2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry
Sunday January 19, 2020
16:00Registration
17:00Opening Remarks
17:30Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire (KL01)
Prof. Sarah E. REISMAN
(CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States)
18:30Poster Session & Welcome Reception
20:30End of Day 1
Monday January 20, 2020
08:30Session 1: Predictive ADME Sciences: Striking a Balance Between In Silico and Experimental Work?
Session Chair
Dr Amit KALGUTKAR
(PFIZER, Groton, United States)
08:30Structural Attributes Influencing Unbound Tissue Distribution (PL01)
Dr Li DI
(PFIZER, Groton, United States)
09:00Metabolism of Strained Rings: Tales of the Unexpected (PL02)
Dr Martin HAYES
(ASTRAZENECA, Gothenburg, Sweden)
09:30Coffee Break
10:00Leveraging In Silico ADMET Profiles and Ancillary Pharmacology to Influence Prioritization of Hit Series with Higher Probability of Success (PL03)
Dr Falgun SHAH
(MERCK & CO., West Point, United States)
10:30Predicting ADME - Reality, Vision or Fantasy? (PL04)
Dr Simone SCHADT
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
Dr Kenichi UMEHARA
(ROCHE PHARMACEUTICAL RESEARCH AND EARLY DEVELOPMENT, Basel, Switzerland)
11:00Outdoor Networking Activities
15:45Networking Break
16:00NovAliX Workshop: DNA-Encoded Libraries, an Integrated Platform for Hit Finding and Beyond
Dr Julien MARIN
(NOVALIX, Illkirch, France)
17:00Session 2: Frontiers of Synthetic Chemistry
Session Chair
Prof. Sarah E. REISMAN
(CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States)
17:00Break-it-to-Make-it Strategies for Complex Molecule Synthesis (PL05)
Prof. Richmond SARPONG
(UNIVERSITY OF CALIFORNIA, BERKELEY, Berkeley, United States)
17:30New Avenues in Synthesis Enabled by Organic Photoredox Catalysis (PL06)
Prof. David NICEWICZ
(UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States)
18:00Coffee Break
18:30Late-Stage Functionalizations (PL07)
Prof. Tobias RITTER
(MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany)
19:00A Radical Way to Abeo-Steroids (PL08)
Prof. Philipp HERETSCH
(FREE UNIVERSITY OF BERLIN, Berlin, Germany)
19:30Poster Session
20:30End of Poster Session
21:00Conference Dinner
23:00End of Day 2
Tuesday January 21, 2020
08:30Session 3: Structure and Biophysics - Companions for Medicinal Chemistry
Session Chair
Dr Wolfgang JAHNKE
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
08:30Membrane Proteins at the SGC – Challenges and Success Stories (PL09)
Dr Katharina DUERR
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
09:00The Mechanism of Outer Membrane Protein Insertion by BamA and its Role as a Target for Novel Antibiotic (PL10)
Prof. Sebastian HILLER
(UNIVERSITY OF BASEL, Basel, Switzerland)
09:30Coffee Break
10:00Discovery of ABL001, an Allosteric Inhibitor of BCR-ABL: Fragments, Biophysics, Structure and Chemistry (PL11)
Dr Wolfgang JAHNKE
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
10:30Discovery of Small Molecule Fascin 1 Inhibitors Using Fragment-Based Drug Discovery (OC01)
Dr Stuart FRANCIS
(THE BEATSON INSTITUTE FOR CANCER RESEARCH, Glasgow, United Kingdom)
11:00Outdoor Networking Activities
15:00Networking Break & "Beyond-the-Science Leadership Development" Workshop
15:00Beyond-the-Science Leadership Development
Session Chair
Dr Michelle CLAFFEY
(CLAFFEY LEADERSHIP, Norwich, United States)
Session Chair
17:00Session 4: Protein Degradation: New Rules for Drug Discovery
Session Chair
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
17:00Targeted Protein Degradation (PL12)
Prof. Andy PHILLIPS
(C4 THERAPEUTICS, Watertown, United States)
17:30Chemical Genomics Approaches to Targeted Protein Degradation (PL13)
Dr Georg WINTER
(RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria)
18:00Four E3 Ligases, One Target: Towards Novel CDK6 Protacs (OC02)
Mr Christian STEINEBACH
(UNIVERSITY OF BONN, Bonn, Germany)
18:30Coffee Break
19:00Expanding the Druggable Genome through Cereblon-Mediated Protein Degradation (KL02)
Dr Lawrence G. HAMANN
(BRISTOL-MYERS SQUIBB, Cambridge, United States)
20:00End of Day 3
Wednesday January 22, 2020
08:30Session 5: Innovation and Inspiration from Natural Products
Session Chair
