Nauta Award for Pharmacochemistry Lecture Targeting IRS1/2 and Targeting the Immune System to Eradicate Metastatic Tumors as New Modalities of Cancer Therapy
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
Structure-Based Design of Novel Antibiotics for Treating Multidrug-resistant Bacterial Infections
Erin DUFFY (RIB-X PHARMACEUTICALS, New Haven, United States)
14:30
Strategies For The Design and Discovery of Compounds with Directed Against Challenging Targets of HIV-1 Life Cycle
Maria Jose CAMARASA (CSIC, Madrid, Spain)
14:50
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)
15:10
Endoperoxide-Vinyl Sulfone Hybrids as Dual Acting Antimalarials
Rudi OLIVEIRA (IMED.ULISBOA, Lisboa, Portugal)
15:30
Exhibition & Coffee
3.7 Chemical Biology Approaches in Drug Discovery
3.8 Fighting Cancer: Kinases and Beyond
3.9 Designing Better Drugs: Ligand Efficiency Guided Optimization in Drug Discovery (ACS Session II)
Session Chair
Craig CREWS (YALE UNIVERSITY, New Haven, United States)
16:20
Small Molecule Control of Intracellular Protein Levels
Craig CREWS (YALE UNIVERSITY, New Haven, United States)
17:00
Fragment-based Chemical Tools Targeting Proteases and Tyrosine Phosphatases Developed by Dynamic Ligation and Design
Robin GANELLIN (UNIVERSITY COLLEGE LONDON, London, United Kingdom)
10:00
Exhibition & Coffee
4.11 Strategies to Tackle Challenging Targets in Oncology
4.12 Recent Highlights in Medicinal Chemistry
4.13 New Opportunities in Lead Discovery
Session Chair
Martin MISSBACH (NOVARTIS, Basel, Switzerland)
10:35
Maximizing Efficacy: How to win the Quest for Highly Potent Drugs
Paul W. MANLEY (NOVARTIS PHARMA, Basel, Switzerland)
11:15
Kinase Inhibitors with Pre-engineered Binding Kinetic Signatures
Gerhard MÜLLER (MERCACHEM, Nijmegen, The Netherlands)
11:35
The Central Valine Concept revealed Indolyl-Imidazole Scaffold as p53-Hdm2 PPI Inhibitors
Keiichi MASUYA (NOVARTIS, Basel, Switzerland)
11:55
Total Synthesis of New Functionalized Epothilone Analogs for Prodrug Design and Tumor Targeting
Fabienne GAUGAZ (ETH ZÜRICH, Zürich, Switzerland)
Session Chair
Maria Luz LOPEZ-RODRIGUEZ (COMPLUTENSE UNIVERSITY OF MADRID, Madrid, Spain)
10:35
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)
11:00
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)
11:25
Potent and Selective Autotaxin (ATX) Inhibitors
Kai SCHIEMANN (MERCK KGAA, DARMSTADT, Germany)
11:50
Discovery of the Clinical Candidate TMC647055, a non Nucleoside Inhibitor of the Hepatitis C Virus NS5B Polymerase
Sandrine VENDEVILLE (TIBOTEC, Beerse, Belgium)
Session Chair
Gerhard KLEBE (PHILIPPS-UNIVERSITY MARBURG, Marburg, Germany)
10:35
Computer-assisted Lead Generation: Fact or Fiction
Karl-Heinz BARINGHAUS (SANOFI-AVENTIS, Frankfurt am Main, Germany)
11:15
Computational Approaches to Polypharmacology and Mode-of-Action Analysis
Andreas BENDER (UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
11:35
Experiences of Fragment-based Drug Discovery
Marcel VERDONK (ASTEX PHARMACEUTICALS, Cambridge, United Kingdom)
11:55
From Determinants of Binding to Modulators of Protein-Protein-Interactions
5.14 Epigenetics - An Area Offering Formidable Challenges and Opportunities for Medicinal Chemists
5.15 New Developments in CNS Drug Research
5.16 Targeting Protein-Protein Interactions
Session Chair
Dashyant DHANAK (JANSSEN PHARMACEUTICAL COMPANIES, United States)
13:50
Chemical Probes for Epigenetics
Mark BUNNAGE (PFIZER, Boston, United States)
14:30
From Chromatin Modulation to Drug Discovery : BET Bromodomain and EZH2 Inhibition
Jean-Christophe HARMANGE (CONSTELLATION PHARMACEUTICALS, Cambridge, United States)
14:50
Discovery of Chemical Probes for Histone Methyltransferases
Jian JIN (UNIVERSITY OF NORTH CAROLINA, Chapel Hill, United States)
15:10
Targeting Oncogenic microRNAs: Toward New Chemotherapies
Maria DUCA (UNIVERSITY OF NICE SOPHIA ANTIPOLIS, Nice, France)
Session Chair
Christopher O'DONNELL (PFIZER, New York, United States)
13:50
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)
14:30
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)
15:10
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)
Session Chair
Kristian STROMGAARD (UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
13:50
Fragment-based Discovery of Modulators for PPI and Allosteric Enzymes
Michelle R. ARKIN (UCSF, San Francisco, United States)
14:30
A Major Leap into the Chemical Space of Protein-Protein Interaction Inhibitors
Olivier SPERANDIO (INSERM, Paris, France)
15:10
Targeting Protein-Protein Interactions in the Brain
(EYEDPHARMA) Kristian STROMGAARD (UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
