5. Molecular Therapies for Iinflammatory and Autoimmune Diseases: Ongoing Clinical Trials and Future Prospects
6. Virtual Screening and Profiling
13:45
Session Chair
Sheng DING (THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States)
13:50
Cardiovascular Derivatives of Human Pluripotent Stem Cells: Chemical Modulation and Use in Drug Discovery, Development, and Toxicology
Christine MUMMERY (LEIDEN UNIVERSITY MEDICAL CENTER, Leiden, The Netherlands)
14:30
Development of Small Molecule Therapeutics for Treating Endogenous Cells for Repair and Regeneration
Francine FAROUZ (FATE THERAPEUTICS, La Jolla, United States)
15:10
Phenotypic Screening using Human Neural Precursor Cells as a Translational in vitro Model to explore the Process of Neurogenesis
Ravi JAGASIA (HOFFMANN - LA ROCHE, Basel, Switzerland)
13:45
Session Chair
Sylviane MULLER (IBMC-CNRS, Strasbourg, France)
13:50
Molecular Therapies for Inflammatory and Autoimmune Diseases - Focus on Systemic Lupus Erythematosus
Sylviane MULLER (IBMC-CNRS, Strasbourg, France)
14:30
Generation and Development of a Series of MAPKAPK5 Inhibitors for the Treatment of Rheumatoid Arthritis
Martin ANDREWS (GALAPAGOS NV, Mechelen, Belgium)
14:50
Discovery And Optimization Of Highly Selective Btk Inhibitors That Bind To An Inactive Enzyme Conformation And Are Efficacious In Animal Models Of Arthritis And Lupus
Kevin CURRIE (CGI PHARMACEUTICALS, INC., Branford, United States)
15:10
Optimisation Of The Diaminopyrimidine Carboxamide Series Leading To Highly Potent, Selective And Orally Bioavailable Syk Inhibitors
Neil GARTON (GLAXOSMITHKLINE, Stevenage, United Kingdom)
13:45
Session Chair
Didier ROGNAN (UNIVERSITY OF STRASBOURG, Illkirch, France)
13:50
Virtual Screening - Success Stories and Challenges
Jürgen BAJORATH (UNIVERSITY OF BONN, Bonn, Germany)
14:30
Targeting the Dynamic Nature of Protein-Protein Interfaces
Alessandro PADOVA (SIENA BIOTECH, Siena, Italy)
14:50
Cinderella’s Shoe For Virtual Drug Discovery, Screening And Design
Vladimir POTEMKIN (CHELYABINSK STATE MEDICAL ACADEMY, Chelyabinsk, Russia)
15:10
Discovery Of New Antimalarial Leads Through A Virtual Screening Approach
Tiago RODRIGUES (IMED.UL. FACULTY PHARMACY, UNIVERSITY LISBON, Lisbon, Portugal)
15:30
Exhibition & Coffee
7. Targeting Pathways
8. Hot Topics in CNS Diseases
9. Toxicity Challenges in Drug Design and Structure-Toxicity Relationships
16:15
Session Chair
Nicholas COSFORD (BURNHAM INSTITUTE FOR MEDICAL RESEARCH, La Jolla, United States)
16:20
Discovery of Small Molecules for Myocardial Differentiation and Protection
Mark MERCOLA (BURNHAM INSTITUTE FOR MEDICAL RESEARCH, La Jolla, United States)
17:00
ASK-dependent Stress Signaling in Cell Death, Inflammation and Disease
Hidenori ICHIJO (UNIVERSITY OF TOKYO, Tokyo, Japan)
17:20
The Discovery of BKM120, a Pan Class I PI3 Kinase Inhibitor in Phase I/II Clinical Trials
Sabina PECCHI (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Emeryville, United States)
17:40
Phenotypic Drug Discovery at Lilly: Merging Images, Informatics and Chemistry to Enable SAR
Thomas ENGLER (ELI LILLY AND COMPANY, Indianapolis, United States)
16:15
Session Chair
Benoit KENDA (UCB, Braine-l'Alleud, Belgium)
16:20
Identification of a PDE9 Clinical Candidate for the Treatment of Alzheimer's Disease utilizing Prospective Design and Novel Protocol Development
Patrick Robert VERHOEST (PFIZER GLOBAL RESEARCH, Groton, United States)
