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|
| Sunday September 7, 2014 |
| 16:15 | Opening Ceremony |
|
| 16:35 | Portugal: the Right Place to build Partnerships in Health |
Dr Joaquim CUNHA
(HEALTH CLUSTER PORTUGAL, Maia, Portugal) |
| 16:50 | Partnership between Public and Private Sources: Pharma and IMI Perspective |
Dr Paul Peter TAK
(EFPIA, Brentford, United Kingdom) |
| 17:10 | EFMC Award Ceremony |
|
| 17:35 | The Nauta Award for Pharmacochemistry
Pursuing Compound Quality |
Dr Paul LEESON
(GLAXOSMITHKLINE, Nuneaton, United Kingdom) |
| 18:20 | High Resolution Mass Spectrometry in Clinical Proteomics |
Prof. Dr Matthias MANN
(MAX PLANCK INSTITUTE OF BIOCHEMISTRY, Martinsried, Germany) |
| 19:10 | Welcome Reception |
|
| Monday September 8, 2014 |
| 08:30 | The UCB-Ehrlich Award for Excellence in Medicinal Chemistry
Small Molecule Control Of Intracellular Protein Levels |
Prof. Craig CREWS
(YALE UNIVERSITY, New Haven, CT, United States) |
| 09:15 | The Prous Institute-Overton and Meyer Award for New Technologies i Drug Discovery
Thermodynamics Assisted Drug Discovery |
Dr György G. FERENCZY (HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary)
Prof. György KESERU (HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary) |
| 10:00 | Exhibition & Coffee |
|
| 1.1 Inflammation: the Common Link in Multifactorial Disorders? | 1.2 Computational Approaches To Guide Medicinal Chemistry | 1.3 Organic Synthesis that Changed Medicinal Chemistry |
| 10:30 | Session Chair |
Prof. Angeliki KOUROUNAKIS
(UNIVERSITY OF ATHENS, Athens, Greece) |
| 10:35 | Inflammation, Obesity and Metabolic Disease |
Dr Ajay CHAWLA
(UNIVERSITY OF CALIFORNIA, San Francisco, United States) |
| 11:15 | CB2 Agonists Protect from Inflammation Related Kidney Damage and Fibrosis |
Dr Uwe GRETHER
(F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
| 11:35 | The Discovery of APD334, a Selective S1P1 Functional Antagonist |
Dr Robert JONES
(ARENA PHARM, SAN DIEGO, United States) |
| 11:55 | Discovery of Small Molecule Rorγ Modulators for the Treatment of Autoimmune Diseases |
Dr Frank NARJES
(ASTRAZENECA, Gothenburg, Sweden) |
|
| 10:30 | Session Chair |
Prof. Helmut GRUBMÜLLER
(MAX PLANCK INSTITUTE FOR BIOPHYSICAL CHEMISTRY, Göttingen, Germany) |
| 10:35 | Mechanoenzymatics of Biomolecular Machines: Free Energies, Dynamics, Function |
Prof. Helmut GRUBMÜLLER
(MAX PLANCK INSTITUTE FOR BIOPHYSICAL CHEMISTRY, Göttingen, Germany) |
| 11:15 | Efficient Determination Of Protein-Ligand Standard Binding Free Energies And Permeabilities With A Computational Microcalorimeter |
Dr Chris CHIPOT
(UNIVERSITY OF ILLINOIS, Urbana, United States) |
| 11:35 | Binding Affinity Prediction from Molecular Simulation – Soon a Standard Method in Structure-Based Drug Design? |
Dr Clara CHRIST
(BAYER, Berlin, Germany) |
| 11:55 | P-Glycoprotein/Membrane Role on Multidrug Resistance: Insights from In Silico Studies |
Mr Ricardo FERREIRA
(FACULTY OF PHARMACY, UNIVERSITY OF LISBON, Lisbon, Portugal) |
