 he received the first Prize of excellence in Science from the FRQNT (Québec) and he was recently honored with the 2012 Ernest Guenther Award from the American Chemical Society, the IUPAC Richter Prize in Medicinal Chemistry, 2012 (announced) and the Montreal Invivo Prize for innovation, 2012. Professor Hanessian holds joint appointments in the Departments of Chemistry, Pharmaceutical Sciences, and Pharmacology at the University of California, Irvine. He is also the Director of the Medicinal Chemistry and Pharmacology Graduate Program at UCI. He presently holds the Isis Pharmaceuticals Research Chair at the University of Montreal. Website: http://osiris.corg.umontreal.ca

Young Investigator Prize by DPhG and GDCh

Christian OTTMANN

MAX-PLANCK SOCIETY, Eindhoven, The Netherlands
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Christian OTTMANN

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Current title and position: Dr. Christian Ottmann, Group leader at the Chemical Genomics Centre of the Max Planck Society. Research field: Small-molecule modulation of 14-3-3 Protein-Protein Interactions, Chemical Biology. Education: 1993-1998, study of biology at the Ruhr-University Bochum, 1999 Diploma in biology. Former professional experience: 2003 Ph.D. at the Center of Molecular Plant Biology, Eberhard-Karls-Universität Tübingen, Germany. 2004 Postdoc at the Max Planck Institute of Molecular Physiology, Structural Biology. Since 07/2006 Group Leader „Modulation of 14-3-3 Protein-Protein Interactions“, Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

New Phase I Enzymes Involved in Drug Metabolism and Prodrug Activation

The Discovery and Development of Anacetrapib

Amjad ALI

MERCK & CO. INC., Kenilworth, United States
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Amjad ALI

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Amjad received his Ph.D. under the direction of Prof. Gerald Pattenden at the University of Nottingham, UK (1993) and carried out postdoctoral work in the laboratories of Prof. Stephen F. Martin at the University of Texas, Austin, USA (1994-1996) and Prof Varinder Aggarwal at Sheffield University, UK (1997). He joined Merck Research Laboratories, Rahway, NJ, USA as a medicinal chemist in January 1998. Over the years he has contributed to drug discovery programs in a variety of therapeutic areas, including antibacterial, inflammation, cardiovascular disease and CNS. Amjad is a co-author on 35 publications and a co-inventor on 36 US patents. He recently co-wrote a book chapter on 'Atherosclerosis: HDL elevation' which was published in 'Burger's Medicinal Chemistry'. He is currently a Senior Research Fellow at Merck Research Laboratories, Rahway, NJ.

Fragment-based Discovery of Modulators for PPI and Allosteric Enzymes

Michelle ARKIN

UNIVERSITY OF CALIFORNIA, San Francisco, CA, United States
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Michelle ARKIN

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Michelle Arkin is the Assoc. Director of Biology at the Small Molecule Discovery Center and Assoc. Adjunct Professor in Pharmaceutical Chemistry at UCSF. Dr. Arkin’s research interests are in developing innovative approaches to tackle challenging targets - such as protein-protein interfaces (PPI) and allosteric enzymes - and orphan/neglected diseases. Dr. Arkin earned her PhD in chemistry at Caltech and then held a Daymon Runyon postdoctoral fellowship at Genentech. She was among the first scientists at Sunesis Pharmaceuticals, where she helped to develop fragment-based approaches for inhibiting PPI and biophysical tools to characterize drug-protein interactions. From 2005 to 2007, she was the Assoc. Director of Cell Biology at Sunesis and led the translational science team for Voreloxin, an anti-cancer agent in phase 3 clinical trials.

Discovery of BAY 94-8862: A non-Steroidal Antagonist of the Mineralocorticoid Receptor for the Treatment of Cardiorenal Diseases

Lars BARFACKER

BAYER HEALTHCARE, WUPPERTAL, Germany
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Lars BARFACKER

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Date of birth: July 20th, 1970 in Oberhausen Until 1996: Studies, degree in Chemistry at the University of Dortmund 1996-1999: Ph.D. thesis under supervision of Prof. Dr. P. Eilbracht at the University of Dortmund: “Hydroformylation of Silylated Olefins, Silylformylation of Alkynes – Variations and Applications” 1999-2000: Postdoctoral research with Prof. Dr. C. J. Forsyth at the University of Minnesota on a fellowship of the Deutsche Forschungsgemeinschaft (DFG) 2000-2010: Senior Scientist in Medicinal Chemistry at Bayer HealthCare AG in Wuppertal. Research areas: Virology, COPD, CNS, cardiovascular diseases Since 2011: Senior Scientist in Medicinal Chemistry at Bayer HealthCare AG in Berlin. Research area: Oncology

Computer-assisted Lead Generation: Fact or Fiction

Karl-Heinz BARINGHAUS

SANOFI, Frankfurt, Germany
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Karl-Heinz BARINGHAUS

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Karl-Heinz Baringhaus is currently Head of Structure, Design & Informatics at Sanofi-Aventis. This comprises Computational Biology & Bioinformatics, Computer-aided Drug Design, Scientific Computing & Data Management as well as Structural Biology. His research field encompasses modern computational techniques in lead finding and lead optimization. Karl-Heinz otained his Ph.D. in synthetic organic chemistry from the University of Muenster, Germany. After a postdoctoral fellowship at Stanford University he joined Hoechst AG where he was working six years in Medicinal Chemistry. Then he moved into Molecular Modeling and in 2000 he became Head of Computational Chemistry at Aventis Pharma. From 2005 to 2010 he was Director of Drug Design at Sanofi-Aventis Pharma Deutschland GmbH.

Computational Approaches to Polypharmacology and Mode-of-Action Analysis

Andreas BENDER

UNIVERSITY OF CAMBRIDGE, United Kingdom
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Andreas BENDER

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Andreas Bender is a Lecturer for Molecular Informatics with the Unilever Centre for Molecular Science Informatics at the University of Cambridge. He received his PhD from the University of Cambridge as a Cambridge Gates Scholar in 2005 and worked in the Lead Discovery Informatics group at Novartis in Cambridge/MA as well as at Leiden University in the Netherlands before his current appointment. In his work, he is involved with the integration and analysis of chemical and biological data, as documented in more than 80 scientific publications in the cheminformatics and related fields. Andreas is on the editorial boards of multiple journals such as Combinatorial Chemistry and High-Throughput Screening and the Journal of Chemical Information and Modeling as well as the recipient of the MGMS Silver Jubilee Prize 2011, the Medicinal Chemistry Innovation Prize of the German Chemical Society 2011 and the EFMC Young Medicinal Chemist in Academia Prize 2010.

Identification of a New Chemical Class of Potent Antimycobacterial Compounds Derived from BM 212: Design, Synthesis, Biological Evaluation and Study of their Mode of Action

Mariangela BIAVA

LA SAPIENZA UNIVERSITY OF ROMA, Roma, Italy
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Mariangela BIAVA

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Title: professor Position: associate professor Research field: Medicinal Chemistry: Synthesis of compounds with antitubercular activity Synthesis of analgesic and anti-inflammatory compounds Education and former experience: 2002 to the present: Full Time Associate Professor of Medicinal Chemistry, Dept.Chemistry and Technology of the Drug, Sapienza University of Rome (Italy) 2008- to the present: Management Committee (MC) member of the COST Action CM0801, title “New drugs in neglected diseases 1990-2001: Researcher in Medicinal Chemistry 1989: PhD in Medicinal Chemistry.

Working with Medicinal Chemistry Experts in Academia and Industry to Generate Novel Inhibitors ("probes") for Novel Epigenetic Proteins

Paul BRENNAN

UNIVERSITY OF OXFORD, Oxford, United Kingdom

The Discovery of UCB5857 a Novel and Selective PI3K delta Inhibitor for the Treatment of Inflammatory Disease

Dan BROOKINGS

UCB, Slough, United Kingdom
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Dan BROOKINGS

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I am currently a Senior Group Leader in the Medicinal Chemistry Department at UCB. After completing my PhD in organic chemistry at the University of Southampton in 1998 I joined British Biotech as a Medicinal Chemist working on antibacterial research before joining Celltech in 2000. During my time at Celltech/UCB I have worked on a variety of projects spanning early hit identification to lead optimisation and preclinical development. My research interests include the use of kinase inhibitors and protein/protein interaction inhibitors in drug discovery and the application of organic chemistry and physicochemical properties to overcome the ADMET and PK challenges of lead optimisation.

GPCR Structure Based Drug Design Using Stabilised Receptors (StaRs)

Giles BROWN

HEPTARES, Hertfordshire, United Kingdom
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Giles BROWN

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Dr. Giles Brown obtained his PhD in Chemistry at the University of Bristol in 2000 working with Prof. Timothy C. Gallagher on a novel azomethine ylide approach to bicyclic -lactams. After his PhD, he worked as a Post-Doctoral Research Associate with Prof. Gary A. Molander at the University of Pennsylvania investigating the development of SmI2 promoted sequential reactions. He returned to the UK in 2002 to work as a medicinal chemist at Evotec OAI. In 2003 he moved to Cambridge BioTechnology, where he focused on developing novel drugs for GPCR’s and protein-protein interactions. He joined Heptares Therapeutics in 2010 and currently co-leads discovery projects utilising the novel StaR™ technology for GPCR’s; focussing on metabolic and CNS indications. He is also responsible for managing all the chemistry outsourcing at Heptares.

Chemical Probes for Epigenetics

Mark BUNNAGE

PFIZER, Boston, United States
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Mark BUNNAGE

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Mark studied chemistry at the University of Durham, graduating in 1990. Mark then undertook his postgraduate studies with Professor S G Davies at the University of Oxford, followed by a move to The Scripps Research Institute, La Jolla, California to work with Professor K C Nicolaou as a NATO postdoctoral fellow. In 1996, Mark returned to the UK to join Pfizer as a medicinal chemist in their research laboratories in Sandwich, Kent. Over the past 16 years at Pfizer, Mark has had a number of roles of increasing responsibility and in November 2010 became Executive Director, Head of Medicinal Chemistry, Sandwich Laboratories. In April 2011, Mark was appointed Vice President, Head of Chemistry, Biotherapeutics Research at Pfizer and is now based in Cambridge, USA.

Strategies For The Design and Discovery of Compounds with Directed Against Challenging Targets of HIV-1 Life Cycle

Maria Jose CAMARASA

CSIC, Madrid, Spain
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Maria Jose CAMARASA

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Current Tittle and position: Research Professor (Full professor) at the Medicinal Chemistry Institute of CSIC (IQM-CSIC), (MADRID, SPAIN) - Co-coordinator of the Chemical Science and Technologies area of the CSIC - Head the of nucleosides and analogues group - Membeof the executive board of International Society for Nucleosides, Nucleotides and Nucleic Acids (IS3Na) Awarded in 2001 with the prestigious René Descartes-Prize of the European Commission. - Member of International Advisory and Editorial Boards of: Nucleosides, Nucleotides and Nucleic Acids, Current Topics in Medicinal Chemistry, ChemMedChem, Current HIV Research, Current Topics in Medicinal Chemistry Research Field: Medicinal Chemistry, drug-design and discovery, antivirals, anticancer, antiinfectives, pro-drugs, organic chemistry, carbohydrates, nucleosi(ti)des, peptides Education and former professional experience: PhD In Chemistry, by the Universidad Complutense of Madrid Head of the Chemotherapy Department of IQM-CSIC Vice-Director of Medicinal Chemistry Institute (IQM-CSIC) - President of the Spanish Society of Medicinal Chemistry (SEQT) (2004-2007) - Member of the executive board of the Chemistry Area of ANEP (2005-2008), coordinator of Medicinal Chemistry.