17:00
Synthesis and Characterization of
1,3-Dihydro-benzo[b][1,4]diazepin-2-one Derivatives as potent
non-competitive metabotropic Glutamate Receptor 2/3 Antagonists
Thomas WOLTERING (F. HOFFMANN-LA ROCHE AG, Basel, Switzerland)
17:20
Discovery of Lu AE51090, an Allosteric Muscarinic M1 Agonist: Pro-cognitive Potential Alone and as Add-on to Antipsychotic Treatment
Anette GRAVEN SAMS (H. LUNDBECK, Valby, Denmark)
17:40
Identification of Functionally Selective Alpha2C-AR Agonists as Potential New Drugs for Treatment of Pain
Andreas BERNKOP-SCHNÜRCH (LEOPOLD-FRANZENS UNIVERSITY, Innsbruck, Austria)
13:45
Session Chair
Peter ETTMAYER (BOEHRINGER INGELHEIM, Vienna, Austria)
13:45
Discovery of Small Molecule Inhibitors of IGF-1R
Mark WITTMAN (BRISTOL-MYERS SQUIBB CO., Wallingford, United States)
14:20
Inhibitors of the MDM2-p53 Interaction
Lutz WEBER (NEXUSPHARMA, Langhorne, United States)
14:55
Discovery of a Potent and Selective SMO Inhibitor
Stefan PEUKERT (NOVARTIS, Cambridge MA, United States)
13:45
Session Chair
Gloria SERRA (UDELAR, Montevideo, Uruguay)
13:50
From Natural Products to Mitochondrial Targeting Agents
Peter WIPF (UNIVERSITY OF PITTSBURGH, Pittsburgh, United States)
14:30
Marine Natural Products as Drug Source
Mercedes ÁLVAREZ (SCIENTIFIC PARC OF BARCELONA, Barcelona, Spain)
15:10
Antibiotic Clusters
Pal HERCZEGH (UNIVERSITY OF DEBRECEN, Debrecen, Hungary)
15:30
Exhibition & Coffee
17. Imaging Biomarkers
18. Hot Topics in Anti-Infectives
19. Covalent Inhibitors in Drug Discovery
16:15
Session Chair
Gilles TAMAGNAN (INSTITUTE FOR NEURODEGENERATIVE DISORDERS AND MOLECULAR NEUROIMAGING, LLC, New Haven, United States)
16:15
PET Imaging in the Discovery of New Therapeutics
Terence HAMILL (MERCK RESEARCH LABORATORIES, West Point, United States)
16:50
The Next Generation of PET Cardiac Imaging Agents: Discovery of Flurpiridaz F 18 for Detection of Coronary Disease and LMI1195 for Sympathetic Neuronal Imaging
Simon ROBINSON (LANTHEUS MEDICAL IMAGING, North Billerica, United States)
17:25
PET Imaging for Oncology
Christer HALLDIN (KAROLINSKA INSTITUTET PET CENTRE, Stockholm, Sweden)
16:15
Session Chair
Lieven MEERPOEL (JOHNSON & JOHNSON PRD, Beerse, Belgium)
16:20
Advances in Bacterial Fatty Acid Synthesis Inhibitors for Use against Toxoplasma gondii and Bacillus anthracis
Alan KOZIKOWSKI (UNIVERSITY OF ILLINOIS, Chicago, United States)
17:00
Benzoxaboroles as Anti-Infective Agents
Stephen BAKER (ANACOR PHARMACEUTICALS, Palo Alto, United States)
17:20
Discovery of TMC-207, a Novel Antituberculosis Agent
Jérôme GUILLEMONT (TIBOTEC, Val de Reuil, France)
17:40
HDAC Inhibitors Able to Reduce Acquired Antifungal Resistance
Antonello MAI (UNIVERSITA DEGLI STUDI DI ROMA, Rome, Italy)
16:15
Session Chair
Tjeerd BARF (MERCK, Oss, The Netherlands)
16:20
Renaissance of Covalent Inhibitors
Tjeerd BARF (MERCK, Oss, The Netherlands)
17:00
Harnessing the Power of Reversible, Covalent Inhibitors: the Discovery of Odanacatib
Cameron BLACK (MERCK FROSST CENTRE FOR THERAPHEUTIC RESEARCH, Pointe-Claire-Dorval, Canada)
17:40
Targeting Drug Resistance in Protein Kinases with Irreversible Inhibitors
Daniel RAUH (CHEMICAL GENOMICS CENTRE OF THE MAX-PLANCK-SOCIETY, Dortmund, Germany)
20. Sunset Session:
Academic curricula and industrial careers More info
How to (re)organize academic curricula to guarantee to young medicinal chemists a successful start in an industrial environment?
