ONLINE REGISTRATION is still OPEN!
|
| Sunday August 28, 2016 |
| 13:30 | Registration |
|
| 16:00 | Opening Ceremony |
Dr Phil JONES
(UNIVERSITY OF DUNDEE, Glasgow, United Kingdom) |
| 16:20 | Science, Art and Drug Discovery, a Personal Perspective |
Sir Simon CAMPBELL
(SCIENTIFIC CONSULTANT, Poole, United Kingdom) |
| Chair |
Dr Phil JONES
(UNIVERSITY OF DUNDEE, Glasgow, United Kingdom) |
| 17:05 | The European Research Council (ERC) and its Support for Medicinal Chemistry |
Prof. Klaus BOCK
(UNIVERSITY OF COPENHAGEN , Copenhagen, Denmark) |
| Chair |
Prof. Rebecca DEPREZ-POULAIN
(UNIVERSITY OF LILLE, Lille, France) |
| 17:30 | Award Ceremony |
Prof. Koen AUGUSTYNS
(UNIVERSITY OF ANTWERP, Antwerp, Belgium) |
| 17:50 | NAUTA AWARD FOR PHARMACOCHEMISTRY
Molecular Recognition Studies with Chemical and Biological Systems: A Multi-Dimensional Approach to Support Structure-Based Drug Design |
Prof. François DIEDERICH
(ETH ZURICH, Zürich, Switzerland) |
| Chair |
Prof. Henk TIMMERMAN
(VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands) |
| 18:40 | Late-Stage Fluorination |
Prof. Tobias RITTER
(MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany) |
| Chair |
Dr Anette GRAVEN SAMS
(H. LUNDBECK, Valby, Denmark) |
| 19:25 | Welcome Reception Sponsored by Concept Life Sciences |
|
| Monday August 29, 2016 |
| 08:30 | UCB-EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
Traversing the Valley of Death in Anticancer Drug Discovery |
Prof. Paul J. HERGENROTHER
(UNIVERSITY OF ILLINOIS, Urbana, United States) |
| Chair |
Dr Laurent PROVINS
(UCB, Braine-l'Alleud, Belgium) |
| 09:15 | Cross-Coupling Approaches to Saturated N-Heterocycles |
Prof. Jeffrey BODE
(ETH ZURICH, Zürich, Switzerland) |
| Chair |
Karin BRINER
(NOVARTIS, South San Francisco, United States) |
| 10:00 | Exhibition & Coffee |
|
| 1.1 Intramolecular Hydrogen Bonding and its Impact in Drug Design and Discovery (ACSMEDI Session) | 1.2 Drug Discovery Approaches Toward Targeting Ras | 1.3 New Antibacterials. An Update |
| 10:30 | Session Chairs |
Dr Amjad ALI (MERCK & CO. INC., Kenilworth, United States)
Dr Tanweer KHAN (MERCK, SHARP & DOHME, Kenilworth, United States) |
|
| 10:30 | Session Chair |
Dr Joachim RUDOLPH
(GENENTECH, South San Francisco, United States) |
|
| 10:30 | Session Chair |
Prof. Malcolm PAGE
(JACOBS UNIVERSITY, Bremen, Germany) |
|
| 10:35 | The Need of Implementing Intramolecular Hydrogen Bonding (IMHB) Considerations in Drug Discovery and How to do it |
Prof. Giulia CARON
(UNIVERSITY OF TORINO, Torino, Italy) |
|
| 10:35 | Studying Ciliary Trafficking and How it Leads to RAS Drug Candidates
|
Prof. Alfred WITTINGHOFER
(MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany) |
|
| 10:35 | New Antibacterial Agents in the Pipeline
|
Dr Eric DESARBRE
(BASILEA PHARMACEUTICA, Basel, Switzerland) |
|
| 11:15 | Intramolecular Hydrogen Bond Expectations in Medicinal Chemistry |
Dr Fabrizio GIORDANETTO
(D.E. SHAW RESEARCH LLC, New York, United States) |
|
| 11:15 | Chemical Biological Modulation of KRas-Signaling |
Prof. Herbert WALDMANN
(MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany) |
|