Prof. Thomas MAGAUER
(UNIVERSITY OF INNSBRUCK, Innsbruck, Austria)
08:30Capturing Biological Activity in Natural Product Fragments: Success and Limitations (PL14)
Prof. Karl GADEMANN
(UNIVERSITY OF ZÜRICH, Zürich, Switzerland)
09:00(De)Construction of Three-Dimensional Molecular Architectures (PL15)
Prof. Thomas MAGAUER
(UNIVERSITY OF INNSBRUCK, Innsbruck, Austria)
09:30Coffee Break
10:00Synthesis of Complex Antiplasmodial Isocyanoterpenes (PL16)
Prof. Christopher VANDERWAL
(UNIVERSITY OF CALIFORNIA, IRVINE, Irvine, United States)
10:30Total Synthesis of Chivosazole F (OC03)
Dr Simon WILLIAMS
(SYNGENTA, Stein AG, Switzerland)
11:00Outdoor Networking Activities
15:45Networking Break & "Panel Discussion on Protein Degradation"
Panel Discussion on Protein Degradation
Session Chair
Dr Klemens HOEGENAUER
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
Prof. Andy PHILLIPS
(C4 THERAPEUTICS, Watertown, United States)
Mr Christian STEINEBACH
(UNIVERSITY OF BONN, Bonn, Germany)
Dr Georg WINTER
(RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria)
17:00Session 6: Accelerating Drug Discovery by Intelligence Augmentation
Session Chair
Dr Thomas TRIESELMANN
(BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany)
17:00Organic Synthesis on a Computer: Should Medicinal Chemists Care? (PL17)
Prof. Bartosz A. GRZYBOWSKI
(ULSAN NATIONAL INSTITUTE OF SCIENCE & TECHNOLOGY, Ulsan, Korea, South)
17:30Exploring an Interface of Synthesis and Data Science (PL18)
Prof. Timothy CERNAK
(UNIVERSITY OF MICHIGAN, Ann Arbor, United States)
18:00Accelerating R&D with Augmented Intelligence (PL19)
Dr Matthias ZENTGRAF
(BOEHRINGER INGELHEIM, Biberach an der Riss, Germany)
18:30Coffee Break
Session 7: Targeted Delivery - Strategies to Help your Drug Substances get to the Right Place
Session Chair
Dr Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States)
19:00Using Small Molecules to Engineer and Explore Human Immunity (PL20)
 (BIOIBÉRICA)
Prof. David SPIEGEL (YALE UNIVERSITY, New Haven, United States)
19:30Poster Session
20:30End of Day 4
Thursday January 23, 2020
08:30Session 7: Targeted Delivery - Strategies to Help your Drug Substances get to the Right Place
Session Chair
Dr Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States)
08:30Discovery of Tumor-Targeted TLR7/8 Immune-Stimulating Antibody Conjugates (ISAC): A New Class of Immuno-Oncology Therapeutics (PL21)
Dr Brian SAFINA
(BOLT BIOTHERAPEUTICS, Redwood City, United States)
09:00Intracellular and Tissue Specific Targeting of Therapeutic Modalities (PL22)
Dr Vadim DUDKIN
(JANSSEN DISCOVERY SCIENCES, Lansdale, United States)
09:30Coffee Break
10:00SBT6050, a HER2-Directed TLR8 Immunotac™ Therapeutic, is a Potent Human Myeloid Cell Agonist with Tumor-Localized Activity (PL23)
Dr Valerie ODEGARD
(SILVERBACK THERAPEUTICS, Seattle, United States)
10:30Outdoor Networking Activities
15:45Networking Break
Session 8: Drug Discovery Tales
Session Chair
Dr Lena RIPA
(ASTRAZENECA, Sweden)
16:00Discovery of GDC-0334: a potent and orally bioavailable clinical candidate for the inhibition of TRPA1 (OC04)
Dr Vishal VERMA
(GENENTECH, South San Francisco, United States)
16:30Investigating the Chameleonic Properties of RGD Integrin Antagonists for the Treatment of IPF (OC05)
Dr James THOMPSON
(GLAXOSMITHKLINE/UNIVERSITY OF STRATHCLYDE, Stevenage, United Kingdom)
17:00Discovery of AZD3458 a Highly Selective PI3Ky Inhibitor: Combining Structure, HDX-MS and Binding Kinetics to Understand the Mode of Action (OC06)
Dr Nils PEMBERTON
(ASTRAZENECA, Mölndal, Sweden)
17:30The Discovery of a Potent and Orally Bioavailable Macrocyclic Cyclophilin Inhibitor Based on The Structural Simplification of Sanglifehrin A (OC07)
Dr Vicky STEADMAN
(EUROFINS DISCOVERY, Essex, United Kingdom)
18:00Coffee Break
18:30The Big Impact of Small Changes : Towards Best-in-Class EZH2 and LSD1 Inhibitors (OC08)
Dr Julian LEVELL
(CONSTELLATION PHARMACEUTICALS, Cambridge, United States)
19:00Controlling the Fate and Function of Proteins with Photopharmacology (KL03)
Prof. Dirk TRAUNER
(NEW YORK UNIVERSITY, New York, United States)
20:00Closing Remarks
20:30End of Symposium

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