|
| 10:30 | Session Chair |
Dr Morten JORGENSEN
(H. LUNDBECK A/S, Valby, Denmark) |
| 10:35 | Recent Advances In Asymmetric Catalysis |
Prof. Erick M. CARREIRA
(ETH ZÜRICH, Zürich, Switzerland) |
| 11:15 | New Stereoselective Organocatalytic Reactions for the Synthesis of Isoquinoline Alkaloids |
Prof. Pier Giorgio COZZI
(UNIVERSITY OF BOLOGNA, Bologna, Italy) |
| 11:35 | Metalation of Polyfunctional Heterocyclic Compounds: Applications in Agrochemistry |
Dr Marc MOSRIN
(BAYER CROPSCIENCE AG, Frankfurt am Main, Germany) |
| 11:55 | Development of Novel Building Blocks to Accelerate Drug Discovery |
Dr Pavel MYKHAILIUK
(ENAMINE, Kyiv, Ukraine) |
|
|
| 12:15 | Exhibition & Lunch |
|
| 2.4 Combating Antibiotic Resistance | 2.5 Taming Natural Products: Novel Natural Products, Complex Synthesis, Mutasynthesis | 2.6 Mechanism-Based Prediction of Drug-Induced Liver Injury
(Eufeps Session) |
| 13:15 | Session Chair |
Prof. Ada YONATH
(WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel) |
| 13:20 | Aminoglycoside Mechanisms of Action, Resistance and Toxicity – Prospects for Antibiotic Drug Development |
Prof. Erik BOËTTGER
(UNIVERSITY OF ZÜRICH, Zürich, Switzerland) |
| 14:00 | Visualising Novel Macrolide Antibiotics Bound to Their Ribosomal Target |
Prof. Stephen DOUTHWAITE
(UNIVERSITY OF SOUTHERN DENMARK, Odensen, Denmark) |
| 14:20 | The Ribosome as a Drug Target: Insights from Structural Investigations - Towards Rational Drug Design |
Dr Moran SHALEV-BENAMI
(WEIZMANN INSTITUTE, Rehovot, Israel) |
| 14:40 | Antagonists of the Pseudomonas Quinolone Signal Receptor (PQSR) as Promising Anti-Virulence Agents |
Dr Martin EMPTING
(HELMHOLTZ-INSTITUTE F. PHARMACEUTICAL RESEARCH SAARLAND, Saarbrücken, Germany) |
|
| 13:15 | Session Chair |
Prof. Anake KIJJOA
(UNIVERSITY OF PORTO, Porto, Portugal) |
| 13:20 | Natural Products as Driving Force for Innovation in Pharmaceutical Research and Development |
Dr Esther SCHMITT
(NOVARTIS, Basel, Switzerland) |
| 14:00 | Sponging Off Nature for New Drug Leads |
Prof. Raymond ANDERSEN
(UNIVERSITY OF BRITISH COLUMBIA, Vancouver, Canada) |
| 14:20 | Bioactive Secondary Metabolites From The Soil And Marine-Derived Fungi Of The Genus Neosartorya |
Prof. Anake KIJJOA
(UNIVERSITY OF PORTO, Porto, Portugal) |
| 14:40 | From Malaysian Biodiversity to the Total Synthesis of Dual Inhibitors of BCL-XL and MCL-1 Anti-Apoptotic Protein |
Dr Fanny ROUSSI
(ICSN - CNRS, Gif sur Yvette, France) |
|
| 13:15 | Session Chair |
Prof. Nico VERMEULEN
(VU UNIVERSITY, Amsterdam, The Netherlands) |
| 13:20 | Mechanism-Based Prediction of Drug-Induced Liver Injury |
Dr Christopher GOLDRING
(UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom) |
| 14:00 | Strategies to Identify and Manage the Risks of Chemically Reactive Drug Metabolites |
Prof. Nico VERMEULEN
(VU UNIVERSITY, Amsterdam, The Netherlands) |
| 14:20 | Being More Certain About Uncertainty In Computational Toxicology Modeling |
Dr Scott BOYER
(KAROLINSKA INSTITUTET, Södertälje, Sweden) |