| 11:15 | Mechanistic and Inhibition Studies on Metallo-Beta-Lactamases |
Prof. Christopher J. SCHOFIELD
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
|
| 11:35 | Intramolecular Hydrogen Bonding as a Design Element in Medicinal Chemistry |
Dr Bernd KUHN
(F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
|
| 11:35 | Inhibition of Prenylated KRAS: Tools to Discover and Characterize RAS Ligands |
Dr Johanna JANSEN
(NOVARTIS, Emeryville, United States) |
|
| 11:35 | Enterobactin-Dependent Iron Uptake Pathway as a Gate for Antibiotic Trojan Horse Strategies Against Pseudomonas Aeruginosa
|
Dr Gaëtan MISLIN
(UNIVERSITY OF STRASBOURG, Illkirch-Graffenstaden, France) |
|
| 11:55 | Intramolecular Hydrogen Bonds in the Design of CREBBP Bromodomain Ligands |
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
|
| 11:55 | Small Molecule Binding Sites on the RAS: SOS Complex Can Be Exploited for Inhibition of RAS Activation |
Dr. Jon WINTER-HOLT
(ASTRAZENECA, Macclesfield, United Kingdom) |
|
| 11:55 | Exploring Hit-Identification Strategies for Energy-Coupling Factor Transporters, a Novel Target for the Development of Antibiotics |
Ms Leticia MONJAS GOMEZ
(UNIVERSITY OF GRONINGEN, Groningen, The Netherlands) |
|
|
| 12:15 | Exhibition & Lunch |
|
| 12:30 | Flash Poster Presentations (12:30-13:10) |
|
| Session Chair |
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
| 2.1 Peptides: Pushing Permeability and Bioavailability Beyond the Rule of 5 (ACSMEDI Session) | 2.2 Recent Progress in the Treatment of Ophthalmological Diseases | 2.3 Molecular Tissue Targeting |
| 13:15 | Session Chairs |
Dr Peter CHENG (BRISTOL-MYERS SQUIBB, Hopewell, United States)
Dr Claudio MAPELLI (BRISTOL-MYERS SQUIBB, United States) |
|
| 13:15 | Session Chair |
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
|
| 13:15 | Session Chair |
Dr Malin LEMURELL
(ASTRAZENECA, Gothenburg, Sweden) |
|
| 13:20 | Peptides and Peptidomimetics: Overcoming Problems of Activity, Selectivity and Bioavailability of Integrin Ligands |
Dr Horst KESSLER
(TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany) |
|
| 13:20 | Molecular Pharmacodynamics of Visual Cycle Modulators in Protection Against Retinal Degeneration
|
Prof. Krzysztof PALCZEWSKI
(CASE WESTERN RESERVE UNIVERSITY, Cleveland, United States) |
|
| 13:20 | Ligand-Targeted Therapeutic and Imaging Agents for Multiple Human Diseases |
Prof. Philip S. LOW
(PURDUE UNIVERSITY, West Lafayette, United States) |
|
| 14:00 | Discovery & Optimzation of Clips-Constrained Bicyclic Peptides (2clips) Using Pepscan Peptide Arrays |
Prof. Peter TIMMERMAN
(PEPSCAN THERAPEUTICS, Lelystad, The Netherlands) |
|
| 14:00 | The Back of The Eye: Treatment Challenges and Opportunities
|
Dr Muneto MOGI
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States) |
|
| 14:00 | Peptide Drugs to Target GPCR - State of the Art and Innovative Applications |
| |
|
| 14:20 | Phage-Encoded Combinatorial Chemical Libraries Based on Bicyclic Peptides |
Prof. Christian HEINIS
(ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE (EPFL), Lausanne, Switzerland) |
|
| 14:20 | Regorafenib Eye Drops for Wet AMD – Challenges in Translatability of Preclinical Data Into Clinical Efficacy