Henk TIMMERMAN (VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands)
18:05
Klaus MÜLLER (F. HOFFMANN-LA ROCHE, Basel, Switzerland)
18:40
Gary TRESADERN (JOHNSON & JOHNSON PHARMACEUTICAL R&D, Toledo, Spain)
18:55
Anne VALADE (UCB, Braine-l'Alleud, Belgium)
08/09/2010
08:30
The UCB-EHRLICH AWARD for Excellence in Medicinal Chemistry Lecture New HIV Therapies: the Discovery of Maraviroc and Lersivirine
Anthony WOOD (PFIZER, Cambridge, United States)
Chair
Christophe GENICOT (UCB SA, Braine-l'Alleud, Belgium)
09:15
The PROUS INSTITUTE-OVERTON & MEYER Award for New Technologies in Drug Discovery Lecture (R)Evolutions in Drug Discovery through Conceptual and Technological Innovations
Klaus MÜLLER (F. HOFFMANN-LA ROCHE, Basel, Switzerland)
Chair
David PROUS (PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain)
10:00
Exhibition & Coffee
21. Process R&D and Scale-up: Chemistry, Crystals & More - Challenges and Success Stories
22. Emerging Drugs - Case Studies of Recently Disclosed New Medicines
23. The Challenges in Designing Multi-Targeted Ligands and Drugs - the Good, the Bad and the Ugly (ACS Session I)
10:30
Session Chair
Herbert STARK (SANOFI-AVENTIS, FRANKFURT/MAIN, Germany)
10:35
Scale-up of API Processes - Challenges of Solid State Properties: Case Studies
Roland THIEME (HOFFMANN-LA ROCHE, Basel, Switzerland)
11:15
Salt Selection for Scale up & Development: “The 100 mg –Approach”
Stefan BALBACH (SANOFI-AVENTIS, Frankfurt/Main, Germany)
11:55
Attrition Induced Grinding for the Synthesis of Some Commercial Drugs
Richard KELLOGG (SYNCOM B.V., Groningen, The Netherlands)
10:30
Session Chair
Nicholas CARRUTHERS (JOHNSON & JOHNSON R&D, San Diego, United States)
10:35
Dapagliflozin, a Novel SGLT2 Inhibitor
William WASHBURN (BMS, Princeton, United States)
11:15
A Novel CHK1 Inhibitor in Advanced Clinical Trials
Timothy GUZI (SCHERING-PLOUGH RESEARCH INSTITUTE, Cambridge, United States)
11:35
TMC 435, a Novel HCV Protease Inhibitor in Advanced Clinical Trials
Pierre RABOISSON (JANSSEN PHARMACEUTICAL COMPANIES, Beerse, Belgium)
11:55
Discovery of a Novel Orexin Receptor Antagonist for the Treatment of Sleep Disorders
Paul COLEMAN (MERCK RESEARCH LABORATORIES, West Point, United States)
10:30
Session Chair
John BUTERA
10:35
Multi-Targeted Drug Discovery: Strategies and Challenges for Medicinal Chemists
Richard MORPHY (MERCK, Lanarkshire, United Kingdom)
11:15
Serotonin/Noradrenaline Reuptake Inhibitors:A Case History in the Challenges of Multipharmacology Drug Discovery
Florian WAKENHUT (PFIZER CENTRAL RESEARCH, Kent, United Kingdom)
11:55
Design, synthesis and evaluation of a series of Biphenylsulfonamides as potent dual
Angiotensin II and Endothelin A receptor antagonists
William WASHBURN (BMS, Princeton, United States)
12:15
Poster Session 3 - Lunch
12:30
ELSEVIER WORKSHOP
