4th Alpine Winter Conference on Medicinal and Synthetic Chemistry

 St. Anton, Austria    January 28-February 1, 2024

Programme



13:00

Registration

14:45

Opening Remarks

Dr Klemens HOEGENAUER
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
Dr Karl Heinz KRAWINKLER
NOVARTIS PHARMA AG DEVELOPMENT, Basel, Switzerland
Dr Antonia F. STEPAN
F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland

Recent Developments in Synthetic Methodologies and their Impact

Session Chair

Dr Fabrice GALLOU
NOVARTIS PHARMA, Basel, Switzerland
15:00

Organic Reactions in Aqueous Medium enabled by Surfactants (PL01)

Dr Niginia BORLINGHAUS
UNIVERSITY OF KONSTANZ, Konstanz, Germany
15:30

Reagents and Catalysts with Translational Potential (PL02)

Dr Josep CORNELLA COSTA
MAX PLANCK INSTITUTE FOR COAL RESEARCH, Mülheim an der Ruhr, Germany
16:00

Coffee Break

16:30

From Batch to Flow: Advancing Synthetic Organic Chemistry through Technological Innovation (PL03)

Prof. Timothy NOËL
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands
17:00

Chemo-Biocatalytic Processes Enabled by a Continuous Flow Set Up (PL04)

Prof. Francesca PARADISI
UNIVERSITY OF BERN, Bern, Switzerland
17:30

Break

17:45

New Catalytic Approaches for Simplifying Complex Molecule Synthesis (KL01)

Prof. Darren J. DIXON
UNIVERSITY OF OXFORD, Oxford, United Kingdom
18:45

Welcome Reception, Sponsored by abcr

20:15

End of the day

From Underground to Mainstream: Neglected and Novel, Emerging Functional Groups for Drug Discovery

Session Chair

Dr Ulrich LÜCKING
FORX THERAPEUTICS, Basel, Switzerland
08:30

Boron Based Heterocycles and their Application in Drug Discovery (PL05)

Prof. Bhaskar DAS
LONG ISLAND UNIVERSITY, Brooklyn, United States
09:00

“Magic Chloro”: Profound Effects of the Chlorine Atom in Drug Discovery (PL06)

Dr Yoshihiro ISHIHARA
VIVIDION THERAPEUTICS, San Diego, United States
09:30

Coffee Break

10:00

Deuterium in Drug Design: From Deuterium Switch to De Novo Drug Discovery (PL07)

Prof. Tracey PIRALI
UNIVERSITY OF PIEMONTE ORIENTALE, Novara, Italy
10:30

New Functional Groups for Synthetic and Discovery Chemistry (PL08)

Prof. Michael WILLIS
UNIVERSITY OF OXFORD, Oxford, United Kingdom
11:00

Outdoor Networking Activities

16:00

Networking Break

16:15

In Silico Prediction of Phase I and II Metabolism: Guiding Optimisation of Drug Metabolism o_BRCompany Workshop by Optibriumc_BR

Dr Matthew SEGALL
OPTIBRIUM LTD, Cambridge, United Kingdom

Latest Advances and Approaches in Bioconjugation Drug Discovery

Session Chair

Dr Karl Heinz KRAWINKLER
NOVARTIS PHARMA AG DEVELOPMENT, Basel, Switzerland
17:00

Bicyclic Peptides as a Novel Therapeutic Modality (PL09)

Dr Philip MURRAY
BICYCLE THERAPEUTICS, Cambridge, United Kingdom
17:30

Next-Generation Bioconjugates for Intra- and Extracellular Targeting (PL10)

Prof. Christian HACKENBERGER
FMP BERLIN, Berlin, Germany
18:00

Coffee Break

18:30

Creating Next-Generation Biotherapeutics Using Novel Chemistry Platform Technologies (PL11)

Dr Vijaya R. PATTABIRAMAN
BRIGHT PEAK THERAPEUTICS, Basel, Switzerland
19:00

Exploring the Versatility of Covalent and Supramolecular Bioconjugation in ADC and AOC (PL12)

