2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry

 St. Anton, Austria    January 19-23, 2020

Programme


16:00

Registration

17:00

Opening Remarks

17:30

Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire (KL01)

Prof. Sarah E. REISMAN
CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States

18:30

Poster Session & Welcome Reception

20:30

End of Day 1

Session 1: Predictive ADME Sciences: Striking a Balance Between In Silico and Experimental Work?

Session Chair

Dr Amit KALGUTKAR
PFIZER, Groton, United States

08:30

Structural Attributes Influencing Unbound Tissue Distribution (PL01)

Dr Li DI
PFIZER, Groton, United States

09:00

Metabolism of Strained Rings: Tales of the Unexpected (PL02)

Dr Martin HAYES
ASTRAZENECA, Gothenburg, Sweden

09:30

Coffee Break

10:00

Leveraging 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

10:30

Predicting 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

11:00

Outdoor Networking Activities

15:45

Networking Break

16:00

NovAliX Workshop: DNA-Encoded Libraries, an Integrated Platform for Hit Finding and Beyond

Dr Julien MARIN
NOVALIX, Illkirch, France

Session 2: Frontiers of Synthetic Chemistry

Session Chair

Prof. Sarah E. REISMAN
CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States

17:00

Break-it-to-Make-it Strategies for Complex Molecule Synthesis (PL05)

Prof. Richmond SARPONG
UNIVERSITY OF CALIFORNIA, BERKELEY, Berkeley, United States

17:30

New Avenues in Synthesis Enabled by Organic Photoredox Catalysis (PL06)

Prof. David NICEWICZ
UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States

18:00

Coffee Break

18:30

Late-Stage Functionalizations (PL07)

Prof. Tobias RITTER
MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany

19:00

A Radical Way to Abeo-Steroids (PL08)

Prof. Philipp HERETSCH
FREE UNIVERSITY OF BERLIN, Berlin, Germany

19:30

Poster Session

20:30

End of Poster Session

21:00

Conference Dinner

23:00

End of Day 2

Session 3: Structure and Biophysics - Companions for Medicinal Chemistry

Session Chair

Dr Wolfgang JAHNKE
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland

08:30

Membrane Proteins at the SGC – Challenges and Success Stories (PL09)

Dr Katharina DUERR
UNIVERSITY OF OXFORD, Oxford, United Kingdom

09:00

The 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

09:30

Coffee Break

10:00

Discovery of ABL001, an Allosteric Inhibitor of BCR-ABL: Fragments, Biophysics, Structure and Chemistry (PL11)

Dr Wolfgang JAHNKE
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland

10:30

Discovery of Small Molecule Fascin 1 Inhibitors Using Fragment-Based Drug Discovery (OC01)

Dr Stuart FRANCIS
THE BEATSON INSTITUTE FOR CANCER RESEARCH, Glasgow, United Kingdom

11:00

Outdoor Networking Activities

15:00

Networking Break & "Beyond-the-Science Leadership Development" Workshop

Beyond-the-Science Leadership Development

Session Chair

Dr Michelle CLAFFEY
CLAFFEY LEADERSHIP, Norwich, United States

Session Chair

Session 4: Protein Degradation: New Rules for Drug Discovery

Session Chair

Prof. Alessio CIULLI
UNIVERSITY OF DUNDEE, Dundee, United Kingdom

17:00

Targeted Protein Degradation (PL12)

Prof. Andy PHILLIPS
C4 THERAPEUTICS, Watertown, United States

17:30

Chemical Genomics Approaches to Targeted Protein Degradation (PL13)

Dr Georg WINTER
RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria

18:00

Four E3 Ligases, One Target: Towards Novel CDK6 Protacs (OC02)

Mr Christian STEINEBACH
UNIVERSITY OF BONN, Bonn, Germany

18:30

Coffee Break

19:00

Expanding the Druggable Genome through Cereblon-Mediated Protein Degradation (KL02)

Dr Lawrence G. HAMANN
BRISTOL-MYERS SQUIBB, Cambridge, United States

20:00

End of Day 3

Session 5: Innovation and Inspiration from Natural Products

Session Chair

Prof. Thomas MAGAUER
UNIVERSITY OF INNSBRUCK, Innsbruck, Austria

08:30

Capturing Biological Activity in Natural Product Fragments: Success and Limitations (PL14)

Prof. Karl GADEMANN
UNIVERSITY OF ZÜRICH, Zürich, Switzerland

09:00

TBA (PL15)

Prof. Thomas MAGAUER
UNIVERSITY OF INNSBRUCK, Innsbruck, Austria

09:30

Coffee Break

10:00

Synthesis of Complex Antiplasmodial Isocyanoterpenes (PL16)

Prof. Christopher VANDERWAL
UNIVERSITY OF CALIFORNIA, IRVINE, Irvine, United States

10:30

Total Synthesis of Chivosazole F (OC03)

Dr Simon WILLIAMS
SYNGENTA, Stein AG, Switzerland

11:00

Outdoor Networking Activities

15:45

Networking 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

Session 6: Accelerating Drug Discovery by Intelligence Augmentation

Session Chair

Dr Thomas TRIESELMANN
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany

17:00

Organic Synthesis on a Computer: Should Medicinal Chemists Care? (PL17)

Prof. Bartosz A. GRZYBOWSKI
ULSAN NATIONAL INSTITUTE OF SCIENCE & TECHNOLOGY, Ulsan, Korea, South

17:30

Exploring an Interface of Synthesis and Data Science (PL18)

Prof. Timothy CERNAK
UNIVERSITY OF MICHIGAN, Ann Arbor, United States

18:00

Accelerating R&D with Augmented Intelligence (PL19)

Dr Matthias ZENTGRAF
BOEHRINGER INGELHEIM, Biberach an der Riss, Germany

18:30

Coffee 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

19:00

Using Small Molecules to Engineer and Explore Human Immunity (PL20)


Prof. David SPIEGEL
YALE UNIVERSITY, New Haven, United States

19:30

Poster Session

20:30

End of Day 4

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

08:30

Discovery 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

09:00

Intracellular and Tissue Specific Targeting of Therapeutic Modalities (PL22)

Dr Vadim DUDKIN
JANSSEN DISCOVERY SCIENCES, Lansdale, United States

09:30

Coffee Break

10:00

SBT6050, 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

10:30

Outdoor Networking Activities

15:45

Networking Break

Session 8: Drug Discovery Tales

Session Chair

Dr Lena RIPA
ASTRAZENECA, Sweden

16:00

Discovery 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

16:30

Investigating the Chameleonic Properties of RGD Integrin Antagonists for the Treatment of IPF (OC05)

Dr James THOMPSON
GLAXOSMITHKLINE/UNIVERSITY OF STRATHCLYDE, Stevenage, United Kingdom

17:00

Discovery 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

17:30

The 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

18:00

Coffee Break

18:30

The Big Impact of Small Changes : Towards Best-in-Class EZH2 and LSD1 Inhibitors (OC08)

Dr Julian LEVELL
CONSTELLATION PHARMACEUTICALS, Cambridge, United States

19:00

Controlling the Fate and Function of Proteins with Photopharmacology (KL03)

Prof. Dirk TRAUNER
NEW YORK UNIVERSITY, New York, United States

20:00

Closing Remarks

20:30

End of Symposium