| Sunday September 1, 2019 |
| 09:00 | Excursions - Tour 1 |
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| 14:00 | Excursions - Tour 2 |
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| 15:30 | Registration |
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| 17:30 | Opening |
Prof. Varinder K. AGGARWAL (UNIVERSITY OF BRISTOL, Bristol, United Kingdom)
Dr Spiros LIRAS (APPLE TREE PARTNERS, New York, United States)
Dr Yves P. AUBERSON (NOVARTIS & EFMC, Basel, Switzerland)
Dr Gene VAISBERG (CHEMBRIDGE CORPORATION, San Diego, United States)
Prof. Emmanuel MIKROS (UNIVERSITY OF ATHENS, Athens, Greece) |
| 18:00 | Opening Lecture
The Art and Science of Total Synthesis and its Impact on Biology and Medicine: From the Fundamentals to the Translational (T01) |
Prof. K.C. NICOLAOU
(RICE UNIVERSITY, Houston, United States) |
| 19:00 | Welcome Reception |
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| 20:00 | End of the Day |
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| Monday September 2, 2019 |
| 08:00 | Registration |
|
| Session Chair |
Prof. Varinder K. AGGARWAL
(UNIVERSITY OF BRISTOL, Bristol, United Kingdom) |
| 08:30 | Nature’s Medicine Chest: Opportunities for Synthesis and Drug Discovery (T02) |
Prof. Margaret Anne BRIMBLE
(THE UNIVERSITY OF AUCKLAND, Auckland, New Zealand) |
| 09:15 | Drug Discovery in Academia (T03) |
Prof. Oliver PLETTENBURG
(LEIBNIZ UNIVERSITY HANNOVER, Hannover, Germany) |
| 10:00 | Practical and Asymmetric Gilman-Speeter Synthesis of B-Lactams (OC01) |
Prof. Plato MAGRIOTIS
(UNIVERSITY OF PATRAS, Patras, Greece) |
| 10:15 | Coffee Break and Exhibition |
|
| 10:45 | Discovery of First in Class, Orally Bioavailable p300/CBP HAT Domain Inhibitors (T04) |
Dr Michael MICHAELIDES
(ABBVIE, North Chicago, United States) |
| 11:30 | Novel Bacterial Topoisomerase Inhibitors (NBTI) with Potent Gram-Negative Activity (T05) |
Dr Cornelia ZUMBRUNN
(IDORSIA PHARMACEUTICALS, Allschwil, Switzerland) |
| 12:15 | Rapid Exploration of Synthetically Tractable Chemical Space and Lead Optimization Using a Combination of Reaction-Based Enumeration, Active Learning, and Free Energy Calculations (OC02)
|
Dr Tatjana BRAUN
(SCHRÖDINGER, Mannheim, Germany) |
| 12:30 | Lunch and Exhibition |
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| 13:00 | Schrödinger Workshop: Using LiveDesign for Collaborative and Data Driven Drug Design |
|
| Session Chair |
Dr Malin LEMURELL
(ASTRAZENECA, Gothenburg, Sweden) |
| 14:00 | Catalytic Chirality Generation: New Strategies for Organic Synthesis (T06) |
Prof. John BOWER
(UNIVERSITY OF BRISTOL, Bristol, United Kingdom) |
| 14:45 | Nucleophilic Boron for the Synthesis of Functionalized Small Rings (T07) |
Prof. Mariola TORTOSA
(AUTONOMOUS UNIVERSITY OF MADRID, Madrid, Spain) |
| 15:30 | A Radical Approach for the Late-Stage Functionalization of Phosphinic Peptides (OC03) |
Mr Angelos LELIS
(UNIVERSITY OF ATHENS, Athens, Greece) |
| 15:45 | Coffee Break and Exhibition |
|
| 16:15 | EFMC Prize Winner EFMC-YMCS 2018