|
Dr Michael BÖTTGER
(BAYER PHARMA, Wuppertal, Germany) |
|
| 14:20 | The Development of Pyrrolobenzodiazepine in Antibody Drug Conjugates |
Dr Philip HOWARD
(SPIROGEN LTD, London, United Kingdom) |
|
| 14:40 | Attempts at Oral Delivery of a Series of Short Unnatural Peptides: Still Like Pushing a Camel Through the Eye of a Needle? |
Dr Claudio MAPELLI
(BRISTOL-MYERS SQUIBB, United States) |
|
| 14:40 | Systemic Administration of an Allosteric GSK-3 Inhibitor Delays Photoreceptor Cell Death and Preserves Visual Function in a Retinitis Pigmentosa Mouse Model |
Prof. Ana MARTINEZ
(CSIC, Madrid, Spain) |
|
| 14:40 | Photoisomerisable Allosteric Modulators Allow a Fine Control of mGlu Receptors with Light in Vivo (EFMC-YMCS Presentation Prize) |
Mr Xavier GÓMEZ-SANTACANA
(VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands) |
|
|
| 15:00 | Exhibition & Coffee |
|
| 3. First Time Disclosures
|
| 15:30 | Session Chair |
Dr David WITTY
(CONVERGENCE PHARMACEUTICALS, United Kingdom) |
|
| 15:35 | Discovery and Development of the Highly Potent, Highly Selective Cathepsin S Inhibitor RG7625 for the Treatment of Autoimmune Diseases
|
Dr Wolfgang HAAP
(F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
|
| 16:05 | First Time Disclosure of a Development Candidate to Treat Severe Acute Pancreatitis through a Drug Discovery Partnership Between GSK and the University of Edinburgh
|
Dr John LIDDLE
(GLAXOSMITHKLINE, Mölndal, Sweden) |
|
| 16:35 | Discovery of AZD3241 is a Potent and Selective Myeloperoxidase Inhibitor for the Treatment of Neurodegenerative Disorders
|
Dr Jörg HOLENZ
(ASTRAZENECA NEUROSCIENCE, Collegeville, United States) |
|
| 17:05 | Discovery of the HCV NS5A Inhibitor MK-8408 (RUZASVIR)
|
Dr Joe KOZLOWSKI
(MERCK, SHARP & DOHME, Rahway, United States) |
|
|
| 17:35 | Poster Session (even numbers) with drinks |
|
| 19:30 | End of the day |
|
| Tuesday August 30, 2016 |
| 08:30 | PROUS INSTITUTE-OVERTON AND MEYER AWARD
FOR NEW TECHNOLOGIES IN DRUG DISCOVERY
Nanobody-Enabled HTS for the Discovery of GPCR Agonists |
Prof. Jan STEYAERT
(VUB, Brussels, Belgium) |
| Chair |
Dr Josep Jr. PROUS
(PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain) |
| 09:15 | EFMC Prize Ceremony |
Prof. Rui MOREIRA
(UNIVERSITY OF LISBON, Lisbon, Portugal) |
| 09:20 | EFMC Prize for a Young Medicinal Chemist in Industry
Inhibition of the COP9 Signalosome as a Novel Approach to Treat Cancer”
|
Dr Jean QUANCARD
(NOVARTIS, Basel, Switzerland) |
| 09:40 | EFMC Prize for a Young Medicinal Chemist in Academia
Sigma Hole Bonding in Kinase Drug Discovery
|
Prof. Frank BÖCKLER
(EBERHARD-KARLS UNIVERSITY TUEBINGEN, Tübingen, Germany) |
| 10:00 | Exhibition & Coffee |
|
| 4.1 Making Small Molecule Synthesis Simpler, General, and Automatic | 4.2 Hot Topics in Cardiovascular Diseases Research | 4.3 Neglected Diseases |
| 10:30 | Session Chair |
Prof. Martin D. BURKE
(UNIVERSITY OF ILLINOIS, Urbana, United States) |
|
| 10:30 | Session Chair |
Dr Susanne ROEHRIG
(BAYER HEALTHCARE, Wuppertal, Germany) |
|
| 10:30 | Session Chair |
Dr Timothy MILES
(GSK, Madrid, Spain) |