| 14:40 | Covalent Modification of Histones by Nevirapine - A Plausible Pathway to Nevirapine-Induced Cancers? |
Dr Alexandra ANTUNES
(INSTITUTO SUPERIOR TÉCNICO, Lisbon, Portugal) |
|
|
| 15:00 | Exhibition & Coffee |
|
| 15:30 | MedChemComm Prize Winner : Phage Selection Of Bicyclic Peptides For Therapeutic Application |
Prof. Christian HEINIS
(ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE (EPFL), Lausanne, Switzerland) |
| 3.7 EFMC Session | |
|
|
| 15:55 | Session Chair |
Dr Phil JONES
(UNIVERSITY OF DUNDEE, Glasgow, United Kingdom) |
| 16:00 | The Open Phacts Discovery Platform - Semantic Data Integration For Medicinal Chemists |
Prof. Gerhard ECKER
(UNIVERSITY OF VIENNA, Vienna, Austria) |
| 16:30 | European Lead Factory - Game Changing For Innovative Medicines |
Dr Dimitrios TZALIS
(TAROS CHEMICALS, Dortmund, Germany) |
| 17:00 | Funding Opportunities with the Innovative Medicines Initiative 2 |
Dr Colm CARROLL
(INNOVATIVE MEDICINES INITIATIVE, Brussels, Belgium) |
|
|
|
| 17:30 | Poster Session I and Networking |
|
| 19:30 | End of the day |
|
| 20:30 | Concert (free of charge, but subject to registration) |
|
| Tuesday September 9, 2014 |
| 08:30 | Prize Ceremony |
|
| 08:35 | EFMC Prize for a Young Medicinal Chemist in Industry
Design, Synthesis and Properties of Potent Inhibitors of Pseudomonas Aeruginosa Deacetylase LpxC |
Dr Grazia PIIZZI
(NOVARTIS PHARMA, Basel, Switzerland) |
| 08:55 | EFMC Prize for a Young Medicinal Chemist in Academia
Inhibitors and Substrates of the Human Lysine Deacylase Enzymes |
Prof. Christian A. OLSEN
(UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark) |
| 09:15 | Plenary Lecture |
Dr Sabine HADIDA
(VERTEX PHARMACEUTICALS, San Diego, United States) |
| 10:00 | Exhibition & Coffee |
|
4.8 Applications of Positron Emission Tomography in Drug Discovery
(ACS Session I) | 4.9 Decoding Disease: Liganding and Drugging Bromodomain Epigenetic Readers | 4.10 Organic Synthesis: New Developments
(EuCHemS Session) |
| 10:30 | Session Chair |
Dr Sam BONACORSI
(BRISTOL-MYERS SQUIBB, Princeton, United States) |
| 10:35 | PET Imaging: Synthesis of Radiopharmaceuticals and their Application in Personalized Medicine and Drug Discovery |
Dr Peter J.H. SCOTT
(UNIVERSITY OF MICHIGAN, Ann Arbor, United States) |
| 11:15 | A Rational Approach to the Development of Radioligands and PET Ligands for Drug Development |
Dr Chad ELMORE
(ASTRAZENECA PHARMACEUTICALS, Mölndal, Sweden) |
| 11:35 | Design, Synthesis and Development of Lysophosphatidic Acid Receptor 1 (LPA1) PET Radioligands for Lung Receptor Occupancy Imaging |
Dr Sam BONACORSI
(BRISTOL-MYERS SQUIBB, Princeton, United States) |
| 11:55 | Quantitative Imaging of Mglu5 Allosteric Binding Site and its Occupancy by Positron Emission Tomography with The Novel Fluorine-18 Labelled Probe [18f]Pss232 |
Dr Stefanie KRAMER
(ETH ZÜRICH, Zürich, Switzerland) |
|
| 10:30 | Session Chair |
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