Development of Release-And-Report Kinase Inhibitors as Molecular Tools for Investigating Neurodegenerative Disorders (OC04) |
Dr Cassandra LEE FLEMING
(UNIVERSITY OF GOTHENBURG, Gothenburg, Sweden) |
| 16:30 | Photoinduced Assembly of C–N Bonds (T08) |
Prof. Daniele LEONORI
(UNIVERSITY OF MANCHESTER, Aachen, Germany) |
| 17:15 | Practical Heteroatom- and Group-Transfer Reactions (T09) |
Dr Laszlo KURTI
(RICE UNIVERSITY, Houston, United States) |
| 18:00 | Closing of the Day |
|
| Tuesday September 3, 2019 |
| Session Chair |
Prof. Emmanuel MIKROS
(UNIVERSITY OF ATHENS, Athens, Greece) |
| 08:30 | Design and Synthesis of Chemical Probes for Bromodomains (T10) |
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
| 09:15 | A Medicinal Chemist's Perspective on Solute Carriers: Avoiding or Targeting them (T11) |
Dr Kim HUARD
(GENENTECH, San Francisco, United States) |
| 10:00 | Stabilizing Inactive Conformations of MALT1 AS an Effective Strategy to Inhibit its Protease Activity (OC05) |
Dr Jean-Baptiste LANGLOIS
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
| 10:15 | Coffee Break and Exhibition |
|
| 10:45 | A Chemical Approach to Map Protein Interactions at the Cell Surface (T12) |
Dr Erik HETT
(MERCK EXPLORATORY SCIENCE CENTER, Boston, United States) |
| 11:30 | From Fragments to Antibody Drug Conjugates in Emerging Oncology Targeted Therapies (T13) |
Dr Laurent SCHIO
(SANOFI, Vitry sur Seine, France) |
| 12:15 | Macrocyclic Modalities for Modulation of Protein-Protein Interactions (OC06) |
Dr Stéphanie GUERET
(ASTRAZENECA MPI SATELLITE UNIT, Mölndal, Sweden) |
| 12:30 | Lunch and Exhibition |
|
| 13:30 | Poster Session 1 (odd numbers) |
|
| Session Chair |
Dr Gene VAISBERG
(CHEMBRIDGE CORPORATION, San Diego, United States) |
| 14:30 | Awareness of PAINS (Pan Assay Interference Compounds) can Accelerate the Drug Discovery Process (T14) |
Prof. Jonathan BAELL
(MONASH UNIVERSITY, Parkville, Australia) |
| 15:15 | Artificial Intelligence in ADMET Modeling and Compound Profiling (T15) |
Dr Karl-Heinz BARINGHAUS
(SANOFI, Frankfurt, Germany) |
| 16:00 | Antimicrobial Activity of Curcumin Analog PGV-6, HGV-6 and GVT-6 (OC07) |
Prof. Leni RITMALENI
(GADJAH MADA UNIVERSITY, Yogyakarta, Indonesia) |
| 16:15 | Coffee Break and Exhibition |
|
| 16:45 | Sustainable by Design Anti-Trypanosomatid Small Molecules: an Aspirational Goal for Medicinal Chemistry (T16) - ChemMedChem Lecture |
Prof. Maria Laura BOLOGNESI
(UNIVERSITY OF BOLOGNA, Bologna, Italy) |
| 17:30 | Artificial Intelligence in de Novo Molecular Design (T17) |
Dr Ola ENGKVIST
(ASTRAZENECA, Mölndal, Sweden) |
| 18:15 | Closing of the Day |
|
| Wednesday September 4, 2019 |
| Session Chair |
Dr Yves P. AUBERSON
(NOVARTIS & EFMC, Basel, Switzerland) |
| 08:30 | Amides and Chemical Education as Vehicles for Innovation (T18) |
Prof. Neil GARG
(UNIVERSITY OF CALIFORNIA, Los Angeles, United States) |
| 09:15 | Discovery of AZD5718, a Novel 5-lipoxygenase Activating Protein (FLAP) Inhibitor (T19) |
Dr Malin LEMURELL
(ASTRAZENECA, Gothenburg, Sweden) |