Dr Alain WAGNER
CNRS/UNIVERSITY OF STRASBOURG, Illkirch, France
19:30

Poster Session 1 (odd numbers)

20:30

End of the Poster Session

Human Dose Prediction in the Discovery Space

Session Chair

Dr Holger FISCHER
F. HOFFMANN-LA ROCHE LTD., BASEL, Switzerland
08:30

Early Human Dose Predictions in Lead Optimization (PL13)

Dr Johan BYLUND
CTC CLINICAL TRIAL CONSULTANTS AB, Uppsala, Sweden
09:00

Early Human Dose Prediction & Machine Learning Models - Can We Impact Lead Selection? (PL14)

Dr Gregori GEREBTZOFF
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
09:30

Coffee Break

10:00

SwiftPK: Development and Implementation of a High Throughput PBPK/PD Framework to Inform Drug Selection in Early Drug Discovery (PL15)

Dr Andres OLIVARES
F. HOFFMANN-LA ROCHE, Basel, Switzerland
10:30

Predicting Human Exposure and Dose of Compounds Targeting the Brain (PL16)

Dr Nicola COLCLOUGH
ASTRAZENECA, Cambridge, United Kingdom
11:00

Outdoor Networking Activities

15:30

Networking Break

Antiviral Drug Discovery

Session Chair

Dr Dafydd OWEN
PFIZER, Cambridge, United States
16:30

Discovery, Chemistry, and Preclinical Development of Pritelivir, a Novel Option for Acyclovir-Resistant Herpes Simplex Virus Infections (PL17)

Dr Alexander BIRKMANN
AICURIS ANTI-INFECTIVE CURES AG, Wuppertal, Germany
17:00

Targeting Viral RNA Degradation Via Small Molecules As a Novel Antiviral Strategy to Achieve HBV Cure (PL18)

Dr Dimitar GOTCHEV
ARBUTUS BIOPHARMA, Doylestown, United States
17:30

Coffee Break

18:00

Direct-Acting Antivirals with a Targeted Protein Degradation Mechanism (PL19)

Prof. Priscilla YANG
STANFORD UNIVERSITY, Stanford, United States
18:30

Discovery of Obeldesivir; Oral Prodrug of Nucleoside GS-441524 That Exhibits Antiviral Efficacy in SARS-CoV-2-Infected African Green Monkeys (PL20)

Dr Rao KALLA
GILEAD SCIENCES, Foster City, United States
19:00

The Discovery of PAXLOVID (KL02)

Dr Dafydd OWEN
PFIZER, Cambridge, United States
20:00

End of the Scientific Programme

20:30

Conference Dinner

Radical Intermediates in Complex Molecule Synthesis

Session Chair

Prof. Nina HARTRAMPF
UNIVERSITY OF ZURICH, Zürich, Switzerland
08:30

Light-Mediated Nickel Catalysis Enabled by Donor-Acceptor Ligands (PL21)

Prof. Bart PIEBER
INSTITUTE OF SCIENCE AND TECHNOLOGY AUSTRIA (ISTA), Klosterneuburg, Austria
09:00

Recent Adventures in Catalysis and Beyond (PL22)

Prof. Bill MORANDI
ETH ZÜRICH, Zürich, Switzerland
09:30

Coffee Break

10:00

Alkenes as Flexible Platforms for Asymmetric Transformations (PL23)

Prof. Cristina NEVADO
UNIVERSITY OF ZURICH, Zurich, Switzerland
10:30

Attempts to Deliver on the Promise of Natural Product Synthesis (PL24)

Prof. Ryan SHENVI
SCRIPPS RESEARCH, La Jolla, United States
11:00

Outdoor Networking Activities

16:00

Networking Break

16:15

AI for Medicinal Chemists: Novel Compounds Design and Retrosynthesis Prediction o_BRCompany Workshop by Iktosc_BR

Dr Quentin PERRON
IKTOS, Paris, France

Drug Discovery Tales I

Session Chair

Dr Scott WOLKENBERG
JANSSEN PHARMACEUTICAL COMPANIES OF JOHNSON & JOHNSON, Spring House, United States
17:00