|
| 10:35 | Towards a More Generalized and Automated Approach for Small Molecule Synthesis
|
Prof. Martin D. BURKE
(UNIVERSITY OF ILLINOIS, Urbana, United States) |
|
| 10:35 | Discovery of a First-in-Class PAR4 Antagonist as a Novel Antithrombotic
|
Dr Scott PRIESTLEY
(BRISTOL-MYERS SQUIBB, Hopewell, United States) |
|
| 10:35 | Utilization of Novel Benzoxaboroles as Drug Candidates to Treat Neglected Tropical Diseases |
Dr Robert T. JACOBS
(ANACOR PHARMACEUTICALS, California, United States) |
|
| 11:15 | Robot Scientists, the Replication Crisis, and Cancer |
Prof. Ross KING
(UNIVERSITY OF MANCHESTER, Manchester, United Kingdom) |
|
| 11:15 | Discovery of Novel LPA1 Antagonist: Design and SAR Studies
|
Dr Masahiko TERAKADO
(ONO PHARMACEUTICAL, Osaka, Japan) |
|
| 11:15 | The Development of DDD853651; a Potential Candidate for the Treatment of Visceral Leishmaniasis |
Dr Michael THOMAS
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom) |
|
| 11:35 | Identifying Synthetic Opportunities Using Chemplanner - How Computers Assist Chemists in Covering a Greater Synthetic Space |
Dr Orr RAVITZ
(WILEY, Chichester, United Kingdom) |
|
| 11:35 | Discovery of Clinical Candidate Ribuvaptan, a Dual Acting Vasopressin V1a/V2 Receptor Antagonist for the Treatment of Heart Failure
|
Dr Carsten SCHMECK
(BAYER, Wuppertal, Germany) |
|
| 11:35 | Pharmacological Reversion of Antibiotic Resistance in Mycobacterium Tuberculosis : Design of SMART Trojan Molecules to Reprogram The Bacteria |
Prof. Benoit DEPREZ
(INSTITUT PASTEUR OF LILLE, Lille, France) |
|
| 11:55 | The evoSpace - A Synthesis-Driven Environment that Finds Accessible, Well-Behaved Compounds by Design |
Dr Marcus GASTREICH
(BIOSOLVEIT, St. Augustin, Germany) |
|
| 11:55 | Classification of Adamts Binding Sites: the First Step Toward Selective ADAMTS7 Inhibitors |
Mrs Michaela MÜLLER
(UNIVERSITÄT ZU LÜBECK, Lübeck, Germany) |
|
| 11:55 | The Discovery and Development of Novel Macrofilaricidal Agents for the Treatment of Onchocerciasis and Lymphatic Filariasis |
Dr Thomas VON GELDERN
(ABBVIE, Chicago, United States) |
|
|
| 12:15 | Exhibition & Lunch |
|
| 12:15 | Advion Lunch Workshop: Compact Mass Spectrometry - The User's Perspective (12:15-13:45) |
|
| 12:30 | Flash Poster Presentations (12:30-13:10) |
|
| Session Chair |
Dr Sharan BAGAL
(ASTRAZENECA, Cambridge, United Kingdom) |
| 5.1 Synthesis Driven Innovation | 5.2 Modulation of Protein-Protein Interactions - Novel Opportunities for Drug Discovery
| 5.3 Current Advances and Future Opportunities for the Treatment of Neurodegenerative Disorders |
| 13:15 | Session Chair |
Dr Jesus EZQUERRA
(LABORATORIOS LILLY, Alcobendas, Spain) |
|
| 13:15 | Session Chair |
Dr Christian OTTMANN
(EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands) |
|
| 13:15 | Session Chair |
Dr Theodora CALOGEROPOULOU
(NATIONAL HELLENIC RESEARCH FOUNDATION, Athens, Greece) |
|
| 13:20 | Expanding the Macrocycle Chemical Space |
Prof. Alexander DÖMLING
(UNIVERSITY OF GRONINGEN, Groningen, The Netherlands) |
|
| 13:20 | Validating New Epigenetic Targets by Selective Protein Interaction Inhibitors of Bromodomains |
Prof. Stefan KNAPP
