3rd Alpine Winter Conference on Medicinal and Synthetic Chemistry

 Virtual Event    January 24-28, 2022

Programme



13:15

Start of sessions

Methodologies to Understand Cellular Target Interaction
Methodologies to Understand Cellular Target Interaction
Session Chair
Prof. Per ARTURSSON
UPPSALA UNIVERSITY, Uppsala, Sweden
13:15
Opening Ceremony
Dr Klemens HOEGENAUER
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
Dr Karl Heinz KRAWINKLER
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
Dr Antonia F. STEPAN
F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland
13:30
IL01 - Intracellular Oligonucleotide Distribution and Protein Binding
Dr Alice GHIDINI
ASTRAZENECA, Gothenburg, Sweden
13:50
IL02 - Monitoring Drug Selectivity and Target Engagement Across Systems – Thermal Shift Assay in Drug Discovery
Dr Anna RUTKOWSKA-KLUTE
GSK, Heidelberg, Germany
14:10
Break
14:25
IL03 - Molecular Chameleonicity and Cell Permeability of Drugs and PROTACs in the bRo5 Space
Prof. Jan KIHLBERG
UPPSALA UNIVERSITY, Uppsala, Sweden
14:45
IL04 - Lessons in Transcellular Membrane Permeability Re-Learned
Dr Mike HANN
GSK MEDICINES RESEARCH CENTRE, Stevenage, United Kingdom
15:05
Session Discussion
15:25
End of Session
15:25
Networking & Exhibition
Networking & Exhibition
15:55

Start of sessions

Targeting Unstructured Proteins
Targeting Unstructured Proteins
Session Chair
Dr Hasane RATNI
F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland
15:55
Introduction
16:00
IL05 - Innovative Strategies to Target Non-Coding RNAs with Synthetic Ligands
Dr Maria DUCA
UNIVERSITY OF CÔTE D'AZUR, Nice, France
16:20
IL06 - Targeting Transcription Factors for Treating Human Cancers and Auto Immune and Inflammatory Diseases
Dr Doriano FABBRO
CELLESTIA BIOTECH AG, Basel , Switzerland
16:40
Break
16:55
IL07 - Drugging RNA – A Structure-based Approach
Dr Jacques DUMAS
ARRAKIS THERAPEUTICS, Boston, United States
17:15
IL08 - Design of Zotatifin (eFT226), a First-in-Class Inhibitor of the RNA Helicase eIF4A
Dr Christian NILEWSKI
GENENTECH, South San Francisco, United States
17:35
KL01 - Attenuating Oncogenic Transcription with Small Molecules

Prof. Angela KOEHLER
MIT KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH, Cambridge, United States
18:15
Session Discussion
18:45
End of the Day
11:00
Poster Session I - Odd Numbers
Networking & Exhibition
Poster Session I - Odd Numbers
Networking & Exhibition
13:15

Start of sessions

Automation and Machine Learning Applications for Medicinal Chemistry
Automation and Machine Learning Applications for Medicinal Chemistry
Session Chair
Dr Michael WLEKLINSKI
MERCK & CO., INC., Kenilworth, United States
13:15
Introduction
13:20
IL09 - Enabling Fragment-based Drug Discovery (FBDD) with Automated Synthesis Technologies
Dr Rachel GRAINGER
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
13:40
IL10 - Rapid Development of Robust Reactions and Multi-Step Syntheses
Prof. Alexei LAPKIN
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
14:00
Break
14:15
IL11 - High-Throughput Experimentation Capabilities to Accelerate Discovery Chemistry
Dr Iulia STRAMBEANU
JOHNSON AND JOHNSON, King of Prussia, United States
14:35
Session discussion
14:55
End of Session
14:55
Networking & Exhibition
Networking & Exhibition
15:25

Start of sessions

Increasing sp3 Fragment Options: Advances in the Synthesis of Small Ring Systems
Increasing sp3 Fragment Options: Advances in the Synthesis of Small Ring Systems
Session Chair
Dr James MOUSSEAU
HALDA THERAPEUTICS, New Haven, United States
15:25
Introduction
15:30
IL12 - Exploring and exploiting propellanes
Prof. Ed ANDERSON
UNIVERSITY OF OXFORD, Oxford, United Kingdom
15:50
IL13 - The Next Generation of BCPs: Exploring Substitutions on the Bridge
Dr Xiaoshen MA
MERCK & CO., INC, Boston, United States
16:10
Break
16:25
IL14 - Synthesis and Functionalization of Cyclopropane Derivatives
Dr Sophie ROUSSEAUX
UNIVERSITY OF TORONTO, Toronto, Canada
16:45
IL15 - No Strain, No Gain: Advances in the Synthesis and Design of New Classes of Building Blocks
Prof. Kevin BROWN
INDIANA UNIVERSITY, Bloomington, United States
17:05
Session Discussion
17:25
End of the Day
13:15