Frontloading Toxicity Detection in order to Lower Costs and Attrition

Bruce D. CAR

BMS, Princeton, United States
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Bruce D. CAR

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Bruce D. Car received Veterinary Medicine with Honours (1983), Masters (1985) degrees, and postgraduate training in pathology at The University of Melbourne, Victoria, Australia. He received his Ph.D. degree in 1989 from Cornell University studying a pulmonary disease model of extravascular coagulation and fibrinolysis. He attained American College of Veterinary Pathology specialty certification in Anatomic Pathology (1987) and Clinical Pathology (1990), and later certification with the American Board of Toxicology (1995) and was elected a Fellow of the International College of Toxicologic Pathology in 2002. Bruce undertook postdoctoral studies in immunology (1989-1994) at the Theodor Kocher Institute, University of Berne, and ETH/University of Zurich, Switzerland where he studied the role of alpha and beta chemokines in inflammatory disease, and cytokines in immunotoxicology and hematoipoiesis. In 1994 he joined DuPont Pharmaceuticals in Pathology and later led the Discovery/Investigative Toxicology group, which he continued after the acquisition of DPC in 2001 by Bristol-Myers Squibb Co. In 2010, Bruce extended his responsibilities to include Metabolism and Pharmacokinetics, Biotransformation, Discovery Analytical and Bioanalytical Sciences, Discovery Toxicology, and Discovery Pharmaceuticals as Vice President, Pharmaceutical Candidate Optimization (PCO); an organization of approximately 300 located in Princeton and Pennington, NJ, Wallingford, Connecticut, and Bangalore, India. PCO’s mission is to facilitate the creation of synthetic and biologic drug candidates with optimal developability profiles and shepherd those compounds through development. Bruce is a frequently invited speaker in the ADME Toxicology field and has published over 70 manuscripts.

Discovery of a Novel 2-aminothiazole Derivative (NVP-BYL719) with Potent and Selective PI3Kalpha Inhibitory Activity

Giorgio CARAVATTI

NOVARTIS, Basel, Switzerland
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Giorgio CARAVATTI

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Current position: Group leader Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Oncology, Basel. Research field: Medicinal Chemistry in the field of protein kinases. Education: Diploma in Chemistry at ETH Zürich (1972 - 1977); Ph.D. at ETH Zürich with Prof. Albert Eschenmoser (1977 - 1981); Postdoc at OSU, Corvallis OR, with Prof. James D. White (1981 - 1982). Professional carrier: - 1982-1983 Central Research Labs, Giba-Geigy AG, Basel. Since 1983 Pharma Research, Ciba Geigy later Novartis Institutes for BioMedical Research, Basel.

Realizing the Potential of Antibody-Drug Conjugates for the Treatment of Cancer

Ravi CHARI

IMMUNOGEN, Waltham, United States
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Ravi CHARI

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Ravi Chari is Executive Director of Chemistry & Biochemistry at ImmunoGen, Inc., a biopharmaceutical company located in Waltham, MA. His group is responsible for the development of potent cytotoxic compounds for tumor-specific delivery in the form of antibody-drug conjugates (ADCs). His group also designs novel linkers to generate ADCs with optimal anti-tumor activity. Dr. Chari received his doctorate in Chemistry from the University of Detroit, Detroit, MI. Subsequently, he was a postdoctoral fellow in the Pharmacology department at the Yale University – School of Medicine, where he was in involved in the design and synthesis of mechanism-based enzyme inhibitors. In 1986, he joined the Dana-Farber Cancer Institute/Harvard Medical School as a research scientist, where he initiated work on the use of monoclonal antibodies to specifically deliver cytotoxic drugs to tumor cells.

Small Molecule Control of Intracellular Protein Levels

Craig CREWS

YALE UNIVERSITY, New Haven, CT, United States
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Craig CREWS

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Craig Crews received his B.A. in Chemistry from the University of Virginia and his Ph.D. in Biochemistry from Harvard. After postdoctoral training in the Department of Chemistry and Chemical Biology at Harvard, Dr. Crews joined the Yale faculty in 1995, where he is the Lewis B. Cullmann Professor in the Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology. Prof. Crews’ interests are mainly in chemical biology and primarily focus on small molecule control of intracellular proteins and the mechanisms of action of biologically active natural products.

Industrialization of QSAR Model Generation-a Paradigm Shift in Predictive Modeling ?

Andy DAVIS

ASTRAZENECA, Mölndal, Sweden
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Andy DAVIS

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Andy gained his first degree in Chemistry from Imperial College of Science and Technology, University of London in 1982 and his PhD at University of Huddersfield with Professor MI Page, studying kinetics and mechanisms of rearrangements of penicillins. He joined Fisons in 1988 as a physical organic chemist, and subsequently became Associate Director of Physical Chemistry at AstraZeneca R&D Charnwood. Through his work on the application of physical chemistry to drug design he was honoured to be appointed an AstraZeneca Senior Principal Scientist. He has also been awarded two AstraZeneca global Scientific and Technical Achievement awards for work on a global ADMET prediction program called C-Lab, and contributions to the development of a high throughput hERG assay. In 2008 became chair of the Charnwood Local Projects Forum, and member of the Respiratory and Inflammatory research area Portfolio Team. In 2011 he moved to Sweden, and a new challenge of lead generation project leader in the recently established Respiratory and Inflammation Innovative Medicines unit at AstraZeneca R&D Mölndal. Through this time he has maintained his involvement in QSAR method development. He has published many highly cited articles in leading peer-reviewed journals, covering his key interests of compound quality, the energetics of drug-receptor interactions, QSAR methods and the co-operative application of physical organic and computational chemistry to drug discovery.

Iwan DE ESCH

VU AMSTERDAM, Amsterdam, The Netherlands
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Iwan DE ESCH

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Dr Iwan de Esch did his PhD research at the Department of Pharmacochemistry, VU University Amsterdam, The Netherlands. In 1998, he became research associate at the Drug Design Group of the University of Cambridge. Dr de Esch is a co-founder of De Novo Pharmaceuticals (2000) where he worked as a group and project leader. Dr de Esch returned to academia in 2003 and is now associate professor at the Medicinal Chemistry Department. The group focuses on two research lines, namely G-protein-coupled receptors (GPCRs) and Fragment-Based Drug Design (FBDD). Dr. de Esch is also co-founder of IOTA Pharmaceuticals Ltd (2007) and Griffin Discoveries BV (2009). In 2011, he was awarded the Galenus Research Price for his research on FBDD and valorisation activities. Next to member of staff of the Pharmacochemistry department, Iwan is also member of staff of the Science, Business & Innovation department at VU University Amsterdam.

Structure-Based Design of Novel Antibiotics for Treating Multidrug-resistant Bacterial Infections

Erin DUFFY

RIB-X PHARMACEUTICALS, Boston, United States
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Erin DUFFY

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Dr. Erin Duffy joined Rib-X early in 2002 and is the Chief Scientific Officer. Her experience includes serving as the Associate Director of Innovative Discovery Technologies at Achillion Pharmaceuticals, Inc. and five years as a computational chemist with Pfizer Global Research and Development in Groton, Connecticut. She was trained at Yale University, received her Ph.D. in 1994 in Physical-organic Chemistry with Professor William L. Jorgensen and moved to the Molecular Biophysics and Biochemistry Department as a Howard Hughes postdoctoral fellow with Professor Axel T. Brünger.

Drug Discovery in Neglected Diseases: Challenges and Opportunities

Rich ELLIOTT

BILL AND MELINDA GATES FOUNDATION, Seattle, United States
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Rich ELLIOTT

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Richard Elliott obtained his BS in chemistry from the University of Connecticut, his Ph.D. in medicinal chemistry working with Dr. Philip Portoghese at the University of Minnesota, and subsequently held organic chemistry postdoctoral fellowships with Dr. Dennis Curran at the University of Pittsburg and Dr. Wolfgang Oppolzer at the University of Geneva. Dr. Elliott has over 20 years pharmaceutical industry experience and has been involved in a number of drug discovery programs at Nova Pharmaceutical Corp., Abbott Laboratories, and Pfizer. During his careerin industry Dr. Elliott performed and directed medicinal chemistry research in numerous hit-to-lead, lead development, and candidate-seeking programs- including Alzheimer’s disease, anti-infectives, obesity, and diabetes. In 2008 Dr. Elliott joined the Bill & Melinda Gates Foundation as a Senior Program Officer working in the Discovery team in Global Health, where he manages a portfolio of grants involved in early-stage drug discovery, as well as assessing future investment opportunities to further the strategic objectives of the Gates Foundation.

Transforming Pharmaceutical Manufacturing: Continuous - The Ultra Lean Way of Manufacturing

James EVANS

NOVARTIS/MIT CENTER FOR CONTINUOUS MANUFACTURING, Cambridge, United States
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James EVANS

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Dr Evans is currently the associate director at the Novartis-MIT Center for Continuous Manufacturing. In this role he has responsibility for delivering a bench scale Integrated Continuous Manufacturing platform that can be utilized as a model and learning tool for transforming the pharmaceutical manufacturing paradigm Dr Evans received his PhD in Chemical and Process Engineering from Herriot Watt University and an MS in Instrumentation and Analytical Chemistry from UMIST. In addition to this he completed postdoctoral research at the Illinois Institute of Technology. Dr Evans has extensive experience in API pharmaceutical manufacturing and R&D for both MNC’s and biotech companies.

Downsizing Proteins: Peptidomimetics Beyond the Rule of Five

David FAIRLIE

UNIVERSITY OF QUEENSLAND, Brisbane, Australia
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David FAIRLIE

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Current Position: Professor David Fairlie Head, IMB Division of Chemistry and Structural Biology IMB Lab Head, Chemistry and Human Therapeutics NHMRC Senior Principal Research Fellow Institute for Molecular Bioscience (IMB), University of Queensland, Brisbane, Qld 4072, Australia Tel: +61-7-3346 2989 Fax: +61-7-3346 2990 Email: d.fairlie@imb.uq.edu.au Professor David Fairlie. BSc (Adelaide), PhD (New South Wales), Postdocs (Stanford, Toronto). He is internationally known as a research and opinion leader in medicinal and biological chemistry and drug discovery. He consults widely to North American and European pharma/biotech companies. His interests are at the interfaces of chemistry, biochemistry, pharmacology, immunology and virology. Currently he is developing small molecules and peptidomimetics for inflammatory and metabolic disorders, viral and parasitic infections, cancer and neurodegenerative diseases. He has special interests in inhibitors of enzymes (especially proteases), agonists and antagonists of proteins (especially GPCRs), protein surface mimetics, and in unraveling mechanisms of disease development and drug action.

From Determinants of Binding to Modulators of Protein-Protein-Interactions

Discovery and Optimization of New Benzimidazole and Benzoxazole Pyrimidone PI3KB Inhibitors for the Treatment of PTEN-deficient Cancers

Frank HALLEY

SANOFI, Vitry-sur-Seine, France
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Frank HALLEY

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Education: 1988-89 : Industrial Post Doc in Quest International (Ashford, Kent, UK). Research of new synthetic routes for organoleptic terpenes. 1987-88 : Post Doc TEXAS A&M University, Texas, USA, (Professor D.H.R. Barton). Selective oxidation of alcanes to ketones, discovery of a new oxidation system, the Gif IV system. 1983-86 : Ph D at the Institut de Chimie des Substances Naturelles, CNRS, Gif-sur-Yvette, France, (Professor D.H.R. Barton). Research of Radicals in O and C phenylation Reaction with Pentavalent Bismuth compounds. Career: 2004-2012 : Team leader in Sanofi-Aventis Pharma France, oncology group (CRVA). 2000-2004 : Lab Head in Aventis Pharma France (in charge of a medicinal chemistry lab 8-10 people). 1999-2000 : Section manager in a medicinal chemistry department. Rhône-Poulenc Rorer (RPR, Dagenham, Essex, UK). Supervise a team of 6 to 8 people including 2 PhDs. 1998 : Senior Research Fellow (RPR). Supervise 3 to 4 synthetic chemists 1992 : Principal scientist 4 (RPR). Supervise 2 to 3 synthetic chemists 1990 : Medicinal chemist (RP), Supervise 1 synthetic chemist. Work experience in different therapeutic areas, cardiovascular (ACAT, angiotensin II, endothelin, PDGF and C5a), Respiratory/Inflammation (RANTES antagonists, prolyl-4-hydroxylase antagonists, VLA-4, CCR2, CCR3, CCR4 antagonists, p38 inhibitors, and cathepsin S inhibitors), anti-infective (Methionine Amino Peptidase and Secretases), oncology (angiogenesis KDR, Tie2, CDKs, IGF-1R,CDKs, HSP90, PI3K, MEK) and CNS (Alzheimer diseases, PDE4, PAK3, CK1). Track records : participation to 6 different programs leading to 7 compounds sent to preclinical development: - 1996 endothelin ETA antagonist for the treatment of chronic obstructive pulmonary disease (COPD) - 1999 p38 inhibitor for the treatment of rheumatoid arthritis - 2003 CK1- inhibitor for the treatment circadian rhythm disorders - 2004 PDE4 inhibitor for the treatment of cognitive disorders and Alzheimer disease - 2004 Tie2/KDR inhibitor for the treatment of solid tumors - 2006 a second Tie2/KDR inhibitor for the treatment of solid tumors - 2010 PI3K inhibitor for the treatment of PTEN deficient solid tumors

Isoform Selective PDE4B Inhibitors: Testing a Hypothesis for Improved Therapeutic Index

Nicole HAMBLIN

GLAXO WELLCOME, Stevenage, United Kingdom
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Nicole HAMBLIN

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Dr Nicole Hamblin is a Senior Project Leader and Medicinal Chemistry Research Leader at GlaxoSmithKline in Stevenage, UK. Nicole has been at GSK for 15 years, working across multiple therapeutic areas in the lead optimization phase, to successfully deliver clinical candidates. Most recently Nicole has been working in the respiratory field, targeting biological mechanisms believed to be important in the underlying inflammation associated with asthma and COPD, including PDE4, P38 and PI3 kinases. Prior to joining GSK, Nicole graduated from Oxford University in 1993 with first class honours in chemistry and then remained at Oxford to complete a D. Phil in synthetic organic methodology with Dr John Sutherland.