(GOETHE UNIVERSITY FRANKFURT, Frankfurt am Main, Germany) |
|
| 13:20 | Possibilities and Pitfalls: Disease Modifying Drugs for Alzheimer's Disease |
Dr Eric KARRAN
(FOUNDATIONAL NEUROSCIENCE CENTER, ABBVIE, Cambridge, United States) |
|
| 14:00 | Potent and Highly Selective Bromodomain Ligands… a Platform for Reaction Discovery
|
Prof. Cristina NEVADO
(UNIVERSITY OF ZURICH, Zurich, Switzerland) |
|
| 14:00 | Releasing the Brake on Apoptosis. Discovery of Bcl-2 Family Protein Inhibitors
|
Dr Steven ELMORE
(ABBVIE, North Chicago, United States) |
|
| 14:00 | Tackling Neurodegenerative Diseases Through Multi-Target and Theranostic Small Molecules
|
Prof. Maria Laura BOLOGNESI
(UNIVERSITY OF BOLOGNA, Bologna, Italy) |
|
| 14:20 | Nucleophilic Boron for the Preparation of Highly Functionalized Small Rings |
Prof. Mariola TORTOSA
(AUTONOMOUS UNIVERSITY OF MADRID, Madrid, Spain) |
|
| 14:20 | DNA-Encoded Chemical Library for Protein-Protein Interactions
|
Dr Jin LI
(HITGEN LTD , Chengdu, Sichuan, China) |
|
| 14:20 | Discovery of Brain-Penetrable LpPLA2 Inhibitor for Alzheimer’s Disease
|
Dr Xiaomin ZHANG
(GLAXOSMITHKLINE, Shanghai, China) |
|
| 14:40 | Rapid Composition of Tricyclic Spiranoid Lactones: Access to Natural Frames and Application in Selective Silencing of the Pain Receptor TRPV1 |
Prof. Dmitry TSVELIKHOVSKY
(THE HEBREW UNIVERSITY OF JERUSALEM, Jerusalem, Israel) |
|
| 14:40 | From Fragment to in vivo Activity for a Challenging PPI Target: the Discovery of Potent Inhibitors of the KEAP1-NRF2 Interaction
|
Dr David NORTON
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom) |
|
| 14:40 | Modulation of RS67,333: from a 5-HT4R Partial Agonist to the Identification of Several Promising Multi-Target Directed Ligands for Alzheimer's Disease |
Prof. Christophe ROCHAIS
(UNIVERSITY OF CAEN, Caen, France) |
|
|
| 15:00 | Exhibition & Coffee |
|
| 15:30 | Robotics, Artificial Intelligence, and Medicinal Chemistry: A Look Into the Future |
Dr Derek LOWE
(VERTEX PHARMACEUTICALS, Cambridge, United States) |
| Chair |
Dr Matthew TOZER
(CONSULTANT, Bognor Regis, United Kingdom) |
| 16:15 | Poster Session (odd numbers) with drinks |
|
| 18:15 | Close Poster Session |
|
| 19:00 | Public Lecture |
|
| 21:30 | End of the day |
|
| Wednesday August 31, 2016 |
| 08:30 | IUPAC-RICHTER PRIZE
The Discovery of Sofosbuvir: A Breakthrough Curative Therapy for Hepatitis C |
Dr Michael SOFIA
(ARBUTUS BIOPHARMA, Doylestown, United States) |
| Chair |
Dr Janos FISCHER
(RICHTER PLC, Budapest, Hungary) |
| 09:15 | DNA-Encoded Chemical Libraries |
Prof. Dario NERI
(ETH ZÜRICH, Zürich, Switzerland) |
| Chair |
| |
| 10:00 | Exhibition & Coffee |
|
| 6.1 Big Data in Medicinal Chemistry | 6.2 New Horizons in GPCR-targeted Medicinal Chemistry | 6.3 Novel Approaches to the Treatment of Cancer |
| 10:30 | Session Chair |
Prof. Andrew HOPKINS
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom) |
|
| 10:30 | Session Chair |
Prof. Christa MÜLLER
(UNIVERSITY OF BONN, Bonn, Germany) |
|
| 10:30 | Session Chair |
Dr Jonathan BENNETT
(MERCK, SHARP & DOHME, Boston, United States) |
|
| 10:35 | Big Dada in Medicinal Chemistry?