| 10:35 | BETting on Bromodomains: Developing Inhibitors of the Bromodomain-Acetyl-Lysine Interaction |
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
| 11:15 | A First In Class Chemical Probe For Family VIII Bromodomains |
Dr Dafydd OWEN
(PFIZER, Cambridge, United States) |
| 11:35 | Epigenetic Drug Discovery: Small Molecule Inhibitors of Class IV Bromodomain Proteins |
Prof. Paul FISH
(UCL SCHOOL OF PHARMACY, London, United Kingdom) |
| 11:55 | Interrogation the Bromodomain Family through Chemical Biology |
Dr Steve BELLON
(CONSTELLATION PHARMACEUTICALS, Cambridge, United States) |
|
| 10:30 | Session Chair |
Prof. Péter MÁTYUS (SEMMELWEIS UNIVERSITY, Budapest, Hungary)
(THERMO FISHER SCIENTIFIC) |
| 10:35 | Experiences with Natural Product Total Synthesis |
Prof. Alois FÜRSTNER
(MAX PLANCK INSTITUT FUR KOHLENFORSCHUNG, Muelheim an der Ruhr, Germany) |
| 11:15 | New Synthetic Routes of Nitrogen and Oxygen Heterocycles and Related Compounds |
Prof. Artur M.S. SILVA
(UNIVERSITY OF AVEIRO, Aveiro, Portugal) |
| 11:35 | Fast and Safe Synthesis of Pharmaceutically Relevant Molecules |
Prof. Thomas WIRTH
(UNIVERSITY OF CARDIFF, Cardiff, United Kingdom) |
| 11:55 | Metal Assisted Synthetic Approaches to Heterocyclic Small Molecules for the Treatment of Cardiovascular Diseases |
Prof. Marko D. MIHOVILOVIC
(VIENNA UNIVERSITY OF TECHNOLOGY, Vienna, Austria) |
|
|
| 12:15 | Exhibition & Lunch |
|
| 5.11 Oncology: Kinases and Beyond | 5.12 Recent Advances in Anti-infective Agents
(AFMC Session) | 5.13 New Strategies for Lead Generation |
| 13:15 | Session Chair |
Dr Mario VARASI
(EUROPEAN INSTITUTE OF ONCOLOGY, Milano, Italy) |
| 13:20 | Therapeutic Opportunities Offered by the Excessive Lactate Production in Cancer |
Prof. Filippo MINUTOLO
(UNIVERSITY OF PISA, Pisa, Italy) |
| 14:00 | Novel Anti-Cancer Treatment Targeting Vps34 |
Dr Jessica MARTINSSON
(SPRINT BIOSCIENCE, Stockholm, Sweden) |
| 14:20 | Exploiting Tumor Metabolic Vulnerabilities with Novel OxPhos Inhibitors |
Dr Maria Emilia DI FRANCESCO
(UTMD ANDERSON CANCER CENTER, Houston, United States) |
| 14:40 | Discovery and Characterization of A-366, a Novel, Potent and Highly Selective Inhibitor of Histone Methyltransferase G9a |
Dr Michael MICHAELIDES
(ABBVIE, North Chicago, United States) |
|
| 13:15 | Session Chair |
Dr Ming-Hua HSU
(NATIONAL TSING HUA UNIVERSITY, Hsinchu, Taiwan) |
| 13:20 | Development of New Anti-Infective Agents and a Novel Delivery Strategy |
Prof. Reuben JIH-RU HWU
(NATIONAL TSING HUA UNIVERSITY, Hsinchu, Taiwan) |
| 14:00 | Synthesis of Anti-infective Cyclic Natural Products and Natural Product-like Compounds |
Prof. Han-Young KANG
(CHUNGBUK NATIONAL UNIVERSITY, Cheongju, Korea, South) |
| 14:20 | Novel Boron-containing Anti-infective Agents |
Dr Jacob PLATTNER
(ANACOR PHARMACEUTICALS, Palo Alto, United States) |
| 14:40 | Lectins as Targets in Antiadhesion Therapy - Example of DC-SIGN And FimH Antagonists |
Prof. Marko ANDERLUH
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia) |
|
| 13:15 | Session Chair |