Start of sessions

Understanding PK and PK/PD relationships in drug discovery - Target Mediated Drug Disposition
Understanding PK and PK/PD relationships in drug discovery - Target Mediated Drug Disposition
Session Chair
Dr Stephanie HARLFINGER
ASTRAZENECA, Cambridge, United Kingdom
13:15
Introduction
13:20
IL16 - General Introduction to TMDD
Dr David FAIRMAN
GSK, Cambridge, United Kingdom
13:40
IL17 - Concept of Pharmacologic Target-Mediated Drug Disposition (TMDD) in Large-Molecule and Small-Molecule Compounds
Prof. Guohua AN
THE UNIVERSITY OF IOWA COLLEGE OF PHARMACY, Iowa City, United States
14:00
Break
14:15
IL18 - Understanding the PKPD and ADME of PF-07059013: An Allosteric Modulator of a High Abundance Target
Dr Kevin BEAUMONT
ASTRAZENECA, Cambridge, United Kingdom
14:35
IL19 - Importance of Mechanistic Models in AHD Prediction (IL)
Dr Birgit SCHOEBERL
NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Cambridge, MA, United States
14:55
Session Discussion
15:15
End of Session
15:15
Networking & Exhibition
Networking & Exhibition
15:45

Start of sessions

Drug Discovery Tales (I)
Drug Discovery Tales (I)
Session Chair
Dr Nadia M. AHMAD
CHARLES RIVER LABORATORIES, Harlow, United Kingdom
15:45
Introduction
15:50
OC01 - Design and Synthesis of Novel RNA Binders for Therapeutic Applications
Ms Maurinne BONNET
ICN, NICE, France
16:10
OC02 - Is Resistance Futile? Discovery of Clinical Candidate AZD3229, A Pan-Mutant C-KIT Inhibitor
Dr James SMITH
ASTRAZENECA, Cambridge, United Kingdom
16:30
Break
16:45
KL02 - Drug Discovery: Where are we Headed?
Dr Wendy YOUNG
MPM CAPITAL, Brisbane, CA, United States
17:25
Session Discussion
17:45
End of the Day
11:00
Poster Session II - Even Numbers
Networking & Exhibition
Poster Session II - Even Numbers
Networking & Exhibition
13:15

Start of sessions

Drug Discovery Tales (II)
Drug Discovery Tales (II)
Session Chair
Dr Nadia M. AHMAD
CHARLES RIVER LABORATORIES, Harlow, United Kingdom
13:15
Introduction
13:20
OC03 - Discovery of a Selective ALK2 Kinase Inhibitor for the Treatment of a Rare Genetic Bone Disease
Dr Thomas ULLRICH
NOVARTIS PHARMA AG, Basel, Switzerland
13:40
OC04 - Dissociative Inhibitors of Thymidylate Synthase Homodimer Accelerate its Proteasomal Degradation and Inhibit Cancer Growth in Vivo
Prof. Maria Paola COSTI
UNIVERSITY OF MODENA AND REGGIO EMILIA, Modena, Italy
14:00
Break
14:15
OC05 - Rational Design of Light-Controlled Bioactive Compounds for Photopharmacology
Mr Piermichele KOBAURI
UNIVERSITY OF GRONINGEN FSSC, Groningen, The Netherlands
14:35
OC06 - Towards the Design of Cell Division Cycle 25 Phosphatases Inhibitors as Anticancer Agents
Dr Carmen CERCHIA
UNIVERSITY OF NAPLES FEDERICO II, Naples, Italy
14:55
Session Discussion
15:15
End of Session
15:15
Networking & Exhibition
Networking & Exhibition
15:45

Start of sessions

Covalent Targeting: Innovating for the Future
Covalent Targeting: Innovating for the Future
Session Chair
Dr Vishal VERMA
GENENTECH, INC., South San Francisco, United States
15:45
Introduction
15:50
IL20 - Lysine-Targeting Covalent Inhibitors
Dr Matthew CHEESEMAN
THE INSTITUTE OF CANCER RESEARCH, Sutton, United Kingdom
16:10
IL21 - Reversible-covalent Inhibitors of the Kinase Activity of FGFR4
Dr Robin FAIRHURST
NOVARTIS, Basel, Switzerland
16:30
Break
16:45
IL22 - Studies with Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors
Dr Agustin CASIMIRO-GARCIA
PFIZER, United States
17:05
Session Discussion
17:25
End of the Day
13:00

Start of sessions

The "Catalytic Cycle" of Complex Molecule Synthesis and Methodology Development
The "Catalytic Cycle" of Complex Molecule Synthesis and Methodology Development
Session Chair
Prof. Tanja GAICH
UNIVERSITY OF KONSTANZ, Konstanz, Germany
13:00
Introduction
13:05
IL23 - Flow-based Methods for Chemical Peptide and Protein Synthesis".
Prof. Nina HARTRAMPF
UNIVERSITY OF ZURICH, Zürich, Switzerland
13:25
IL24 - Prins Cyclization in Natural Product Synthesis
Prof. Ang LI
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, Shanghai, China
13:45
Break
14:00
IL25 - Taming Multifaceted Nickel Catalysts: An Academic Fascination
Prof. Ruben MARTIN
INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA, Tarragona, Spain
14:20
IL26 - Computationally Augmented Total Synthesis
Dr Timothy NEWHOUSE
YALE UNIVERSITY, New Haven, United States
14:40
KL03 - Functionalization of N-Heterocycles using Li, Mg, and Zn Organometallics
Prof. Paul KNOCHEL
LUDWIG MAXIMILIANS UNIVERSITY, Munich, Germany
15:20
Session Discussion
15:50
Closing Ceremony
16:00
End of Alpine Winter Conference 2022