|
Prof. Gisbert SCHNEIDER
(ETH ZÜRICH, Zürich, Switzerland) |
|
| 10:35 | Identification of Allosteric Inhibitors of GPCRs Using SBDD
|
Dr Miles CONGREVE
(HEPTARES, Welwyn Garden City, United Kingdom) |
|
| 10:35 | Small Molecule Approaches to Immune-Modulation in Cancer |
Dr Ronan O'HAGAN
(MERCK, SHARP & DOHME, Boston, United States) |
|
| 11:15 | Exploiting Linked Open Data - Transporter Profiling and Beyond |
Prof. Gerhard ECKER
(UNIVERSITY OF VIENNA, Vienna, Austria) |
|
| 11:15 | Medicinal Chemistry of Purinergic Signalling:
Targets and Drugs for the Immunotherapy of Cancer
|
Prof. Christa MÜLLER
(UNIVERSITY OF BONN, Bonn, Germany) |
|
| 11:15 | The Identification of GSK2879552, a Mechanism Based Irreversible Inhibitor of the Histone Lysine Demethylase LSD1
|
Dr Neil W. JOHNSON
(GLAXOSMITHKLINE, Collegeville, United States) |
|
| 11:35 | Mining Structural Protein-Ligand Interactions to Navigate Medicinal Chemistry Space |
Dr Chris DE GRAAF
(VU UNIVERSITY AMSTERDAM, Cambridge, United Kingdom) |
|
| 11:35 | Targeting Long-Chain Fatty Acid Receptors FFA1 and FFA4 for Treatment of Metabolic Diseases |
Prof. Trond ULVEN
(UNIVERSITY OF SOUTHERN DENMARK, København Ø, Denmark) |
|
| 11:35 | Discovery of AG-120 – A First-in-class Inhibitor of IDH1 Mutant Enzymes for the Treatment of Cancers Harboring IDH1 Mutations |
Dr Janeta POPOVICI-MULLER
(AGIOS PHARMACEUTICALS, United States) |
|
| 11:55 | Non Coding RNA as a Small Molecule Druggable Target |
Dr Graham SMITH
(MERCK, SHARP & DOHME, Boston, United States) |
|
| 11:55 | Optimising Membrane Interactions to Achieve Duration of Action for Inhaled Drug Candidates |
Dr Mark HEALY
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States) |
|
| 11:55 | Targeting the Janus-Faced Nature of IDO1 in Immuno-Oncology |
Prof. Antonio MACCHIARULO
(UNIVERSITY OF PERUGIA, Perugia, Italy) |
|
|
| 12:15 | Exhibition & Lunch |
|
| 12:15 | Chemical Computing Group Lunch Workshop: Stucture-Based Drug Design and Ligand Modification (12:15-13:45) |
|
| 7.1 Emerging Topics
| 7.2 Innovation in Kinase Drug Discovery | 7.3 The Importance of Solute Carrier Transporters in Drug Discovery (MedChemComm Session) |
| 13:15 | Session Chair |
Prof. Antonello MAI
(SAPIENZA UNIVERSITY OF ROME, Rome, Italy) |
|
| 13:15 | Session Chair |
Dr Christel MENET
(CONFO THERAPEUTICS, Brussels, Belgium) |
|
| 13:15 | Session Chair |
Dr David HEPWORTH
(PFIZER MEDICINES DESIGN, Cambridge, United States) |
|
| 13:20 | Phenotypic Screening for the Discovery of Novel Molecules for Therapeutic Heart Regeneration |
Dr Alleyn T. PLOWRIGHT
(ASTRAZENECA, Cambridge, United Kingdom) |
|
| 13:20 | Broad Multiparametric Profiling of Kinase Inhibitors |
Dr Herman VAN VLIJMEN
(JANSSEN, Beerse, Belgium) |
|
| 13:20 | Solute Carriers, Metabolism and Drug Response: a Magic Triangle |
Prof. Giulio SUPERTI-FURGA
(RESEARCH CENTER FOR MOLECULAR MEDICINE (CEMM), Vienna, Austria) |
|
| 13:45 | How can Advances in Cryo-Electron Microscopy Revolutionize Medicinal Chemistry? |
Dr Neil RANSON
(UNIVERSITY OF LEEDS, Leeds, United Kingdom) |
|
| 14:00 | New Pseudokinase Drug Targets in the Human Kinome |
Prof. Patrick EYERS
(UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom) |
|
| 14:00 | The Design and Evaluation of URAT1 Inhibitors for the Treatment of Hyperuricemia and Gout |