NLRP3 Inhibitors for Neurodegenerative Disorders (OC01)

Dr Oscar MAMMOLITI
JANSSEN RESEARCH & DEVELOPMENT, Beerse, Belgium
17:30

Discovery of a Bivalent Protein Kinase CK2 Inhibitor with Activity in Renal Cell Carcinoma (OC02)

Dr Isabelle KRIMM
CLB, Lyon, France
17:50

Coffee Break

18:20

Discovery of BI 7446: A Potent Cyclic Dinucleotide Sting Agonist with Broad-Spectrum Variant Activity for the Treatment of Cancer (OC03)

Dr Christian KUTTRUFF
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach, Germany
18:40

Discovery of [18F]RoSMA-18-D6 for PET Imaging of Cannabinoid Type 2 Receptors (OC04)

Dr Luca GOBBI
F. HOFFMANN-LA ROCHE, Basel, Switzerland
19:00

Selective Inhibition of Tead Transcription and Impact on the Up-Stream Effector Kinases of the Hippo Pathway to Halt Metastatic Colorectal Cancer Cell Growth (OC05)

Prof. Maria Paola COSTI
UNIVERSITY OF MODENA AND REGGIO EMILIA, Modena, Italy
19:20

Poster Session 2 (even numbers)

20:30

End of the Poster Session

Cryo-EM: Applications for Structure-Based Drug Discovery

Session Chair

Dr Katharina DÜRR
OMASS THERAPEUTICS, Oxford, United Kingdom
08:30

Deep Learning-Driven De Novo Drug Design Based on Gastric Proton Pump Structure (PL25)

Prof. Kazuhiro ABE
NAGOYA UNIVERSITY, Nagoya, Japan
09:00

Cryo-EM Enables Structure-Based Drug Design for Membrane Protein Targets at BI (PL26)

Dr Rebecca EBENHOCH
BOEHRINGER INGELHEIM, Biberach, Germany
09:30

Coffee Break

10:00

Single Particle CryoEM at 200 kV & Itchy GPRCs (PL27)

Prof. Jonathan F. FAY
UNIVERSITY OF NORTH CAROLINA CHAPEL HILL, Chapel Hill, United States
10:30

Examples from Structure-Based Drug Discovery Using Cryo-EM at MSD (PL28)

Dr Harini KRISHNAMURTHY
MERCK, SHARP & DOHME, Blue Bell, United States
11:00

Outdoor Networking Activities

16:00

Networking Break

Drug Discovery Tales II

Session Chair

Dr Scott WOLKENBERG
JANSSEN PHARMACEUTICAL COMPANIES OF JOHNSON & JOHNSON, Spring House, United States
17:00

Discovery of a Novel Oral NO- and Heme-Independent sGC Activator Runcaciguat (BAY 1101042) (OC06)

Dr Michael G. HAHN
BAYER AG PHARMACEUTICALS, Wuppertal, Germany
17:30

Heterocyclic Compounds as Delta-5 Desaturase Inhibitors (OC07)

Dr Ana MINATTI
AMGEN INC, Copenhagen, Denmark
18:00

Coffee Break

18:30

Novel Approaches to Molecular Glue Discovery: Design of Clinical Candidate NVP-DKY709 an IKZF2 Degrader by Re-Programming of CRBN Selectivity and Screening for Cooperativity Using DNA Encoded Libraries (OC8)

Dr Frédéric ZECRI
NOVARTIS, Cambridge, United States
19:00

Discovery of LY3154885, a Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Drug-Drug Interaction Risk Profile (OC09)

Dr Erik HEMBRE
ELI LILLY AND COMPANY, Indianapolis, United States
19:30

Site-Selective C—H Oxidations for Late-Stage Functionalizations (KL03)

Prof. M. Christina WHITE
UNIVERSITY OF ILLINOIS URBANA-CHAMPAIGN, Urbana, United States
20:30

Closing Remarks