From Chromatin Modulation to Drug Discovery : BET Bromodomain and EZH2 Inhibition

Jean-Christophe HARMANGE

CONSTELLATION PHARMACEUTICALS, Cambridge, United States
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Jean-Christophe HARMANGE

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Jean-Christophe Harmange, Pharm.D., Ph.D., is Executive Director of Drug Discovery at Constellation Pharmaceuticals. His current responsibilities include providing leadership for Drug Discovery support in the areas of automation, assay development and screening, structural biology and medicinal chemistry. Prior to Constellation Pharmaceuticals, Dr. Harmange was Director Research at Amgen where he led medicinal chemistry teams responsible for delivering AMG 208 and AMG 337. Prior to Amgen, Dr.Harmange occupied different positions at Eisai (Andover, MA) and at Servier (Suresnes, France). Dr. Harmange holds a Pharm. D. and a Ph.D. in organic chemistry from Paris XII University and was a postdoctoral fellow in the Laboratory of Pr. Yoshito Kishi at Harvard University.

The Interface between Academia and Industry – Opportunities for Medicinal Chemists

Torsten HOFFMANN

F. HOFFMANN-LA ROCHE, Basel, Switzerland
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Torsten HOFFMANN

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Narrative CV Torsten Hoffmann Torsten Hoffmann is Head of Discovery Chemistry in Basel since February 2005. He received his Ph.D. in chemistry from the ETH Zürich in 1996 which was followed by a postdoctoral fellowship from 1996-1997 at The Scripps Research Institute, La Jolla, CA. In 1997 he joined the Medicinal Chemistry section of the CNS Department in Basel as a research chemist. He worked on a number of projects as team member and later as project team leader. During this time, his team identified different portfolio compounds which entered clinical trials at Roche, among them befetupitant and netupitant. In 2003 he received the task to set up Discovery Enabling Sciences in Basel, a newly founded department which encompassed the areas of Assay Development and High Throughput Screening, Microtechnology and Automation, Discovery Drug Metabolism and Pharmacokinetics as well as Molecular Properties determinations. He received different prices and awards, among them a fellowship of the Studienstiftung des deutschen Volkes, the Feodor Lynen award of the Alexander von Humboldt Foundation and a Kekulé fellowship. He is author on over 60 research publications, published conference reports and patent applications.

Stem Cells and Small Molecules

Lilian HOOK

PLASTICELL LTD., London, United Kingdom
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Lilian HOOK

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Biography: Dr Lilian Hook is Research Director at Plasticell Limited. She has over 15 years’ experience in stem cell research, gained both in academia and industry. Her work has focused on the developmental biology and clinical application of haemopoietic stem cells and the use of embryonic stem and adult stem cells in drug discovery applications, particularly in the neural field. Dr Hook holds a PhD in Developmental Haematology from the University of Edinburgh and a first degree in Natural Sciences from Cambridge University.

Discovery of Chemical Probes for Histone Methyltransferases

Jian JIN

UNIVERSITY OF NORTH CAROLINA, Chapel Hill, United States
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Jian JIN

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Dr. Jin is an Associate Professor and Director of Medicinal Chemistry in the Center for Integrative Chemical Biology and Drug Discovery at the University of North Carolina - Chapel Hill (UNC-CH). His current research interests include discovering chemical probes for protein and DNA methyltransferases and functionally selective GPCR ligands. Prior to joining UNC-CH in 2008, Dr. Jin had >10 years of drug discovery experience at GlaxoSmithKline, where he had most recently served as a Manager of Medicinal Chemistry from 2003 to 2008. Dr. Jin has published 61 peer-reviewed papers and is an inventor of 41 issued patents and patent applications

Antitubercular Nitroimidazoles

Takushi KANEKO

TB ALLIANCE, New York, United States
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Takushi KANEKO

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Dr. Takushi Kaneko is Senior Project Leader at TB Alliance (Global Alliance for TB Drug Development), a New York based not-for profit organization dedicated to the discovery and development of better, faster-acting, and affordable tuberculosis drugs. After obtaining a degree at the University of Michigan and conducting post-doctoral work at Harvard University, he spent most of his time in drug discovery research in Bristol-Myers Squibb and Pfizer in the areas of cancer chemotherapy, natural product discovery, and antibacterial agents.

Danijel KIKELJ

UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
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Danijel KIKELJ

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Professor Danijel Kikelj obtained his PhD degree from the University of Heidelberg, Germany in 1988. Since 2000 he is full professor of medicinal chemistry at the Faculty of Pharmacy, University of Ljubljana, Slovenia. His scientific expertise includes medicinal and organic chemistry with the focus on peptidomimetics, serine protease inhibitors and designed multiple ligands. His research activities comprise design and synthesis of peptidomimetics, structure-based design of thrombin inhibitors, dual antithrombotic compounds, inhibitors of bacterial Mur ligases and sodium channel modifiers based on leads of marine origin. He is a member of EFMC Council and has acted as member of EFMC Education and Training Committee from 2006 till 2010. Together with his coworkers he is organizing the 2nd Meeting of the Paul Ehrlich MedChem Euro-PhD Network in September 2012 in Ljubljana.

Session Chair

Gerhard KLEBE

PHILIPPS-UNIVERSITY MARBURG, Marburg, Germany

API Bioavailability Hurdles - What Formulation Can Do

Peter LANGGUTH

JOHANNES GUTENBERG UNIVERSITY MAINZ, Mainz, Germany
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Peter LANGGUTH

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Peter Langguth is pharmaceutical scientist by training. He received a Ph.D. in Pharmacology (1985) from the Johann Wolfgang Goethe-University in Frankfurt, did post-doctoral studies in pharmacokinetics at the University of Florida in Gainesville and received a habilitation degree in Pharmaceutical Technology and Biopharmaceutics from the ETH Zürich in 1995. Thereafter he joined the Department of Pharmacokinetics and Drug Metabolism at Astra HässleAB in Mölndal, Sweden, as Group Leader in Drug Absorption Research. Since 1998 he is heading the Department of Pharmaceutical Technology and Biopharmaceutics at the University of Mainz. He develops and characterizes formulations for biopharmaceutically challenging molecules for oral, pulmonary and parenteral drug administration with particular emphasis on optimizing bioavailability and achieving targeting. Some of his concepts have been taken into humans.

Ligand Efficiency Metrics: A Cure for Molecular Inflation?

Paul LEESON

GLAXOSMITHKLINE, Nuneaton, United Kingdom
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Paul LEESON

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Paul Leeson is a consultant in drug discovery with more than 30 years of experience in major pharmaceutical companies. He obtained BSc and PhD degrees in chemistry from the Universities of Liverpool and Cambridge, followed by postdoctoral work at Sussex University. His industrial career began at Smith Kline and French Research Laboratories, and has taken him to Merck Sharp and Dohme, then to Wyeth (USA), and from 1997-2011, AstraZeneca, where he was Head of Medicinal Chemistry at the Charnwood site. His drug discovery contributions, published in >150 papers and patents, have been in the cardiovascular, neuroscience, respiratory and inflammation therapy areas. He has a special interest in the generation and application of lead-like and drug-like properties, with an emphasis on compound quality in relation to pipeline attrition.

The Role of Passive Diffusion and Carrier-Mediated Transport in the Intestinal Drug Absorption Process

Hans LENNERNAS

UPPSALA UNIVERSITY, Uppsala, Sweden
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Hans LENNERNAS

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Dr. Hans Lennernäs is a full professor of Biopharmaceutics at Uppsala University since 1 July 2000, Sweden.Since 2004 he is also the chief Scinetific Office of LIDDS AB (www.liddspharma.com). His research interest is focused on clinical significance of mechanisms and regulation of membrane transport and metabolism of drugs/metabolites in the gastrointestinal tract, hepatobiliary system and tumor tissues. This work is performed in vivo with clinical models in humans and in various tissue and cell culture models. His research aims to develop novel strategies of tissue drug targeting and delivery that aims to improve the clinical use and efficacy of drugs in various disease states, such as metabolic and cancer diseases. Hans Lennernäs has together with gastroenterologists developed and validated two new clinical intestinal perfusion techniques for investigations of intestinal transport and metabolism of drugs and nutrients. He has been the Principal Investigator in an extensive collaboration with Food Drug & Administration, USA, University of Michigan, USA, and Medical Product Agency, Sweden during several years to develop a new guideline for the Biopharmaceutics Classification System. He is also one of the innovators to a novel sublingual drug delivery system currently used for the treatment of various acute pain conditions. The product, Rapinyl®, has been approved in EU and USA. These two start-up companies are focused of a novel oral replacement therapy (www.duocort.com) for Addison disease and focal drug treatment of localised prostate cancer (www.liddspharma.com). The oral modified release product, Plenadren®, was approved by EMA in July 2011. His research team is currently composed of 5 Ph.D. students and one post-doc, and has an extensive national and international interdisciplinary collaboration with both universities and national and international pharmaceutical companies.

Alessio LODOLA

UNIVERSITY OF PARMA, Parma, Italy
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Alessio LODOLA

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Università degli Studi di Parma (www.unipr.it) Dipartimento Farmaceutico Assistant Professor in Medicinal Chemistry I received the Pharm. D in 2001 from the Faculty of Pharmacy of the University of Parma. In 2005, I obtained the PhD in medicinal chemistry, working in the group of Prof. Marco Mor. During my PhD and later, as a visiting scientist, I made a noteworthy research experience in the group of Prof. Adrian Mulholland, at the University of Bristol (UK). I became assistant professor at the University of Parma in 2005. Since that year, I’ve been working as a research scientist in the medicinal chemistry group of Prof. Marco Mor. I also actively collaborate with the Italian Institute of Technology (IIT), with the Drug Discovery & Development Unit led by Prof. Daniele Piomelli. My research activities are mainly focused on i) the design of covalent inhibitors of enzymes (FAAH and NAAA) catalyzing the inactivating hydrolysis of neuromodulatory fatty acid ethanolamides, such as anandamide and palmitoylethanolamide; ii) the design of anti-cancer agents including inhibitors of EGFR and antagonists of the Eph-ephrin system.

Selective Ion Channel Blockers for the Treatment of Atrial Fibrillation

David MADGE

XENTION, London, United Kingdom
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David MADGE

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Dr David Madge is VP, Research at Xention Ltd., a Cambridge, UK, drug discovery company with a focus on ion channel targets. David began his medicinal chemistry career at the Wellcome Foundation, working on early-stage drug discovery projects, mainly in the neuroscience area and involving, in particular, ion channel research. David then went on to complete a PhD in Medicinal Chemistry at Imperial College, London, in 1994. In 1995 David moved to the Wolfson Institute, at University College, London. In 2001 David took on the role of Chief Operating Officer for a chemical services company (NCE Discovery) that had been spun-out of the medicinal chemistry group at the Wolfson Institute, specializing in providing support to early-stage drug discovery companies. David joined Xention Ltd. In 2005 as VP, Chemistry, and was responsible for drug discovery chemistry and clinical manufacturing and support. In 2009 David became VP, Research, taking responsibility for all internal and collaborative drug discovery activities at Xention.

Maximizing Efficacy: How to win the Quest for Highly Potent Drugs

Paul W. MANLEY

NOVARTIS PHARMA, Basel, Switzerland
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Paul W. MANLEY

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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.

Inhibiting Glucose Transport via SGLT Inhibitors - the Next New Diabetes Drug Family?