| 10:00 | Discovery of GSK701, a Novel Orally Effective Preclinical Drug Candidate for the Treatment of Malaria (OC08) |
Dr Jose Ignacio MARTIN
(GSK, Tres Cantos, Spain) |
| 10:15 | Coffee Break and Exhibition |
|
| 10:45 | Design and Implementation of de Novo Biosynthetic Cascades (T20) |
Prof. Sabine FLITSCH
(UNIVERSITY OF MANCHESTER, Manchester, United Kingdom) |
| 11:30 | Catalysis for Total Synthesis (T21) |
Prof. Alois FÜRSTNER
(MAX PLANCK INSTITUT FUR KOHLENFORSCHUNG, Muelheim an der Ruhr, Germany) |
| 12:15 | Developing a ‘Reverse-Biomimetic’ Synthesis of Arogenate and its Analogues (OC09) |
Ms Louise EAGLING
(UNIVERSITY OF BRISTOL, Bristol, United Kingdom) |
| 12:30 | Lunch and Exhibition |
|
| 13:30 | Poster Session 2 (even numbers) |
|
| Session Chair |
Prof. Christoforos KOKOTOS
(UNIVERSITY OF ATHENS , Athens, Greece) |
| 14:30 | Development and Application in Flow of Sustainable Synthetic Methodologies that Use Singlet Oxygen as Green Oxidant and Cascade Reaction Facilitator (T22)
|
Prof. Georgios VASSILIKOGIANNAKIS
(UNIVERSITY OF CRETE, Heraklion, Greece) |
| 15:15 | Prize Ceremony |
Dr Yves P. AUBERSON
(NOVARTIS & EFMC, Basel, Switzerland) |
| 15:20 | EFMC Prize for a Young Medicinal Chemist in Academia
From the Elucidation of the Mechanism of Vitamin E to the Design of Innovative Drugs that Limit Inflammation and Enhance Resolution (OC10) |
Dr Andreas KOEBERLE
(UNIVERSITY OF JENA, Jena, Germany) |
| 15:35 | EFMC Prize for a Young Medicinal Chemist in Industry
Cipargamin-Biocatalysis in the Discovery and Development of an Antimalarial Drug (OC11) |
Dr Radka SNAJDROVA
(NOVARTIS PHARMA AG, Basel, Switzerland) |
| 15:50 | Coffee Break and Exhibition |
|
| 16:20 | Flow Chemistry and Photochemistry as a Tool for Drug Discovery (T23) |
Dr Jesus ALCAZAR
(JANSSEN RESEARCH & DEVELOPMENT, Toledo, Spain) |
| 17:05 | Closing of the Day |
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| 20:00 | Symposium Banquet |
|
| Thursday September 5, 2019 |
| Session Chair |
Dr Spiros LIRAS
(APPLE TREE PARTNERS, New York, United States) |
| 08:30 | Start Selective and Rigidify: The Discovery Path Towards the Next Generation of EGFR Tyrosine Kinase Inhibitors (T24) |
Dr Harald ENGELHARDT
(BOEHRINGER-INGELHEIM, Vienna, Austria) |
| 09:15 | RNA Therapeutics: New Chemical Modalities Becoming a Therapeutic Reality (T25) |
Dr Konrad BLEICHER
(F.HOFFMANN-LA ROCHE LTD, Basel, Switzerland) |
| 10:00 | Removable Directing Groups for Late-Stage Functionalisation (OC12) |
Dr Miriam O'DUILL
(NATIONAL UNIVERSITY OF IRELAND, Galway, Ireland) |
| 10:15 | Coffee Break and Exhibition |
|
| 10:45 | TLR7/8 Antagonists: from Screening to in vivo Potency (T26) |
Dr Claudia BETSCHART
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
| 11:30 | Allosteric Activation of a Master Metabolic Regulator AMPK: Drug Discovery Opportunities and Challenges (T27) |
Dr Kimberly CAMERON
(PFIZER, Cambridge, United States) |
| 12:15 | Closing Remarks & Prize Ceremony |
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| 12:30 | End of the Symposium |
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