Dr David HEPWORTH
(PFIZER MEDICINES DESIGN, Cambridge, United States) |
|
| 14:10 | Interaction of 4,5,6,7-Tetrahydrobenzo[1,2-D]Thiazoles with the Cellular Chaperone HSP90 as a Potential Pathway to Inhibit Hepatitis C Virus Replication |
Prof. Tihomir TOMASIC
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia) |
|
| 14:20 | Switch Control Inhibitors: an Advance in Type II Kinase Inhibition |
Dr Daniel FLYNN
(DECIPHERA PHARMACEUTICALS, Lawrence, United States) |
|
| 14:20 | The Cellular Uptake of Pharmaceutical Drugs is Transporter-Mediated - A Problem not of Biophysics but of Systems Biology |
Prof. Douglas KELL
(UNIVERSITY OF MANCHESTER, Manchester, United Kingdom) |
|
| 14:35 | RSC Prize Lecture:
Advanced Chemical Genetics for Epigenetics: Bump and Hole and PROTACs
(2016 MedChemComm Emerging Investigator Lectureship) |
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom) |
|
| 14:40 | First Disclosure of CDZ173 - Discovery of a New Generation of Potent and Selective PI3K Delta Inhibitors for Autoimmune and Inflammatory Diseases |
Dr Nicolas SOLDERMANN
(NOVARTIS, Basel, Switzerland) |
|
| 14:40 | Drug Targets in the Solute Carrier Classification (SLC) |
Dr Daniela DIGLES
(UNIVERSITY OF VIENNA, Vienna, Austria) |
|
|
| 15:00 | Excursions |
|
| 20:00 | Banquet |
|
| Thursday September 1, 2016 |
| 8.1 Covalent Drugs Revisited (AFMC Session)
| 8.2 Novel Molecular Probes for in Vivo Chemistry | 8.3 Recent Advances on Approaches to Treat Pain |
| 08:30 | Session Chair |
Prof. Zhengying PAN
(PEKING UNIVERSITY, Shenzhen, China) |
|
| 08:30 | Session Chair |
Dr Marc ROBILLARD
(TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands) |
|
| 08:30 | Session Chair |
Dr Alan BROWN
(STRATIFIED MEDICAL, Deal, United Kingdom) |
|
| 08:35 | Targeted Covalent Inhibitors of Bruton's Tyrosine Kinases - Design, Evaluation and Follow-up |
Prof. Zhengying PAN
(PEKING UNIVERSITY, Shenzhen, China) |
|
| 08:35 | Antibody Imaging and Therapy Using in Vivo Click and Click-to-Release Strategies |
Dr Marc ROBILLARD
(TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands) |
|
| 08:35 | The Painful Reality of Drug Discovery and Development
|
Dr Paul BESWICK
(UNIVERSITY OF SUSSEX, Brighton, United Kingdom) |
|
| 09:15 | Chemical Biology Efforts in Cancer Drug Discovery |
Prof. Huchen ZHOU
(SHANGHAI JIAO TONG UNIVERSITY, Shanghai, China) |
|
| 09:15 | Novel Antibody-Tetrazine Conjugate for Breast Cancer Imaging |
Mr Eduardo RUIVO
(UNIVERSITY OF ANTWERP, Antwerp, Belgium) |
|
| 09:15 | Challenges in the Discovery of Sigma-1 Receptor Antagonists for the Treatment of Pain
|
Dr Carmen ALMANSA
(ESTEVE, Barcelone, Spain) |
|
| 09:35 | Advances in the Development of Covalent EGFR Inhibitors: from Early Hits to Osimertinib
|
Dr Gail WRIGLEY
(ASTRAZENECA, Cambridge, United Kingdom) |
|
| 09:35 | Atypical Bile Acids as Chemical Probes for Diagnosis and Therapy Monitoring of Progressive Cholestatic Liver Disease in HSD3B7 Patients |
Prof. Antimo GIOIELLO
(UNIVERSITY OF PERUGIA, Perugia, Italy) |
|
| 09:35 | Functionally Irreversible Non-Covalent Inhibitors of FAAH: a Safer Approach? |
Dr Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States) |
|
| 09:55 | Rapid Discovery of Potent and Selective Covalent Inhibitors via Covalent Docking |