Michael MARK

BOEHRINGER INGELHEIM, Biberach, Germany
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Michael MARK

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Michael Mark PhD is the Vice President and Global Head of CardioMetabolic Diseases Research at Boehringer Ingelheim, Germany. In this role, he is responsible for the research and development of new treatments for cardiovascular and metabolic diseases including type 2 diabetes mellitus, obesity, atherosclerosis and chronic kidney disease. Dr Mark has more than 25 years’ experience in the pharmaceutical industry. Early in his career, Dr Mark contributed to the discovery and development of repaglinide, an approved treatment of type 2 diabetes. He pioneered the discovery of the DPP-4 inhibitor linagliptin and was instrumental in the initiation of the preclinical work for the SGLT2 inhibitor empagliflozin, which is currently in phase 3 clinical trials. Dr Mark has been appointed as Project Co-ordinator for SUMMIT, an Innovative Medicines Initiative (IMI)-sponsored European consortium of 19 academic centres and six major pharmaceutical partners, which aims to identify and characterize novel biomarkers and genetic markers for diabetic complications.

The Central Valine Concept revealed Indolyl-Imidazole Scaffold as p53-Hdm2 PPI Inhibitors

Keiichi MASUYA

NOVARTIS, Basel, Switzerland
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Keiichi MASUYA

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Current title and position: Group Leader, Global Discovery Chemistry, Oncology Basel, Novartis Institutes of BioMedical Research Research field: Medicinal chemistry in oncology area, particularly Protein-Protein Interaction, Kinase and protease inhibitors Education and former professional experience: Group Leader, Novartis, Basel, Switzerland 09/2010 – present Project Leader, Novartis, Basel, Switzerland 04/2005 – 08/2010 Project Leader, Novartis, Tsukuba, Japan 09/2001 – 03/2005 Mitsubishi Pharma, Research Center, Yokohama, Japan 04/1998 – 08/2001 Chemistry Ph.D, Tokyo Institute of Technology, Tokyo, Japan 04/1995 – 03/1998

Development of M1 Allosteric Modulators for the Treatment of CNS Disorders and Improving Cognition

Bruce MELANCON

VANDERBILT CENTER FOR NEUROSCIENCE DRUG DISCOVERY, Nashville, United States
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Bruce MELANCON

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Bruce Melancon received his bachelor’s degree in Chemistry from Louisiana State University. Under the direction of Professor Robert M. Strongin, he worked on the synthesis of resorcinarene chromophores for the sensing of mono- and oligosaccharides in solution. Upon graduation, he moved to the University of Notre Dame and began his graduate research. Under the direction of Professor Richard E. Taylor, he developed novel cationic cyclopropanation reactions with high enantiospecificity from enantiomerically enriched sulfonate intermediates. He also investigated biomimetic approaches to cyclopropanes found in polyketide natural products. After successful completion of his Ph.D., he moved to Vanderbilt University to begin postdoctoral studies under Professor Gary A. Sulikowski. He was awarded an NIH fellowship through the Vanderbilt Institute of Chemical Biology. Bruce then moved to the Vanderbilt Center for Drug Discovery where he began work on small molecule antagonists which are selective for the M1 muscarinic receptor. He is also working on the development of small molecule agonists of the M1 receptor

Predicting the Safety Profile of Bioactive Small Molecules

Jordi MESTRES

IMIM AND UNIVERSITY POMPEU FABRA, Girona, Spain
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Jordi MESTRES

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Jordi Mestres holds a PhD in Computational Chemistry from the University of Girona (Catalonia, Spain). After a post-doctoral stay at Pharmacia&Upjohn (Kalamazoo, Michigan, USA), in 1997 he joined the Molecular Design & Informatics department at N.V. Organon (Oss, The Netherlands) and in 2000 he was appointed Head of Computational Medicinal Chemistry at Organon Laboratories (Newhouse, Scotland, UK). In 2003, he took on his current position as Head of Chemogenomics at the IMIM Hospital del Mar Research Institute in Barcelona (Catalonia, Spain). He is also Associate Professor at the University Pompeu Fabra. His research interests focus on the use and development of computational approaches to integrate chemical, biological, and phenotypic spaces and their application to systems chemical biology and drug discovery. He is the author of over 110 publications, 8 patents among them. In March 2006, he founded Chemotargets as a spin-off company of his laboratory. The company’s main asset is a proprietary software for the prediction of the affinity of small molecules on almost 5,000 proteins that can be applied from identifying new targets for approved drugs, to deconvoluting the target space of bioactive small molecules identified in phenotypic screens, up to anticipating drug side effects.

In vitro – in vivo Extrapolation: Application of in vitro Approaches for Reaction Phenotyping and the Prediction of Metabolic Drug Clearance and Drug-Drug Interaction Potential

John MINERS

FLINDERS UNIVERSITY SCHOOL OF MEDICINE, Bedford Park, Australia
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John MINERS

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John Miners received his BSc, MSc and PhD (Medicinal Chemistry) from Victoria University of Wellington (New Zealand) and was awarded a DSc by Flinders University in 1997. He is currently Professorial Head of the Department of Clinical Pharmacology of Flinders University (Adelaide, Australia). His primary research interests are the application of in vitro approaches to predict drug metabolism parameters in vivo, and structure-function relationships of drug metabolising enzymes. He is the author of 250 research papers in these areas, and an ISI Highly Cited author in the discipline of pharmacology. He is President-elect of the International Society for the Study of Xenobiotics, a member of the Executive Committee of the International Union of Basic and Clinical Pharmacology, and a member of the Editorial Boards of seven international journals.

Medicinal Chemistry Challenges for Kinetoplastid Diseases

Charlie MOWBRAY

DRUGS FOR NEGLECTED DISEASES INITIATIVE (DNDI), Geneva, Switzerland
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Charlie MOWBRAY

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Dr. Mowbray joined DNDi in August 2011 as Head of Drug Discovery with responsibility for lead optimization in drug discovery projects. Prior to joining DNDi, Dr. Mowbray spent 19 years at Pfizer Worldwide Research and Development where he was most recently a Research Fellow in Worldwide Medicinal Chemistry at the Sandwich Laboratories, UK. During this time he developed experience as a medicinal chemist, project leader and people manager. He has delivered projects across many disease areas, target classes and medicinal chemistry strategies and from target selection through to clinical candidate delivery. Two of these molecules have completed Phase IIb clinical studies. Dr. Mowbray was awarded his Ph.D. by the University of Exeter and completed postdoctoral fellowships at the University of British Columbia and the University of Nottingham.

Kinase Inhibitors with Pre-engineered Binding Kinetic Signatures

Gerhard MUELLER

MERCACHEM, Basel, Germany
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Gerhard MUELLER

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Gerhard Müller, Senior Vice President Medicinal Chemistry, Mercachem bv, Nijmegen, The Netherlands Research Field: Small Molecule Drug Discovery, Lead Finding and Optimization, Kinase Inhibitors, Epigeneitc Drug Discovery, Protein-Protein Interaction Education and former positions: PhD in Organic Chemistry from Technical University, Munich, group of Prof. Horst Kessler 1992-1994: Research Scientist at Glaxo, Verona, Italy 1994-2001: Research Scientist and Project Manager at Bayer AG, Leverkusen, Germany 2001-2003: Section Head Medicinal Chemistry at Organon, Oss, The Netherlands 2003-2005: Chief Scientific Officer, Axxima Pharmaceuticals, Munich, Germany 2005-2008: Vice President Drug Discovery, GPC Biotech AG, Munich, Germany 2008-2011: Chief Scientific Officer at Proteros Fragments GmbH, Munich, Germany Since 2011: Senior Vice President Medicinal Chemistry, Mercachem bv, Nijmegen, The Netherlands

Arming Antibodies with Drugs and other Payloads: from the Bench to the Clinic

Dario NERI

ETH ZÜRICH, Zürich, Switzerland
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Dario NERI

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Born in Rome (Italy) on 1 May 1963, Dario Neri studied Chemistry at the Scuola Normale Superiore of Pisa. In 1992, he earned his doctorate in Chemistry at the ETH Zurich under the guidance of Professor Kurt Wüthrich, winning the ETH medal for his dissertation. With a EU Bridge Bursary, he spent four years at the Cambridge Centre for Protein Engineering, Medical Research Council, where he worked under the supervision of Sir Gregory Winter. Dario Neri has now been a Professor at the ETH Zurich since 1996. Dario Neri has published over 200 articles in peer-reviewed scientific journals and is inventor in numerous patents. He is the recipient of the ISOBM Abbott Prize 2000, of the Amgen-Dompe’ Biotec Award 2000, of the Mangia d’Oro 2001, of the Prous Award 2006 of the European Federation of Medicinal Chemistry, of the Robert-Wenner-Prize 2007 of the Swiss Cancer League, of the SWISS BRIDGE Award 2008 and of the Prix Mentzer 2011 of the French Medicinal Chemistry Society. In 1996, Dario Neri co-founded Philogen (www.philogen.com), a biotech company with headquarters in Siena (Italy) and in Otelfingen (Switzerland).

PF-4958242: A Novel AMPA Positive Allosteric Modulator (PAM) for the Treatment of Cognitive Deficits Associated with Schizophrenia

Christopher O'DONNELL

PFIZER, New York, United States
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Christopher O'DONNELL

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Chris obtained a B.S. in Chemistry from the University of Illinois in Urbana/Champaign in 1992 and a Ph.D. in Organic Chemistry in 1997 from the University of Wisconsin, Madison under the direction of Professor Steven D. Burke. As an NIH pre-doctoral fellow, his thesis work focused on the design and synthesis of unnatural ionophores. Chris then joined the group of Professor Larry E. Overman at the University of California-Irvine as an American Cancer Society postdoctoral fellow where he completed the total synthesis of gelsemine. Chris joined Pfizer in 1999 as a medicinal chemist in the Neuroscience Medicinal Chemistry group and has worked in the areas of addiction, cognition, psychosis, Alzheimer ’s disease, and Bipolar. As a scientist, project leader, and manager in these areas, he has led project teams to the nomination of several clinical candidates, and his efforts were instrumental to the discovery of clinical candidates in the 7 nAChR agonist program, the GABAA inverse agonist program, the SERT/5-HT2A antagonist program, the PDE2 inhibitor program and the AMPA PAM program. In 2011, Chris moved to the Oncology Medicinal Chemistry group and currently leads the Antibody Drug Conjugate discovery efforts. Chris is an author/inventor on over 50 publications/patents.

Small-Molecule Stabilization of 14-3-3 Protein-Protein Interactions: a Feasible Approach in Drug Discovery?

Christian OTTMANN

MAX-PLANCK SOCIETY, Eindhoven, The Netherlands
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Christian OTTMANN

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Current title and position: Dr. Christian Ottmann, Group leader at the Chemical Genomics Centre of the Max Planck Society. Research field: Small-molecule modulation of 14-3-3 Protein-Protein Interactions, Chemical Biology. Education: 1993-1998, study of biology at the Ruhr-University Bochum, 1999 Diploma in biology. Former professional experience: 2003 Ph.D. at the Center of Molecular Plant Biology, Eberhard-Karls-Universität Tübingen, Germany. 2004 Postdoc at the Max Planck Institute of Molecular Physiology, Structural Biology. Since 07/2006 Group Leader „Modulation of 14-3-3 Protein-Protein Interactions“, Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

The Resurgence of Covalent Drugs

Russell PETTER

CELGENE AVILOMICS RESEARCH, Bedford, United States
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Russell PETTER

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Dr. Petter is Vice President of Drug Discovery at Avila Therapeutics. Dr. Petter has a broad background in organic and medicinal chemistry in both academia and the private sector. In industry he has focused on the discovery and development of therapeutics to treat cancer, cardiovascular disease, and autoimmune disorders. Prior to joining Avila he was VP of Research at Mersana Therapeutics, Director of Small Molecule Drug Discovery at Biogen, Fellow and Head of Chemistry in the Oncology/Adhesion Biology Department at Sandoz/Novartis, and Assistant Professor of Chemistry at the University of Pittsburgh. Dr. Petter earned his PhD in organic chemistry at Duke University and completed his post-doctoral training at Columbia University.