(THERMO FISHER SCIENTIFIC) |
| 13:20 | Integration of New Chemical Diversity and Design Approaches in Lead Generation |
Dr Timothy GRESE
(ELI LILLY AND COMPANY, Indianapolis, United States) |
| 14:00 | The Impact of Polypharmacology on Lead Generation |
Dr Jordi MESTRES
(IMIM AND UNIVERSITY POMPEU FABRA, Girona, Spain) |
| 14:20 | Starting Small, Thinking Big: The Application of Fragment Based Drug Discovery to Lead Generation |
Dr Steve WOODHEAD
(TAKEDA CALIFORNIA, San Diego, United States) |
| 14:40 | Discovery of the First and Only Small Molecule Il-17 Blockers |
Dr Nils HANSEN
(VIPERGEN, Copenhagen, Denmark) |
|
|
| 15:00 | Exhibition & Coffee |
|
| 15:30 | Medicinal Chemistry Experts in Pharma are Helping us to Generate Freely Available Novel Probes in Order to Facilitate Target Discovery |
Prof. Chas BOUNTRA
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
| 16:30 | Poster Session II and Networking |
|
| 18:30 | End of the day |
|
| Wednesday September 10, 2014 |
| 08:30 | IUPAC Richter Prize Lecture
Medicinal Chemistry, Quo Vadis? - The Changing Climate In R&D |
Dr Helmut BUSCHMANN
(PHARMA CONSULTING AACHEN, Aachen, Germany) |
| 09:15 | Innovation Through Chemistry at the Interfaces of the Scientific Disciplines |
Dr Martin MISSBACH
(NOVARTIS, Basel, Switzerland) |
| 10:00 | Exhibition & Coffee |
|
| 6.14 New Chemical Entities: Beyond Small Molecules | 6.15 Novel Agents for the Treatment of C. Difficile
(ACS Session II) | 6.16 Kinetic and Thermodynamic Aspects of Ligand Binding |
| 10:30 | Session Chair |
Prof. Stan VAN BOECKEL
(LEIDEN INSTITUTE OF CHEMISTRY, Leiden, The Netherlands) |
| 10:35 | Cyclic Peptides from the nature to the synthetic ones |
Prof. Fernando ALBERICIO
(INSTITUTE FOR RESEARCH IN BIOMEDICINE, Durban , South Africa) |
| 11:15 | Successful Drug Discovery And Development Case Studies Of Protein Epitope Mimetics |
Dr Daniel OBRECHT
(POLYPHOR, Allschwil, Switzerland) |
| 11:35 | Cell-Permeable Peptide Therapeutics to Effectively Access Intracellular Targets in Cancer Stem Cells |
Dr Jörg VOLLMER
(NEXIGEN, Cologne, Germany) |
| 11:55 | Novel Inhibitors of Alzheimer's Associated Beta-Secretase-Clusters of Heparan Sulfate |
Dr Olga ZUBKOVA
(VICTORIA UNIVERSITY OF WELLINGTON, Lower Hutt , New Zealand) |
|
| 10:30 | Session Chair |
Prof. Steven FIRESTINE
(WAYNE STATE UNIVERSITY, Detroit, United States) |
| 10:35 | Discovery and Development of Surotomycin for the Treatment of C. difficile |
Dr Jared SILVERMAN
(CUBIST PHARMACEUTICALS, Lexington, United States) |
| 11:15 | Invited Lecture |
Dr Terry BOWLIN
(MICROBIOTIX, Worcester, United States) |
| 11:35 | Targeting Spore Germination to Prevent Clostridium Difficile Infections |
Dr Ernesto ABEL-SANTOS
(UNIVERSITY OF NEVADA, LAS VEGAS, Nevada, Las Vegas, United States) |
| 11:55 | Cadazolid: A New Antibiotic in Development for the Treatment of Clostridium Difficile-Associated Diarrhea (CDAD) |
Dr Philippe PANCHAUD
(ACTELION PHARMACEUTICALS LTD, Allschwil, Switzerland) |
|