15:30
Exhibition & Coffee
6.17 What's New in GPCR Research?
6.18 Next Generation of Cardiovascular Drugs
6.19 Hot Trends in Process Chemistry
Session Chair
Ad P. IJZERMAN (UNIVERSITY OF LEIDEN, Leiden, The Netherlands)
16:20
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)
17:00
GPCR Structure Based Drug Design Using Stabilised Receptors (StaRs)
Giles BROWN (HEPTARES, Hertfordshire, United Kingdom)
17:20
Novel Paradigms for GPCR Allosteric Modulator Identification
Stephan SCHANN (DOMAIN THERAPEUTICS, Strasbourg, France)
17:40
Fragments, Fits, Fingerprints: Structure-Based Virtual Screening for Fragment-Like GPCR Ligands
Chris DE GRAAF (VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands)
Session Chair
Hanno WILD (BAYER HEALTHCARE, Wuppertal, Germany)
16:20
The Discovery and Development of Anacetrapib
Amjad ALI (MERCK, SHARP & DOHME, Rahway, United States)
17:00
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)
17:20
Selective Ion Channel Blockers for the Treatment of Atrial Fibrillation
David MADGE (XENTION, London, United Kingdom)
17:40
Tetrahydroquinoline Derivatives as Potent and Selective Factor XIA Inhibitors
Mimi QUAN (BMS, Pennington, United States)
Session Chair
Vittorio FARINA (JANSSEN R&D, Beerse, Belgium)
16:20
Transforming Pharmaceutical Manufacturing: Continuous - The Ultra Lean Way of Manufacturing
James EVANS (NOVARTIS/MIT CENTER FOR CONTINUOUS MANUFACTURING, Cambridge, United States)
17:00
Importance of Particle Size Control for Poorly Soluble Drugs
Thomas RAMMELOO (JANSSEN R&D, BEERSE, Belgium)
17:40
A Novel Asymmetric Propargylation Reaction and its Application to the Large Scale Synthesis of Drug Candidates
Nathan YEE (BOEHRINGER INGELHEIM PHARMACEUTICALS, Ridgefield, United States)
7.20 Sunset Session: Productivity vs. Development of Independent and Creative Thinking During the PhD Period
18:00
Chair
Silvia ORTEGA GUTIERREZ (UNIVERSIDAD COMPLUTENSE DE MADRID, Madrid, Spain)
Danijel KIKELJ (UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia)
Iwan DE ESCH (VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands)
Alessio LODOLA (UNIVERSITY OF PARMA, Parma, Italy)
Freya KLEPSCH (UNIVERSITY OF VIENNA, Vienna, Austria)
05/09/2012
08:30
Prize ceremony
08:45
EFMC Prize for a Young Medicinal Chemist in Industry Minimising CNS Side Effects: DMPK Considerations in the design of Drugs with Limited Brain Penetration
8.21 Predictive Tools, Virtual Screening and Cheminformatics
8.22 New Promising Developments
8.23 Drug Safety: What Toxic Effects can be Reasonably Predicted?
Session Chair
Andy DAVIS (ASTRAZENECA, Mölndal, Sweden)
10:35
Industrialization of QSAR Model Generation-a Paradigm Shift in Predictive Modeling ?
Andy DAVIS (ASTRAZENECA, Mölndal, Sweden)
11:15
Improved Prediction of in vivo Effects by Combining Cheminformatics and Short-term Assay Data
Alexander TROPSHA (UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States)
11:55
The Power of Molecular Matched-Pair Analysis in Drug Design: Case Study of Oxadiazoles
Alleyn T. PLOWRIGHT (ASTRAZENECA, Mölndal, Sweden)
Session Chair
Rui MOREIRA (UNIVERSITY OF LISBON, Lisbon, Portugal)
10:35
Anti-Adhesion Therapy for the Treatment of Infective Diseases
Beat ERNST (UNIVERSITY OF BASEL, Basel, Switzerland)
11:00
Disrupting the Amyloid Cascade- BACE 1 Inhibition for the Treatment of Alzheimer's Disease
Daniel LA (AMGEN, Cambridge, United States)
11:25
New Selective Androgen Receptor Modulators (SARM) for the Treatment of Cachexia
Pierre DEPREZ (GALAPAGOS, Romainville, France)
11:50
The Discovery and Early Clinical Development of CNV1014802: A Novel, NAV1.7 Selective, State-Dependent Sodium Channel Blocker for the Treatment of Neuropathic Pain
New Inhibitors of Cathepsin A for the Treatment of Cardiovasuclar Diseases
Sven RUF (SANOFI-AVENTIS, Frankfurt, Germany)
Session Chair
John MINERS (FLINDERS UNIVERSITY SCHOOL OF MEDICINE, Bedford Park, Australia)
08:35
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)
09:15
New Phase I Enzymes Involved in Drug Metabolism and Prodrug Activation
BERND CLEMENT (UNIVERSITY OF KIEL, Kiel, Germany)
09:55
Aldehyde Oxidase Metabolism - An Emerging but Surmountable Problem in Modern Drug Discovery
Peter JONES (PFIZER, Cambridge, United States)
10:15
Exhibition & Coffee
10.27 From Nano to Macro (EUCHEMS Session)
10.28 Late Breaking News
10.29 The Impact of Transporters in Drug Discovery and Oral Bioavailability Enhancement (EUFEPS Session)
Session Chair
Péter MÁTYUS (SEMMELWEIS UNIVERSITY, Budapest, Hungary)
10:50
Polymer-conjugates as Nano-sized Medicines
Maria VICENT (RESEARCH CENTRE PRÍNCIPE FELIPE, Valencia, Spain)
11:30
Nanomedicinal Chemistry and Nanotechnology
Maurizio PRATO (UNIVERSITY OF TRIESTE, Trieste, Italy)
12:10
Targeted, Polymer-Based Nanoparticles for Delivery of Camptothecin
Han HAN (CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States)