Nanomedicinal Chemistry and Nanotechnology

Maurizio PRATO

UNIVERSITY OF TRIESTE, Trieste, Italy
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Maurizio PRATO

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Maurizio Prato graduated in Padova, where he was appointed Assistant Professor in 1983. Moved to Trieste as an Associate Professor in 1992, where was promoted Full Professor in 2000. He spent a sabbatical terms at Yale University (1986-7) and at the University of California, Santa Barbara (1991-2). He was Visiting Professor at the Ecole Normale Supérieure de Paris (2001) and at the University of Namur, Belgium (2010). His research focuses on the functionalization chemistry of carbon nanostructures for applications in materials science and medicinal chemistry. His scientific contributions have been recognized by National and International awards. He was the recipient of an ERC Advanced Research Grant, European Research Council, 2008 and has become a Member of the National Academy of Sciences (Accademia Nazionale dei Lincei) in 2010.

Fragment-based Chemical Tools Targeting Proteases and Tyrosine Phosphatases Developed by Dynamic Ligation and Design

Jörg RADEMANN

UNIVERSTITÄT LEIPZIG, Leipzig, Germany
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Jörg RADEMANN

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Jörg Rademann studied chemistry and biochemistry at the University of Konstanz, Germany, and at Rutgers University (USA) and obtained a PhD with Prof RR Schmidt on the solid phase synthesis of oligosaccharide. Following to a PostDoc at Carlsberg Laboratory (Denmark), he established his independent research group 1999 at the Eberhard-Karls-University in Tübingen. In 2004 he became Professor of Medicinal Chemistry at the Free University of Berlin and Head of the Medicinal Chemistry section at the Leibniz Institute for Molecular Pharmacology (FMP) including an academic Screening Unit. Since 2010 he has been chair of Medicinal Chemistry at the University of Leipzig. His research is focused on the fragment-based development of chemical tools in the area of protease, phosphatases, and protein-protein interactions.

Importance of Particle Size Control for Poorly Soluble Drugs

Thomas RAMMELOO

JANSSEN R&D, BEERSE, Belgium
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Thomas RAMMELOO

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Thomas Rammeloo graduated from the Ghent University in 1999 as biological engineer. He continued as PhD scholar at the Faculty of Bioscience Engineering within the same university. During his PhD work he investigated new pathways towards 2,4 methanoproline and derivatives. After finishing his PhD in 2003, he started working at Jansen Pharmaceutical. Currently he is Technical Integrator and Chemistry Lead within the API Small Molecule Development department. As Technical Integrator, he covers all phases of development ranging from the first non-GMP batch up to full development and commercialization. For more than five years, he is the crystallization lead for the department and ensures that desired physical API properties can be met through scalable crystallization processes.

LE, LLE and FBDD

David REES

ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
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David REES

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David Rees joined Astex in January 2003 and is Senior Vice-President Medicinal Chemistry. Astex have pioneered fragment based drug discovery (FBDD) and have progressed several compounds into clinical trials in cancer patients. David is a co-recipient of the Royal Society of Chemistry Malcolm Campbell Memorial Prize 2007 for the discovery of sugammadex (Bridion) and he is President of the Organic Division of the Royal Society of Chemistry

Biologics: Future Medicines for Metabolic Diseases?

Cristina RONDINONE

MEDIMMUNE, Gaithersburg, United States
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Cristina RONDINONE

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Dr. Cristina Rondinone received her Ph.D. in Biochemistry from University of Buenos Aires, studying the immunosuppresive effect of novel steroids. Her postdoctoral training was at the Laboratory of Cellular and Developmental Biology, NIDDK, NIH as a Visiting Fellow where her interest in fat metabolism and insulin signaling began and where she investigated the role of perilipin in adipocyte differentiation and lipolysis. In 1995, she moved to Sweden where she was first Senior Scientist for the Lundberg Laboratory for Diabetes Research, Department of Internal Medicine, University of Gothenburg and then she was appointed as Associate Professor in Molecular Medicine, University of Gothenburg. During her time in Sweden, she developed a research program investigating insulin signaling in human fat as well as the mechanisms of insulin resistance in Type 2 diabetes. From 1998 to 2005, she worked at Abbott Laboratories, where she became first Associate Research Fellow of the Volwiler Society and then Group Leader in the metabolic disease research area. In 2005 she moved to Hoffmann-La Roche as Research Director of Metabolic Diseases and in 2007 became Senior Director and Therapeutic Area Head overseeing drug discovery programs in metabolic and vascular diseases, including target identification, lead optimization and advancement of preclinical candidates into clinical development. In 2011 she moved to MedImmune, Inc., as Vice President Research and Development and Head Cardiovascular and Metabolic Diseases, leading the portfolio of biologics in this therapeutic area. She has published more than 65 academic publications in the field of diabetes, insulin resistance and obesity, and coinventor of 4 patents. She was also Editor of the book Therapeutic Aplications of RNAi. She has also has been invited speaker in numerous national and international symposiums as well as Chairman of numerous sessions at the Keystone Symposia, American Diabetes Association and European Diabetes Association. She was member of the Editorial Board of the journal Endocrinology and Associate Editor of Archives of Physiology and Biochemistry as well as reviewer for the American Diabetes Association, NAASO, National Institutes of Health (NIH), National Science Foundation (US), Institut Curie, French Ministry of the Research and Education, Czech Science Foundation, Israel Science Foundation and the Australian Science Foundation. She is also member of the Scientific Advisory Board for the Keystone Symposia and she recently was inducted as a member of the Real National Academy of Pharmacy in Spain.

Stem Cell Chemistry and its Impact in Drug Discovery

Angela RUSSELL

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Angela RUSSELL

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Angela Russell is currently a University Lecturer in Medicinal Chemistry jointly between the Departments of Chemistry and Pharmacology at the University of Oxford. Her research interests broadly encompass the development of small molecules to control developmental processes. She has worked on several successful multidisciplinary research collaborations in areas including oncology, muscular dystrophy and, more recently, regenerative medicine through the discovery and application of small molecules to manipulate stem cell fate. Her work has resulted in over 60 publications and patent filings to date. She gained her MChem degree from the University of Oxford in 2000, and her DPhil in 2004 under the supervision of Professor Steve Davies. In July 2007 was awarded a Research Councils’ UK Fellowship in Medicinal Chemistry in the Departments of Chemistry and Pharmacology in Oxford.

Novel Paradigms for GPCR Allosteric Modulator Identification

Stephan SCHANN

DOMAIN THERAPEUTICS, Strasbourg, France
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Stephan SCHANN

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Stephan Schann currently holds the Head of Research position at Domain Therapeutics, a biopharmaceutical company focusing on GPCR drug discovery and early development. He is managing different projects from the gene to the preclinical candidate on targets such as mGluR4 PAM, mGluR2 NAM, mGluR3 PAM or GLP-1R PAM for CNS and metabolic indications. He is also responsible for DTect-All™, the technological platform used for drug discovery on challenging GPCRs. Before that, Stephan spent 6 years at Faust Pharmaceuticals, a CNS clinical biopharmaceutical company, where he set up the medicinal chemistry activity. Prior to his position at Faust, Stephan was Team Leader at EvotecOAI, Abingdon, UK from 2001 to 2003. Stephan received his PhD in medicinal chemistry from University de Strasbourg, France in 2001 working on the synthesis of the first imidazoline I1-selective ligands.

Structures of Active and Inactive G Protein Coupled Receptors: Implications for the Activation Mechanism and Pharmacology

Gebhard F.X. SCHERTLER

PAUL SCHERRER INSTITUTE, Villigen, Switzerland
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Gebhard F.X. SCHERTLER

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Prof. Gebhard Schertler is investigating G protein coupled receptors (GPCRs). When the group was located at the MRC Laboratory for Molecular Biology (Cambridge, UK), they focused on 3D structural analysis by X-ray and electron crystallography and solved the atomic structures of GPCRs (rhodopsin, beta adrenergic receptors). With this expertise, Schertler successfully revealed the mechanisms of light-induced rhodopsin activation and agonist-binding to a GPCR. Since his move to the PSI in 2009, Schertler established an interdisciplinary research group on GPCRs, including crystallography, electron microscopy, NMR, biophysics and bioinformatics and a platform for protein expression/purification/crystallization. He is also responsible for biological applications on the Swiss Free Electron Laser (SwissFEL) and is involved in the experimental setup and design of biology beamlines for optimization of both biomolecular nanocrystallography and biological X-FEL imaging. He is leading the Biomolecular Research Laboratory at the Paul Scherrer Institute (PSI) and he is Professor for structural biology at the ETH in Zürich, Switzerland.

The Discovery and Optimization of a Novel Series of LPA Receptor Antagonists with Efficacy in Multiple Mouse Models of Fibrosis

Jon SEIDERS

BMS, San Diego, United States
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Jon SEIDERS

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Senior Director of Chemistry BMS. Previous Positions: Senior Director of Chemistry Amira Pharmaceuticals (2005-2011 acquired by BMS); Research Fellow Merck (2001-2005);Postdoctoral Fellow Cal Tech (1999-2001 Bob Grubbs advisor); Ph.D. University of California at San Diego (1993-1999 Jay Siegel advisor); B.S. San Diego State University

Empowered Antibodies for Cancer Therapy

Peter SENTER

SEATTLE GENETICS, Bothell, United States
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Peter SENTER

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Peter Senter joined Seattle Genetics in August 1998 and has served as Vice President, Chemistry since September 2002. In February 2009, Dr. Senter was recognized as the company's first Distinguished Fellow. He leads Seattle Genetics' chemistry department, which carries out research in antibody-drug conjugate technologies, including the development of potent drug payloads, novel linker systems, conjugation methodology and mechanism of action studies. Prior to joining the company, Dr. Senter was with Cytokine Networks, Inc., the Bristol-Myers Squibb Pharmaceutical Research Institute and the Dana-Farber Cancer Institute, Harvard Medical School. Dr. Senter received a Ph.D. in Chemistry from the University of Illinois, and an A.B. in Biochemistry from the University of California, Berkeley. He is the Senior Editor of Bioconjugate Chemistry and is an Affiliate Professor of Bioengineering at the University of Washington. His research interests include targeted drug delivery, protein chemistry and biochemistry, and anti-cancer drug design. Dr. Senter has authored more than 120 scientific publications and holds more than 40 patents.

A Major Leap into the Chemical Space of Protein-Protein Interaction Inhibitors

Olivier SPERANDIO

INSERM, Paris, France
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Olivier SPERANDIO

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Olivier Sperandio received two Master Degrees, one in computational chemistry at the University of Paris Diderot, and the other in bioinformatics, biochemistry, and molecular biology at the University of Alabama at Birmingham (UAB) in the US. He then worked for a French start-up, MEDIT SA, and conversely completed a Ph.D training in the field of chemoinformatics and got his degree in 2007 in collaboration with the University of Paris Descartes. He is co-directing with Dr B. Villoutreix the in silico division of the CDithem Inserm plateform, specialized in protein-protein interactions (PPI) and the discovery of new therapeutic compounds against cancer and infectious and rare diseases. He has developed several chemoinformatics tools and has worked on the in silico screening of several protein targets including PPI targets, mainly in the field of Hemophilia and cancer. He is intensively working on the rationalization of the chemical space of protein-protein interaction inhibitors using chemoinformatics approaches and is now senior research associates at the Inserm since September 2010.

RaPID Discovery of Non-Traditional Peptide Drug Leads

Hiroaki SUGA

UNIVERSITY OF TOKYO, Tokyo, Japan
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Hiroaki SUGA

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Professor in the Laboratory of Bioorganic Chemistry and Chemical Biology, Department of Chemistry, School of Science, The University of Tokyo 3-7-1 Hongo, Bunkyo-ku, 113-0033 Tokyo, Japan http://www.chem.s.u-tokyo.ac.jp/users/bioorg/index.html Hiroaki Suga was Professor in Research Center for Advanced Science and Technology in the University of Tokyo from 2003 to 2010, and is now in the Department of Chemistry, Graduate School of Science in the same school. He is also a founder of biotechnology company, PeptiDream Inc. Tokyo.

Improved Prediction of in vivo Effects by Combining Cheminformatics and Short-term Assay Data

Experiences of Fragment-based Drug Discovery

Translational Strategies for Identifying Chemically Reactive Metabolites as Cause for Adverse Drug Reactions

Nico VERMEULEN

VU UNIVERSITY, Amsterdam, The Netherlands
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Nico VERMEULEN

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Selected employments: Professor of Molecular Toxicology (1985- ), Director of the Amsterdam Institute for Molecules, Medicines and Systems (AIMMS, 2010- ) and Head of the Department of Chemistry and Pharmaceutical Sciences (CPS, 2010-). Selected activities/honors: President-elect, President and Past-president (‘00-’05); Honorary member of ISSX (2004, lifetime); European ISSX Scientific Achievement Award (2006) and Honorary Doctorate of the University of Copenhagen (2011). Research interests: In general: Roles molecular and computational toxicology and drug metabolism can play in drug discovery, development and safety assessment; More specifically: toxication/detoxication mechanisms involving Cytochromes P450 (P450s) and Glutathione S-transferases (GSTs); in silico and in vitro prediction and screening of ADME-Tox properties, biocatalytic metabolite production and profiling and translational biomarkers of adverse drug reactions (ADRs).