| 10:30 | Session Chair |
Prof. György KESERU
(HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary) |
| 10:35 | Exploring the Dynamics of Ligand-Protein Interactions using SPR Biosensors |
Prof. Helena DANIELSON
(UPPSALA UNIVERSITY, Uppsala, Sweden) |
| 11:15 | Breaking The Equilibrium Dissociation Constant Into Fragments: The Use Of Binding Kinetics And Thermodynamics In The Development Of Selective Ligands. |
Prof. Iwan DE ESCH
(VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands) |
| 11:35 | Medicinal Chemistry Optimisation Of Binding Kinetics |
Prof. Mike WARING
(ASTRAZENECA, Newcastle upon Tyne, United Kingdom) |
| 11:55 | CRTH2: Can Residence Time Help? |
Dr Elena GOMEZ
(ALMIRALL, BARCELONA, Spain) |
|
|
| 12:15 | Exhibition & Lunch |
|
| 7.17 Recent Highlights in Medicinal Chemistry | 7.18 Hot Topics in Ion Channels | 7.19 Allosteric Modulators for CNS Diseases |
| 13:15 | Session Chair |
Prof. Carlos MONTANARI
(UNIVERSITY OF SAO PAULO, Sao Paulo, Brazil) |
| 13:20 | Cebranopadol, a Novel, Potent Analgesic |
Dr Henning STEINHAGEN
(GRÜNENTHAL, Verona, Italy) |
| 13:40 | Discovery of BAY 1002670 - A Highly Potent and Selective Progesterone Receptor Modulator for Gynecological Therapies |
Dr Wolfgang SCHWEDE
(BAYER, Berlin, Germany) |
| 14:00 | Design, Synthesis and Biological Evaluation of Potent and Selective Class IIA Histone Deacetylase Inhibitors as a Potential Therapy for Huntington's Disease |
Dr Christopher LUCKHURST
(BIOFOCUS, Saffron Walden, United Kingdom) |
| 14:20 | Structure-Guided Design of Potent, Selective, Orally Bioavailable Tankyrase Inhibitors |
Dr Erin DIMAURO
(AMGEN, Cambridge, United States) |
| 14:40 | Novel Potent Inhibitors of the Histone Demethylase KDM1A |
Dr Paola VIANELLO
(EUROPEAN INSTITUTE OF ONCOLOGY, Milan, Italy) |
|
| 13:15 | Session Chair |
Prof. Brian COX
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Brighton, United Kingdom) |
| 13:20 | An Introduction To Ion Channels As Drug Targets |
Prof. Morten GRUNNET
(LUNDBECK, Valby, Denmark) |
| 14:00 | CNV1014802, a Novel Nav1.7 Selective State-Dependent Sodium Channel Blocker for the Treatment of Chronic Pain: From Discovery to Phase 2 Clinical Study |
Dr Gerard GIBLIN
(CONVERGENCE PHARMACEUTICALS, Cambridge, United Kingdom) |
| 14:20 | Pain-relieving Peptides Targeting Acid-Sensing Ion Channels |
Dr Eric LINGUEGLIA
(CNRS-UNIVERSITY OF NICE SOPHIA ANTIPOLIS, Valbonne, France) |
| 14:40 | Discovery of Ivacaftor (Vx-770), a Cftr Potentiator for the Treatment of Cystic Fibrosis in G551d Patients |
Dr Sabine HADIDA
(VERTEX PHARMACEUTICALS, San Diego, United States) |
|
| 13:15 | Session Chair |
Dr Wolfgang FROESTL
(AC IMMUNE, Lausanne, Switzerland) |
| 13:20 | Functional and Structural Insights into GPCR Allostery |
Prof. Arthur CHRISTOPOULOS
(MONASH UNIVERSITY, Parkville, Australia) |
| 14:00 | Discovery of the mGlu5 Negative Allosteric Modulator RO4917523 |
Dr Georg JAESCHKE
(F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