REAXYS WORKSHOP: "GETTING TO KNOW REAXYS – ENHANCING YOUR CHEMISTRY RESEARCH"
15:00
Excursion
20:00
Gala Dinner
09/09/2010
24. G-Protein Coupled 7TM Receptors - New Insights into their Structure and Ligand Recognition
Hans BRAUNER-OSBORNE (THE DANISH UNIVERSITY OF PHARMACEUTICAL SCIENCES, Copenhagen, Denmark)
08:35
New G-Protein Coupled Receptor Crystal Structures: Insights and Limitations
Gebhard F.X. SCHERTLER (PAUL SCHERRER INSTITUTE, Villigen, Switzerland)
09:15
Activation Mechanism of class C GPCRs
Jean-Philippe PIN (CNRS / INSERM / UNIVERSITY OF MONTPELLIER, Montpellier, France)
09:55
Dualsteric Gpcr Targeting: A Novel Route To Subtype Selective Agonists And Antagonists Of The Muscarinic Receptors
Ulrike HOLZGRABE (UNIVERSITY OF WUERZBURG, Wuerzburg, Germany)
08:30
Session Chair
Eckhard OTTOW (BAYER HEALTHCARE, Berlin, Germany)
08:35
Structural Design and Optimization of Orally Available Renin Inhibitors
David CLAREMON (VITAE PHARMACEUTICAL, Fort Washington, United States)
09:00
BGG492, a Competitive AMPA/kainate Antagonist in Clinical Development for the Treatment of Migraine and Epilepsy
Yves P. AUBERSON (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
09:25
Discovery of a Potent, Selective and Orally Bioavailable Acidic 11betaHydroxysteroid Dehydrogenase Type 1 (11beta-HSD1) Inhibitor
Paul WHITTAMORE (ASTRAZENECA, Macclesfield, United Kingdom)
09:50
MK-1903: a Potent Niacin Receptor (GPR109a/ HCA2) Agonist
Douglas BOATMAN (ARENA PHARMACEUTICALS, San Diego, United States)
08:30
Session Chair
Javier FERNANDEZ (JANSSEN R&D, Toledo, Spain)
08:35
Protein-Protein Interactions and Apoptosis in Cancer Cells
John FLYGARE (GENENTECH, California, United States)
09:15
Small molecule inhibitors of the neuropilin-1 VEGF-A interaction
Ashley JARVIS (DOMAINEX LTD, Cambridge, United Kingdom)
09:55
Targeting Pdz Domains: From Computational Library Design, To Nmr And X-Ray, To In Vivo Studies
Dmytro KOVALSKYY (KIEV NATIONAL UNIVERSITY, KIEV, Ukraine)
10:15
Exhibition & Coffee
27. Finding the Right Binding Pockets: Allosteric Modulators of G-Protein Coupled Receptors for Non-CNS Diseases(ACS Session II)
28. Recent Case Studies in DD and Development
29. New Medicines Beyond Small Molecules - Novel Biologics
10:45
Session Chair
Robert A. FECIK (UNIVERSITY OF MINNESOTA, Minneapolis, United States)
10:50
The Discovery of Maraviroc, an Allosteric CCR5 Antagonist for HIV Infection
Patrick DORR (SURREY UNIVERSITY, Surrey, United Kingdom)
11:30
Allosteric, Small Molecule Agonists of the GLP-1 Receptor for Diabetes
Lotte KNUDSEN (NOVO-NORDISK, Bagsværd, Denmark)
12:10
Follicle Stimulating Hormone Receptor Negative Allosteric Modulators (Fshr Nam): Discovery And Development Of A New Series Of Orally Bioavailable Dimethoxy-Benzamides
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