Polymer-conjugates as Nano-sized Medicines

Maria VICENT

RESEARCH CENTRE PRÍNCIPE FELIPE, Valencia, Spain
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Maria VICENT

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María J. Vicent is the Head of the Polymer Therapeutics at Príncipe Felipe Research Center. After a PhD in material sciences between Castellón (Spain, Luis’ Lab.) and U.C. Berkeley (USA, Frechet’s Lab.), a Marie Curie funded postdoc in Prof. Duncan’s Lab. (Cardiff, UK) and one-year research associate position through a Marie Curie Reintegration contract at CIPF (Valencia, Spain); she was appointed as principal investigator in June 2006 to build the first Polymer Therapeutics Lab. in Spain. She has published more than 50 papers and book’s chapters, 2 editorials and she is a named inventor in 5 patents 2 of them already licensed. María was awarded with the ‘Idea Award’ from ‘Fundación de las Artes y las Ciencias’ for its ‘Polymer-based combination therapy’ approach in June 2008. She is the President of the Spanish-Portuguese Chapter of the Controlled Release Society and is chairing the Polymer Therapeutics Symposium: from Lab to Clinic, one of the most recognized conferences in the field.

Antimalarial Medicinal Chemistry “Opportunities and Challenges"

David WATERSON

MEDICINES FOR MALARIA VENTURE, Geneva, Switzerland
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David WATERSON

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David is a Project Director and medicinal chemistry adviser within the Discovery Team at Medicines for Malaria Venture (MMV) and is responsible for a number of Lead Generation and Lead Optimization projects within the MMV portfolio. He has over 25 years of experience in the global pharmaceutical sector as a medicinal chemist (principally at AstraZeneca UK) working in a variety of therapeutic areas. He also worked at AstraZeneca’s Bangalore site for two years where the focus was on the identification of new treatments for tuberculosis. He holds a PhD from Cambridge University.

A Novel Asymmetric Propargylation Reaction and its Application to the Large Scale Synthesis of Drug Candidates

Nathan YEE

BOEHRINGER INGELHEIM PHARMACEUTICALS, Ridgefield, United States
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Nathan YEE

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Nathan Yee received his Ph.D. degree in Organic Chemistry from the University of Illinois at Urbana-Champaign in 1991. After he completed his postdoctoral research at Yale University in 1992, he joined Boehringer Ingelheim Pharmaceuticals, Inc. and is currently Director of Department of Chemical Development. He is currently responsible for leading multidisciplinary functions including Process Research, Analytical Research, Chemical Catalysis, and Solid State/Crystallization Engineering, and developing scalable and cost-effective chemical processes for drug substance, and producing Active Pharmaceutical Ingredients to support preclinical and clinical studies. He published >70 scientific papers in peer-reviewed journals and is the co-inventor of >30 patent applications.

Ligand Efficiency and Physical Properties Control, the Keys to Successful Drug Discovery?

Rob YOUNG

GLAXOSMITHKLINE, Hertfordshire, United Kingdom
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Rob YOUNG

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Dr Robert J. Young, Group Leader, CSC Medicinal Chemistry, GlaxoSmithKline, Stevenage UK Education: undergraduate and postgraduate at University of Oxford, research with Professors Sir Jack Baldwin and George Fleet; post-doc Ben May Cancer Institute, University of Chicago, with Professor Ron Harvey; currently Honorary Visiting Lecturer, University of St Andrews. Professional experience, joined Wellcome in 1990, assimilated into GlaxoWellcome and subsequently GSK, working in antiviral, nitric oxide and anticoagulant fields, specialising in property based design. More recently in early stage projects, interfacing with Physical Chemistry and Fragment based drug design.

Innovation Needs New Ways of Thinking: Talk to a Chemical Biologist in Academia

Giovanna ZINZALLA

KAROLINSKA INSTITUTET, Cambridge, United Kingdom
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Giovanna ZINZALLA

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Dr Giovanna Zinzalla, Assistant Professor (Senior), Centre for Advanced Cancer Therapies (ACT!), MTC, Karolinska Institutet Stockholm (Sweden)
Research Field: Synthetic & Medicinal Chemistry/Chemical Biology, Protein-Protein Interactions, Cancer Therapy
Education and Formal Professional Experience: Giovanna Zinzalla is Assistant Professor (Senior) at the Centre for Advance Cancer Therapies of the Karolinska Institutet in Stockholm (Sweden). She obtained her MChem (2000) and PhD in bioorganic & organometallic chemistry (2003) at the University of Milan (Italy). In January 2004 she was awarded a Marie Curie EIF Fellowship and carried out postdoctoral research at the University of Cambridge (UK) with Prof. Steven Ley. In June 2006 she joined the UCL School of Pharmacy (London, UK) as a CRUK Senior Research Fellow in the Cancer Research UK unit directed by Prof. David Thurston. In January 2012 she was appointed Assistant Professor (Senior) with a tenure-track (forskare position) in Chemical Biology at Karolinska Institutet. Her research focuses on the development of chemical approaches to modulate protein-protein interactions in signalling pathways relevant to cancer.

Development of Small Molecule Embryonic Stem Cell Stimulators of Cardiogenesis: Case Study of a Medicinal Chemistry Approach

Targeting Protein-Protein Interactions in the Brain

Kristian STROMGAARD

UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
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Kristian STROMGAARD

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Professor Kristian Strømgaard received an MSc from University College London working in the laboratory of Robin Ganellin, the PhD was obtained from the Danish University of Pharmaceutical Sciences in 1999 and subsequently worked as a postdoctoral fellow in the group of Koji Nakanishi at Columbia University. He is currently Professor of Chemical Biology at the Department of Medicinal Chemistry, University of Copenhagen, where he works with a group of ca. 20 people with expertise in applying chemistry and biology in studies of membrane-bound proteins in the central nervous system. Specifically the group currently focuses on neuronal protein-protein interactions, ionotropic glutamate receptors and neurotransmitter transporters.

Discovery and SARs of Novel Benzimidazole Derivatives as Potential Flap Inhibitors Based on a Combined Ligand- and Structure-Based Virtual Screening

Erden BANOGLU

GAZI UNIVERSITY, Ankara, Turkey
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Erden BANOGLU

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Prof. Dr. Erden BANOĞLU Gazi University, Faculty of Pharmacy Department of Pharmaceutical Chemistry 06330 Yenimahalle, Ankara, Turkey Professor Banoğlu receives his B.S. (Pharmacy) and M.Sc. degrees (Pharmaceutical Chemistry) from the Gazi University (Turkey) and the Ph.D. degree from the University of Iowa (U.S.), having worked under supervision of Professor Michael W. Duffel at the Department of Medicinal and Natural Products Chemistry. He also preformed short term pre-doctoral (Aberdeen University, Scotland) and post-doctoral (University of Rhode Island, U.S. and Kumomoto University, Japan) studies in the area of medicinal chemistry. In 2010, he was promoted to be a full professor of medicinal chemistry at Gazi University, Faculty of Pharmacy. His research interests are concerned with the development of novel medicinal agents for inflammatory pathologies, especially targeting several enzymes in the arachidonate pathway, i.e. 5-lipoxygenase, FLAP and mPGES-1, as well as exploring the metabolic fates of some pro-carcinogen compounds leading to their bioactivation. His group uses molecular modeling techniques and synthetic approaches to develop novel inhibitors of these enzymes.

Structure-Activity-Relationship Study of (2S,3R)-3-(3-Carboxy-phenyl)-pyrrolidine-2-carboxylic Acid: Towards First Selective Kainate Receptor Subtype 3 (GluK3) Antagonist

Lennart BUNCH

UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
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Lennart BUNCH

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Lennart Bunch, Associate Professor, PhD. In 1996 he obtained his BSc degree in chemical engineering from the Technical University of Denmark. Shortly hereafter he moved to the USA to pursue a MSc degree in organic chemistry at Florida State University. In 1998 he graduated and returned to his home country to commence a PhD program at the University of Copenhagen focusing on organic chemistry as well as medicinal chemistry. In 2006 he was promoted to Associate Professor and established the research group: Chemical Neuroscience Group at the Department of Drug Design and Pharmacology, University of Copenhagen. His research interests include: Rational design and total synthesis of target molecules including development of new methodology as well as computer-aided molecular modelling. At the biological front the glutamate neurotransmitter system is in focus. He is dedicated to making a significant contribution to the development of novel psychiatric and neurological therapeutics.

Towards a Differential Antimalarial Drug Through the Tres Cantos Antimalarial Set (TCAMS)

Félix CALDERÓN

GLAXOSMITHKLINE, Madrid, Spain
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Félix CALDERÓN

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My research career started as an undergraduate student at the University of Turin, Italy (2000). As a graduate student, before starting my Ph. D. studies, I Joined to GlaxoSmithKline (2001) as a trainee for one year and to Ana Castro`s group at the Medicinal Chemistry Institute (Spanish Council for Scientific research (CSIC)). In 2002 I started my Ph. D. Studies focused in the synthesis of aza-sugars through a organocatalytic methods under the supervision of Dr. Alfonso Fernández Mayoralas at the Organic Chemistry Institute (CSIC) and, related with this project, I collaborated with Dr. ken Houk (University of California Los Angeles) in the elucidation of the double asymmetric induction of proline-catalyzed reactions by computational models. In 2007 I joined to GSK as a senior scientist of the former Medicinal Chemistry Department and since 2010 I was promoted to Principal Scientist in the Malaria Discovery Performance Unit (Tres Cantos-Medicines Development Campus).

Discovery of JNJ-18038683, a Selective 5-HT7 Receptor Antagonist: Preclinical and Clinical Evaluation

Nicholas CARRUTHERS

JOHNSON & JOHNSON R&D, San Diego, United States
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Nicholas CARRUTHERS

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Dr. Carruthers joined Janssen Pharmaceutical Research & Development L.L.C. 1999 as Chemistry Team Leader for La Jolla Neuroscience. Amongst his roles in the Neuroscience Team was to guide the chemistry effort in the histamine H3 receptor antagonist program, which has resulted in several clinical candidates. In addition he is responsible for other programs aimed at exploiting the many targets identified by his biology counterparts in La Jolla. Prior to joining Janssen Dr. Carruthers was at Schering-Plough for 13 years and at Hoechst Pharmaceuticals in the U.K. Dr. Carruthers obtained his Ph.D. in 1980 from Heriot-Watt University, Edinburgh, Scotland which was followed by a NATO-Research Fellowship at the University of California, Berkeley. He has over eighty published papers, in excess of one hundred patents and patent applications and was elected a Fellow of the Royal Society of Chemistry in 1997.

Fragments, Fits, Fingerprints: Structure-Based Virtual Screening for Fragment-Like GPCR Ligands

New Selective Androgen Receptor Modulators (SARM) for the Treatment of Cachexia

Pierre DEPREZ

GALAPAGOS, Romainville, France
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Pierre DEPREZ

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Pierre Deprez is head of medicinal chemistry at Galapagos in Paris. He is organic chemist by training and is graduate from the engineer school of chemistry in Paris (ENSCP) in 1987. He did his PhD thesis at the “Institut de Chimie des Substances naturelles” (ICSN) at Gif sur Yvette in France under the supervision of Pr Husson where is worked on asymmetric 1,3 dipolar cyclo-addition. He then joined the pharma company Roussel-Uclaf in 1991. He worked there for 10 years and became Aventis after different mergers. Pierre Deprez was involved in cardiovascular and then bone disease drug discovery. In 2002 he moved to a spin-off company of Aventis called proSkelia dedicated to bone diseases, where he was head of medicinal chemistry. Proskelia was eventually purchased by Galapagos in 2006 and Pierre Deprez is now heading a group of 50 medicinal chemists at Galapagos, involved mainly in bone and joint diseases, like osteoarthritis. Today he will give a presentation the identification of GLPG0492 as a selective androgen receptor modulator for the treatment of cachexia.