| 14:20 | Allosteric Protein Kinases Inhibitors for Neurodegenerative Diseases Therapies |
Prof. Ana MARTINEZ
(INSTITUTO DE QUIMICA MEDICA-CSIC, Madrid, Spain) |
| 14:40 | Antibodies as Tools to Enable Small Molecule Drug Discovery |
Dr Marta WESTWOOD
(UCB, Slough, United Kingdom) |
|
|
| 15:00 | Excursions |
|
| 20:00 | Banquet |
|
| Thursday September 11, 2014 |
| 8.20 GPCR Structural Biology: New Therapeutic Opportunities? | 8.21 Neglected Tropical Diseases: Shaping Future Trends | 8.22 New Therapies for Metabolic Disorders |
| 08:30 | Session Chair |
Prof. Jan STEYAERT
(VUB, Brussels, Belgium) |
| 08:35 | High End Design for GPCRs: Combining Protein Structure, Biophysical Data and Computational Water Network Energies |
Dr. Jonathan MASON
(HEPTARES THERAPEUTICS, Welwyn Garden City, United Kingdom) |
| 09:15 | Nanobody-Enabled Fragment Screening On Active-State Constrained GPCRs |
Prof. Jan STEYAERT
(VUB, Brussels, Belgium) |
| 09:35 | Covalent Agonists Facilitating Crystallisation of GPCRs |
Prof. Peter GMEINER
(FRIEDRICH ALEXANDER UNIVERSITY, Erlangen, Germany) |
| 09:55 | Crystallographic Structures Enable the Discovery of Selective 5-Ht1b Receptor Ligands through Virtual Screening |
Dr David RODRIGUEZ DIAZ
(STOCKHOLM UNIVERSITY, Solna, Sweden) |
|
| 08:30 | Session Chair |
Prof. Kelly CHIBALE
(UNIVERSITY OF CAPE TOWN, Cape Town, South Africa) |
| 08:35 | Update on Chemotherapy of Tropical Diseases Caused by Protozoan Parasites |
Prof. Reto BRUN
(SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE, Basel, Switzerland) |
| 09:15 | Antimalarial Trioxolanes - Exploiting Peroxide Reduction For Parasite-Selective Drug Delivery |
Dr Adam RENSLO
(UNIVERSITY OF CALIFORNIA, San Francisco, United States) |
| 09:35 | Antimalarial Lead Discovery from phenotypic screening: Unraveling the Black Box |
Dr Francisco-Javier GAMO
(GLAXOSMITHKLINE, Madrid, Spain) |
| 09:55 | Improving Physiochemical Properties of a Lapatinib-Based Lead Compound that Targets Trypanosoma Brucei |
Prof. Jennifer WOODRING
(NORTHEASTERN UNIVERSITY, Boston, United States) |
|
| 08:30 | Session Chair |
Dr Jürgen MACK
(BOEHRINGER INGELHEIM, Biberach an der Riss, Germany) |
| 08:35 | Pharmaceutical Protein & Peptide Engineering: From Once Daily To Once Weekly GLP-1 Dosing |
Dr Jesper LAU
(NOVO NORDISK, Maaloev, Denmark) |
| 09:15 | 1,1’-Spiro-Substituted Hexahydrofuroquinoline Derivatives As Potent And Polar Cholesteryl Ester Transfer Protein (CETP) Inhibitors |
Dr Thomas TRIESELMANN
(BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany) |
| 09:35 | Omarigliptin: A Once-weekly Oral Antidiabetic Agent |
Dr Tesfaye BIFTU
(MERCK, Rahway, United States) |
| 09:55 | Discovery of GPR103 Ligands Demonstrating the Anorexigenic Effect in vivo of GPR103 Antagonism |
Dr Anneli NORDQVIST
(ASTRAZENECA, BIOPHARMACEUTICALS R&D, Gothenburg, Sweden) |
|
|
| 10:15 | Exhibition & Coffee & Snacks |
|
| 9.23 Late Breaking News | 9.24 Neurodegeneration: Deeper Understanding of Disease Biology and Emerging Therapeutic Options | 9.25 Translational Medicine: Case Studies with Biomarkers and PKPD Modeling |