Dr Nir LONDON
(THE WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel) |
|
|
| 09:55 | Towards Low-Risk Painkillers: Human Dipeptidyl Peptidase III (hDPPIII) as a Novel Target for Therapeutic Pain Intervention |
Ms Shalinee JHA
(GRAZ UNIVERSITY OF TECHNOLOGY, Graz, Austria) |
|
|
| 10:15 | Exhibition & Coffee |
|
| 9.1 High Throughput Screening Strategies to Obtain High Quality Leads | 9.2 Late Breaking News | 9.3 Showcase Brazil |
| 10:45 | Session Chair |
Prof. Jonathan BAELL
(MONASH UNIVERSITY, Parkville, Australia) |
|
| 10:45 | Session Chair |
Dr Luc VAN HIJFTE
(SCT & NOVALIX, Nijmegen, The Netherlands) |
|
|
| 10:50 | Histone Acetyltransferase Inhibitors, from Screening to Optimization - a Tricky Track
|
Prof. Jonathan BAELL
(MONASH UNIVERSITY, Parkville, Australia) |
|
| 10:50 | Discovery of PF-06840003, a Novel IDO1 Inhibitor for Cancer Immunotherapy |
Dr Stefano CROSIGNANI
(ITEOS THERAPEUTICS SA, Gosselies, Belgium) |
|
| 10:50 | Molecular Design, Synthesis and Trypanocidal Activity of Dipeptidyl Nitriles as Cruzain Inhibitors |
Prof. Carlos MONTANARI
(UNIVERSITY OF SAO PAULO, Sao Paulo, Brazil) |
|
| 11:30 | Direct and Synergistic Inhibition of The HCV NS5A Protein |
Dr Makonen BELEMA
(BRISTOL-MYERS SQUIBB, Wallingford, United States) |
|
| 11:15 | Driving Tumors into Mitotic Catastrophe - Lead Generation of MPS1 Inhibitors Leading to Two Clinical Candidates BAY 1161909 and BAY 1217389 |
Dr Volker K. SCHULZE
(BAYER PHARMA AG, Berlin, Germany) |
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| 11:30 | Research, Development & Innovation at Aché Laboratórios Farmacêuticos
|
Dr Cristiano GUIMARAES
(ACHÉ PHARMACEUTICAL, Brazil) |
|
| 11:50 | Discovery of In Vivo Active and Selective Diacylglycerol Lipase-Alpha Inhibitors |
Dr Mario VAN DER STELT
(LEIDEN UNIVERSITY, Leiden, The Netherlands) |
|
| 11:40 | Delivering First-in-Class In Vitro Chemical Probes Against Poly (ADP Ribose) Glycohydrolase (PARG) |
Dr Allan JORDAN
(CANCER RESEARCH UK MANCHESTER INSTITUTE, Manchester, United Kingdom) |
|
| 11:50 | Effects of Novel Acylhydrazones Derived From 4-Quinolone on the Acetylcholinesterase Activity and Aβ42 Peptide Fibrils Formation |
Mrs Gisele SILVESTRE DA SILVA
(UNICAMP, São Paulo, Brazil) |
|
| 12:10 | Anti-Wolbachia (A·WOL) Drug Discovery: Novel Hit Finding Via Ligand Based Virtual Screening Combined With HTS |
Dr Neil G BERRY
(UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom) |
|
| 12:05 | Discovery of Ubrogepant (MK-1602): a Potent, Selective and Orally Bioavailable CGRP Receptor Antagonist for the Acute Treatment of Migraine |
Dr Mark FRALEY
(MERCK, SHARP & DOHME, West Point, United States) |
|
| 12:10 | Antiplatelet and Antithrombotic Activity of 1,2,5-Oxadiazole-2-N-Oxide Derivatives |
Mr Luiz Antonio DUTRA
(STATE UNIVERSITY OF SAO PAULO - UNESP, Araraquara, Brazil) |
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|
| 12:30 | Heterocycles and Medicinal Chemistry: The Importance of Innovative Synthesis
|
Dr Anthony WOOD
(PFIZER, Waltham, United States) |
| Chair |
Dr Franz VON NUSSBAUM
(BAYER PHARMA, Berlin, Germany) |
| 13:15 | Closing Remarks, Poster Prizes and Welcome to EFMC-ISMC 2018 |
Prof. Marko ANDERLUH
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia) |
|
.jpg "EFMC-ISMC 2016")