Optimization of Novel Alkylpyrazoles as Potent Antimalarial Agents

Beatriz DÍAZ HERNÁNDEZ

GLAXOSMITHKLINE R&D SPAIN, Tres Cantos, Spain
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Beatriz DÍAZ HERNÁNDEZ

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Beatriz Díaz, Medicinal Chemist. I joined GlaxoSmithKline in 2003 right after graduating in Chemistry from the Universidad Autonoma de Madrid. Since then, I have been working in the antimalarial drug discovery research, being part of different lead generation and lead optimization projects in collaboration with the MMV (cysteine protease inhibitors, cytochrome bc1 complex inhibitors and more recently in the whole-cell approach)

Targeting Oncogenic microRNAs: Toward New Chemotherapies

Maria DUCA

UNIVERSITY OF NICE SOPHIA ANTIPOLIS, Nice, France
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Maria DUCA

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Maria Duca is a CNRS Scientific Researcher at Chemistry Institut of Nice (University of Nice Sophia Antipolis). Dr. Duca earned her PhD in Molecular Biochemistry at Biophysics laboratory at National History Museum in Paris (France) under the supervision of Dr. Paola B. Arimondo. After a 2-years Research Associate position in the laboratory of Prof. Sidney M. Hecht at the University of Virginia (USA), she began her academic career as a CNRS Researcher in 2007. Dr. Duca’s research interests are in the domain of medicinal chemistry and focus on the design and synthesis of new antiviral and anticancer agents targeting specific sequences of DNA and RNA as well as on the biophysical studies related with the interactions between these agents and nucleic acids.

Anti-Adhesion Therapy for the Treatment of Infective Diseases

Beat ERNST

UNIVERSITY OF BASEL, Basel, Switzerland
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Beat ERNST

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Education & professional experience: Study of Chemistry at the ETH Zürich; 79-81: Postdoc with Prof. R. E. Ireland, Caltech, Pasadena, USA; 81-96: Ciba, Central Research Laboratory (84: group leader; 92: section head); 97-98: Novartis, Transplantation (Program head); 98: Professor of Molecular Pharmacy, University of Basel. Research Interests: Expression of therapeutically relevant lectins, synthesis of their carbohydrate ligands and mimetics thereof, investigation of carbohydrate-lectin interactions by molecular modeling, NMR, SPR and ITC. In collaboration with academic and industrial partners, in vivo evaluation of the potential of our mimetics in disease models and in the clinic (GMI-1070, sickle cell disease).

Boosting Ethionamide as a New Strategy to Fight Tuberculosis: in vitro and in vivo Validation of 1,2,4-Oxadiazole EthR Inhibitors

Marion FLIPO

U761 BIOSTRUCTURE AND DRUG DISCOVERY, Lille, France
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Marion FLIPO

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Marion Flipo graduated from the National Graduate School of Chemistry and Chemical Engineering of Lille (France). She received a masters degree in organic chemistry (2003) and a PhD in medicinal chemistry (2006) at the University of Lille (France). During her thesis she designed and synthesized metalloprotease inhibitors as antimalarial agents. Then she spent 6 months at the Ferring Research Institute (San Diego, CA), a company specializing in peptide research. In 2007 she took up a postdoctoral position in medicinal chemistry at the school of pharmacy of Lille (France). During her post-doc she synthesized focused libraries using combinatorial chemistry for the discovery of new antituberculous agents. She has been an assistant professor in organic chemistry at the University of Lille in the Biostructures and Drug Discovery unit (Inserm U761) directed by Pr Benoit Deprez since September 2008. Her research focuses on the development of new strategies to fight tuberculosis, based on the boosting of known antibiotics. She works on the design and optimization of inhibitors of EthR, a transcriptional repressor implicated in the innate resistance of Mycobacterium tuberculosis to the antituberculosis drug ethionamide.

Total Synthesis of New Functionalized Epothilone Analogs for Prodrug Design and Tumor Targeting

Fabienne GAUGAZ

ETH ZÜRICH, Zürich, Switzerland
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Fabienne GAUGAZ

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Fabienne Gaugaz studied pharmacy first at the University of Lausanne (2002-2004), Switzerland for the first and second years and then moved to ETH Zürich (2004-2007) to finish the Federal Pharmacist Diploma and obtain a master degree in pharmaceutical sciences in 2007. Fabienne then spent four months working in community pharmacy before starting a PhD. Now in her fourth year as a PhD student at ETH Zürich, Fabienne’s research field reaches from the total synthesis of drugs to the analysis of their biological activities in vitro and modulation of their activities by conjugation with peptides. Her PhD thesis entitled “Synthesis and Biological Profiling of Epothilone Analogs, Prodrugs and Conjugates” is supervised by Prof. Dr. Karl-Heinz Altmann.

The Discovery and Early Clinical Development of CNV1014802: A Novel, NAV1.7 Selective, State-Dependent Sodium Channel Blocker for the Treatment of Neuropathic Pain

Gerard GIBLIN

CONVERGENCE PHARMACEUTICALS, Cambridge, United Kingdom
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Gerard GIBLIN

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http://www.convergencepharma.com

Ged is a co-founder of Convergence Pharmaceuticals, based in Cambridge UK, and is presently Head of Chemistry and Preclinical Development and a member of the Executive Management Team. In this role Ged is responsible for Discovery Chemistry, Preclinical and Manufacturing. Ged has over 20 years Drug Discovery experience including 12 years in Pain Discovery. He has been responsible for more than 12 development candidates including multiple phase I and II assets for pain. Prior to the launch of Convergence Ged was Head of Medicinal Chemistry at GlaxoSmithKline where he built and led a department of over 30 chemists that pursued all aspects of drug discovery up to clinical candidate nomination. Ged has over 100 patents and peer reviewed publications to his name and is a member of the Biological and Medicinal Chemistry Committee of the RSC and Chair of the RSC Ion Channels conference organising committee.

A Chemical Biology Tool Developed in Yeast for Direct Targets Identification of a Bioactive Compound

Marie-Edith GOURDEL

HYBRIGENICS SAS, Paris, France
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Marie-Edith GOURDEL

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Marie-Edith GOURDEL is currently Head of Chemistry at Hybrigenics, a biotechnology-oriented company based in Paris. She‘s involved in Chemical Biology, Protein-Protein Interactions, HTS and Medicinal Chemistry follow-up in various therapeutic areas. She received her PhD in Organic Chemistry in 1996 under the direction of Pr Huet at the University of Le Mans (France). Her research focused on the synthesis of anti-viral agents and asymmetric synthesis. She carried out 2 postdoctoral works: the first one with Pr G. Guillaumet and Pr M-C Viaud at the University of Orléans (France), a UCB Pharma collaboration for 18 months. She then moved to the University of Nottingham (UK) end of 1998 with Pr A. Armstrong (Imperial College now) and worked on the synthesis of natural products. She started her industrial career at Cephalon (France/USA) early 2000 as a Medicinal Chemist, and was involved in CNS and Oncology diseases (2000-2005). She then joined Novexel, in 2005, a biopharmaceutical company specialized in antibacterial discovery and development, to overcome antimicrobial resistance. She was a Principal Scientist leading a group in Medicinal Chemistry in one side, and project leader of a development program targeted pseudomonas aeruginosa. Novexel was acquired by AstraZeneca in 2010.

Targeted, Polymer-Based Nanoparticles for Delivery of Camptothecin

Han HAN

CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States
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Han HAN

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Han received her combined bachelors degree in Chemical Engineering and Chemistry from the University of Melbourne in 2008. She is currently pursuing a PhD in Chemical Engineering at Caltech under the guidance of Professor Mark E. Davis (expected completion December 2012). Han’s thesis project involves the design and development of a targeted, polymer-based nanoparticle delivery system that is capable of being translated into clinical studies. She has experience in nanoparticle delivery of small hydrophobic drugs and siRNA; specifically, in targeted nanoparticle design, synthesis and characterization both in vitro and in vivo. Han’s long-term career goal is to be involved in the design and development of innovative therapeutics from the lab bench to the clinic.

Aldehyde Oxidase Metabolism - An Emerging but Surmountable Problem in Modern Drug Discovery

Peter JONES

PFIZER, Cambridge, United States
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Peter JONES

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I am currently a Medicinal Chemist working at the Cambridge North (Massachusetts) site within Pfizer Worldwide Medicinal Chemistry. I graduated from the University of Manchester Institute of Science and Technology in the UK, and then did a Ph.D at the University of Cambridge, UK, in the group of Professor Steve Ley. This was followed by a Postdoctoral Fellowship in the group of Paul Wender at Stanford University, California. I then worked at a biotechnology start-up company for 2 years, Genesoft Pharmaceuticals, in South San Francisco, before returning to the UK to join Pfizer Worldwide Medicinal Chemistry in Sandwich. I recently transferred to the Cambridge North site in Massachusetts to continue with Pfizer Worldwide Medicinal Chemistry, where I am now entering my 8th year with the company.

4-Phenyl Imidazoles: A Novel Class of Phosphodiesterase 10A (PDE10A) Inhibitors as a Potential New Generation of Antipsychotics

Jan KEHLER

H. LUNDBECK A/S, Valby, Denmark
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Jan KEHLER

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Current and past appointments: Research fellow, Royal Danish School of Pharmacy, Copenhagen, Denmark (1998–1999), Research Chemist, Med. Chem. Research, H. Lundbeck A/S, Denmark (1999–2002); Principal Scientist, Med. Chem. Research, H. Lundbeck A/S, Denmark (2002-2004); Sectionleader, Med. Chem. Research, H. Lundbeck A/S, Denmark (2004-2006); Group Leader, Med. Chem. Research, H. Lundbeck A/S, Denmark (2006–2010); senior scientist, Discovery Chemistry & DMPK. H. Lundbeck A/S, Denmark (2010-present) Research interests: (1) Synthetic bioorganic chemistry (2) neurochemical research (3) Drug discovery in psychiatric and neurological diseases (4) project management and research leadership (5) ”mind altering drugs” and neuropsychology. Management, publications, innovation and patents: (1) eight years experience as a research group leader and project manager (2) Author or co-author of more than 50 research papers in peer-reviewed scientific journals, (3) Inventor or co-inventor on more than thirty five patents or patent applications, (4) Co-inventor of five clinical candidates (5) supervisor for several master- and Ph.D.-students (6) Referee/censor at the University of Copenhagen.

Disrupting the Amyloid Cascade- BACE 1 Inhibition for the Treatment of Alzheimer's Disease

Daniel LA

AMGEN, Cambridge, United States
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Daniel LA

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Daniel, a New York native, received his Ph.D. in 2000 from the lab of Prof. Amir Hoveyda at Boston College studying asymmetric catalysis. Subsequently, he joined the lab of Prof. Dave Evans as an American Cancer Society postdoctoral fellow working primarily in the realm of natural product synthesis. He later joined the medicinal chemistry department at Amgen, Cambridge in 2003. Currently he is a Principal Scientist working in the neuroscience and oncology therapeutic areas.

From the Clinic to the Lab and Back -Discovery of PAN-CDK Inhibitors

Ulrich LÜCKING

BAYER HEALTHCARE, Basel, Switzerland
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Ulrich LÜCKING

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Ulrich Lücking is a Senior Research Scientist at Bayer HealthCare AG in Berlin. Ulrich started his industrial career with the former Schering AG in 2001, working across multiple therapeutic areas, mainly in lead optimization, to successfully deliver multiple clinical candidates. His efforts were instrumental in the discovery of clinical candidates in the CDK inhibitor programs, and in the Androgen Receptor Suppressor program. Prior to joining industry, Ulrich studied chemistry at the University of Hannover in Germany. As an Erasmus student, he spent a year in the laboratory of Prof. Steven Ley at Cambridge University, UK. He then received his Ph.D. under the direction of Prof. Andreas Pfaltz at the Max-Planck-Institut für Kohlenforschung, Mülheim an der Ruhr, Germany, and carried out postdoctoral work in the laboratories of Prof. Julius Rebek at the Scripps Research Institute, USA.

Novel Triazolopyridine Compounds as Selective JAK1 Kinase Inhibitors: From Target Discovery to the Clinical Candidate GLPG0634

Christel MENET

GALAPAGOS, Brussels, Belgium
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Christel MENET

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Christel Menet. I did my PhD at the University of Manchester with professor Clayden, on ionionic cyclisations. I then moved to EvotecOAI, where I stayed almost two years. Moved to Strasbourg in France to work for Faustpharmaceuticals, on CNS targets. And finally to Galapagos, where I worked on a number of targets involved in inflammation or osteoporosis. I am now a group Leader and a project director working for 7 years at Galapagos.