| 10:45 | Session Chair |
Dr Laurence LAFANECHERE
(CNRS, Grenoble, France) |
| 10:50 | CHF-6001, an Inhaled PDE4 Inhibitor for Asthma and COPD: Synthesis, In Vitro and In Vivo Characterization |
Dr Maurizio DELCANALE
(CHIESI, Parma, Italy) |
| 11:10 | The Discovery of AZD5069; a CXCR2 Antagonist In Phase II Clinical Trials for the Treatment of Asthma |
Dr Rhona COX
(ASTRAZENECA, Mölndal, Sweden) |
| 11:30 | Discovery of BAY 85-8501, a Novel and Highly Potent Induced-Fit Binder of Human Neutrophil Elastase for Pulmonary Diseases |
Dr Franz VON NUSSBAUM
(BAYER PHARMA, Berlin, Germany) |
| 11:50 | Discovery of TD-5959 (Batefenterol/GSK-961081): A
First-in-Class Dual Pharmacology Multivalent
Muscarinic Antagonist and Beta-2 Agonist (MABA) for
the Treatment of COPD |
Dr Adam HUGHES
(THERAVANCE INC., South San Francisco, United States) |
| 12:10 | Identifying Selective Inhibitors of FGFR4 Kinase |
Dr Kurt PIKE
(ASTRAZENECA, Cambridge, United Kingdom) |
|
| 10:45 | Session Chair |
Dr Andrew THOMAS
(F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland) |
| 10:50 | CaV1.3-Selective L-Type Calcium Channel Negative Allosteric Modulators. Novel Therapeutics to Slow the Progression of Parkinson’s Disease |
Prof. Rick SILVERMAN
(NORTHWESTERN UNIVERSITY, Evanston, United States) |
| 11:30 | Restoration of Muscle Mass and Lifespan in a Mouse Model of Spinal Muscular Atrophy by Molecular Correction of SMN2 Splicing Defect |
Dr Hasane RATNI
(F. HOFFMANN-LA ROCHE LTD, Basel , Switzerland) |
| 11:50 | Fragment-Based Discovery of BACE Inhibitors for Alzheimer’s Disease |
Dr Andrew STAMFORD
(MERCK RESEARCH LABORATORIES, Rahway, United States) |
| 12:10 | The Evolution of an in vivo Efficacious Bace1 Inhibitor |
Dr Daniel OEHLRICH
(JANSSEN RESEARCH AND DEVELOPMENT, Beerse, Belgium) |
|
| 10:45 | Session Chair |
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
| 10:50 | Translational Modeling in Support to Discovery and Early Development |
Dr Thierry LAVE
(F.HOFFMANN-LA ROCHE LTD, Basel, Switzerland) |
| 11:30 | Non-Clinical Characterization And Clinical Translation Of LY2811376 And LY2886721 |
Dr Dustin James MERGOTT
(ELI LILLY, Indianapolis, United States) |
| 11:50 | A HTS Assay Predicting Both Passive Intestinal Absorption and Affinity Constant Towards Human Serum Albumin in a Two End-Point Measurement |
Mr Alban BUJARD
(UNIVERSITY OF GENEVA, Geneva, Switzerland) |
| 12:10 | Biomarkers after Bacteriochlorin Based Photodynamic Therapy against Cancer |
Dr Martyna KRZYKAWSKA-SERDA
(FACULTY OF BIOCHEMISTRY, BIOPHYSICS AND BIOTECHNOLOGY, JAGIELLONIAN UNIVERSITY, Krakow, Poland) |
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| 12:30 | Closing Lecture
Personalised Medicinal Systems Chemistry |
Prof. Hans WESTERHOFF
(VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands) |
| 13:15 | Closing Remarks, Poster Prizes and Welcome to EFMC-ISMC 2016 |
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