Multi-Criteria Decision Making Methods: A Paradigm Applied to the Discovery of the First SV2C Selective Chemical Series

Joël MERCIER

UCB, BRAINE-L'ALLEUD, Belgium
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Joël MERCIER

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I am currently research project leader and associate director in medicinal chemistry within the Discovery Research Team at UCB Pharma (Belgium) and I am responsible of leading CNS research projects from the lead generation until the candidate selection phase. Professional experience: I have over 10 years of experience in the biopharmaceutical sector as a medicinal chemist leading various CNS projects (SV2 proteins, GPCRs, ion channels). I also worked one year in the PET (Positron Emission Tomography) center at the University of Louvain-la-Neuve (Belgium) where I gained experience in PET radiochemistry which I now use to lead the PET chemistry activities within UCB Pharma. Education: Master in Chemical sciences obtained from the University of Namur in 1998, PhD in organic synthesis (stopped in 2000) at the University of Namur in the laboratory of Professor Alain Krief

Endoperoxide-Vinyl Sulfone Hybrids as Dual Acting Antimalarials

Rudi OLIVEIRA

IMED.UL, Lisboa, Portugal
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Rudi OLIVEIRA

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Rudi Oliveira received his master degree in Pharmaceutical Sciences from the Faculty of Pharmacy, University of Lisbon (2009). As an undergraduate student, he participated in medicinal chemistry research projects in the Faculty of Pharmacy, Lisbon, and in the Institute of Cancer Therapeutics, Bradford, UK. Currently he is developing a PhD project in Medicinal Chemistry, focused on development of endoperoxide-based hybrid compounds and pro-drugs targeting the blood-stage of infection by malaria parasites, as a strategy to overcome drug resistance. This project is being developed at the Research Institute for Medicines and Pharmaceutical Sciences (iMed.UL), University of Lisbon, and at the University of Liverpool, UK, under the supervision of Professors Rui Moreira, Francisca Lopes, and Paul M O'Neill.

Developments of an Integrated in Silico Prediction System of Drug Toxicity Endpoints

Manuel PASTOR

UNIVERSITAT POMPEU FABRA, Barcelona, Spain
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Manuel PASTOR

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Born in Madrid (Spain) in 1965. PhD in Pharmacy by the University of Alcalá (Spain). Post-doctoral stays at the Laboratory of Chemometics, University of Perugia (Italy), under the supervision of Sergio Clementi and Gabriele Cruciani and at the Laboratory of Molecular Pharmacology, University of Alcalá, under the supervision of Federico Gago. Since 2000, professor at the University Pompeu Fabra, and head of the Computer-Aided Drug Design laboratory, at the GRIB, Barcelona (Spain). Author of more than 50 scientific articles and book chapters and main responsible of research projects in the field of drug design. Developer of numerous scientific software and methods used in pharmaceutical research (GOLPE, ALMOND, Greater, SHOP, Pentacle). At present, the main research lines are related with the development of in silico toxicity prediction systems and multi-scale modeling.

Discovery and Profiling of Potent and Selective mTOR Inhibitor GDC-0349

Zhonghua PEI

GENENTECH, INC, South San Francisco, United States
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Zhonghua PEI

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Dr. Pei is currently a senior scientist at Genentech (a member of Roche) and project team leader, leading a multidisciplinary team to discover innovative new medicine. He has extensive drug discovery experience in therapeutic areas of diabetes/obesity, oncology and immunology. He has made significant contributions the discovery of several clinical candidates of small molecules. Zhonghua started his industrial career at Abbott Laboratories after he obtained his Ph. D degree from MIT in organic chemistry, his MS degree from Rensselaer Polytechnic Institute and BS from University of Science and Technology of China.

The Power of Molecular Matched-Pair Analysis in Drug Design: Case Study of Oxadiazoles

Alleyn T. PLOWRIGHT

ASTRAZENECA, Cambridge, United Kingdom
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Alleyn T. PLOWRIGHT

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Dr. Alleyn Plowright Employed in AstraZeneca R&D (2002-today) Current position as Senior Principal Scientist in the Medicinal Chemistry Department within the Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca R&D. Based in Mölndal, Sweden. Previously held roles as an Associate Director, leading a section of 40 people working on a range of Drug projects, and Team Leader in both Medicinal Chemistry AstraZeneca Mölndal, Sweden and Alderley Park, UK, working on a range of projects in Oncology and CVGI diseases. Previously carried out Postdoctoral Studies with Professor Andrew Myers (Harvard University, USA, 2000-2001) and before this carried out Postgraduate Studies with Professor Gerry Pattenden (University of Nottingham, UK, 1996-1999).

Tetrahydroquinoline Derivatives as Potent and Selective Factor XIA Inhibitors

Mimi QUAN

BMS, Pennington, United States
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Mimi QUAN

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Dr. Mimi Quan is currently a Research Fellow at Bristol-Myers Squibb Pharmaceutical Company. Mimi received her B.S. (1985) and Ph.D.(1990) degrees in Organic Chemistry from the University of California, Los Angeles under the direction of Professor Donald J. Cram. Mimi joined the Medicinal Chemistry Department of DuPont Pharmaceuticals in 1990 and moved to Hopewell, New Jersey in 2002 after the Bristol-Myers Squibb acquisition of DuPont Pharmaceuticals. During her career, Mimi has worked on many targets in the cardiovascular area including angiotensin II receptor antagonists, IIb/IIIa receptor antagonists, thrombin inhibitors, factor Xa inhibitors, and factor XIa inhibitors. She is a recipient of the BMS Ondetti Cushman award for her contributions in the factor Xa program and the discovery of raxazaban. She has authored and co-authored over 100 scientific publications and patents.

4,4-Dioxo-5,6-Dihydro-[1,4,3]Oxathiazines as a Novel Class of 11ß-HSD1 Inhibitors for the Treatment of Diabetes

Kurt RITTER

SANOFI, Frankfurt, Germany
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Kurt RITTER

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Kurt received his Ph.D. in chemistry from the University of Tübingen in 1985 and joined as post-doc the group of Prof. E.J. Corey at Harvard University working on a biomimetic route to preclavulone A. He spent two years (87-89) at the University of Heidelberg as Liebig Stipendiate developing novel approaches to and applications of organotin compounds. In 1989 he joined BASF AG, Ludwigshafen, as a medicinal chemist and worked in the field of immunology and oncology (Pgp-modulators, dolastatins). In 1995 he moved again to the US to establish a medicinal chemistry group at the BASF Bioresearch Corporation in Worcester (since 2001 Abbott Bioresearch Center). He iniated a collaboration with Mitotix, Cambridge, on cell cycle inhibitors and focused on the identification and development of kinase inhibitors for the treatment of immunological disorders (LCK, COT) and the reduction of tumor angiogenesis (KDR, TIE-2). After his return 2001 to Germany, he became section head of medicinal chemistry at Aventis, now Sanofi-Aventis, in Frankfurt am Main and worked on a number of different projects in the area of cardiovascular and metabolic diseases (protease and kinase inhibitors, GPCR agonists).

New Inhibitors of Cathepsin A for the Treatment of Cardiovasuclar Diseases

Sven RUF

SANOFI, Frankfurt, Germany
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Sven RUF

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Dr. Ruf received his PhD in organic chemistry in 1999 after working in the group of Prof. Regitz at the University of Kaiserslautern. After a post-doctoral stay in 2000 in Prof. Trost's group at Stanford University as a Feodor Lynen Fellow, he joined the Medicinal chemistry department at Sanofi in Frankfurt. He developed a focus on metal-catalyzed reactions, parallel syntheses and the application of these technologies for the design of novel enzyme inhibitors. As a project team leader, he is responsible for several lead identification and optimization programs and is currently holding a position as senior scientist in the Lead Generation and Compound Realization unit in Frankfurt.

Potent and Selective Autotaxin (ATX) Inhibitors

Kai SCHIEMANN

MERCK KGAA, DARMSTADT, Germany
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Kai SCHIEMANN

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02/ 1992 Diploma in the group of Prof. Dr. L. F. Tietze, Göttingen 03/ 1992-01/ 1995 Doctoral thesis guided by Prof. Dr. L. F. Tietze, Göttingen, ”diastereoselective allylation of carbonyl compounds, design of enantiomerically pure secondary und tertiary homoallylic alcohols” 11/ 1995-11/ 1996 Postdoc working on the „partial asymmetric synthesis of N-Methylwelwit¬indolinone C isothiocyanate“, in the group of Prof. Dr. J. P. Konopelski, University of California, Santa Cruz, USA 04/ 1997-02/ 1999 Postdoctoral Fellow at Parke-Davis, Division of Warner Lambert, Ann Arbor, MI, USA, in the MedChem department working in cancer research and combinatorial chemistry Since 02/ 1999 Medicinal Chemistry department, Merck KGaA, Merck Serono in Darmstadt 12 publications/poster and ca. 60 patents in the area of central nervous system and oncology.

Novel Potent and Selective NAM'S of the GABAA 5 Receptor Sub-Type

Andrew THOMAS

F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland
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Andrew THOMAS

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Dr Andrew W. Thomas, Senior Leader, Vice-Director, Medicinal Chemistry, F. Hoffmann-La Roche, Ltd. Basel, Switzerland. Andrew received his chemistry education in the University towns of Aberdeen, St. Andrews and Cambridge before joining F. Hoffmann-La Roche, Ltd. Basel, Switzerland, in 1999 as a Medicinal Chemist. After an initial period working in anti-infective research, his research has mainly been devoted to the areas of neuroscience and is an inventor on 59 patents and is an author on 40 publications (more than 800 citations). Andrew has been involved as a Lead Chemist on a number of programs covering both early and late stage research with a focus on Schizophrenia and cognitive disorders such as Alzheimer’s disease and more recently in orphan indications such as Down Syndrome. Andrew is currently Head of Medicinal Chemistry 3, where his team focus on innovative approaches to discover novel medicines in the areas of both neuroscience and cardiovascular metabolic disease. Andrew is also responsible for recruitment in Discovery Chemistry and hosts the biannual European meeting Roche Symposium – Leading Chemists. Andrew became a Fellow of the Royal Society of Chemistry in 2007 and is a member of the EFMC-ILC since 2011.

Discovery of the Clinical Candidate TMC647055, a non Nucleoside Inhibitor of the Hepatitis C Virus NS5B Polymerase

Sandrine VENDEVILLE

JANSSEN INFECTIOUS DISEASES, Beerse, Belgium
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Sandrine VENDEVILLE

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Dr Sandrine Vendeville is a Principal Scientist and Medicinal chemistry project leader at Janssen Infectious Diseases in Beerse, Belgium. Over 12 years she has contributed to multiple lead optimization projects in the antiviral field, including HIV protease inhibitors active on multidrug resistant mutants, and HCV protease and non-nucleoside inhibitors. She successfully delivered several clinical candidates for Hepatitis C. Prior to joining Janssen, Sandrine obtained a PhD in medicinal chemistry from the University of Lille (France) in 1999. Sandrine also completed her education with a post-doc at University College London with Prof. Karl Hale and a master in pharmaceutical sciences from the School of Pharmacy of UCL (Belgium, 2010). Sandrine is an inventor/author of 38 patents and publications.

Towards Modulators of GABA Transporters: Screening of "Pseudo-static" Dynamic Combinatorial Libraries by ms Binding Assays

Klaus T. WANNER

LUDWIG - MAXIMILIANS-UNIVERSITÄT MÜNCHEN, Munich, Germany
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Klaus T. WANNER

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Prof. Dr. Klaus T. Wanner is full professor of Pharmaceutical Chemistry at the Ludwig-Maximilians-Universität München. His research fields are the development of subtype selective inhibitors of GABA transporters, asymmetric syntheses, and the development of biological binding assays based on mass spectrometry. He studied chemistry and pharmacy at the Technical University Munich and the Ludwig-Maximilians-Universität München. After obtaining his PhD under supervision of Prof. Dr. F. Eiden (Ludwig-Maximilians-Universität München) in 1983, he worked as Post-Doc in the research group of Prof. A. I. Meyers at Colorado State University, Fort Collins. When he returned to Munich, he began working on his 'Habilitation' (professoral thesis) on asymmetric synthesis of bioactive compounds which he completed in 1988. He became associate professor of Pharmaceutical Chemistry at the Freie Universität Berlin in 1990. Since 1994, he is full professor at the Ludwig-Maximilians-Universität München.

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