3rd Alpine Winter Conference on Medicinal and Synthetic Chemistry
Keynote Speakers
Monday 24/01/2022
Methodologies to Understand Cellular Target Interaction
Session Chair
Prof. Per ARTURSSON
(UPPSALA UNIVERSITY, Uppsala, Sweden)
13:15Opening 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)
13:30IL01 - Intracellular Oligonucleotide Distribution and Protein Binding
Dr Alice GHIDINI
(ASTRAZENECA, Gothenburg, Sweden)
13:50IL02 - Monitoring Drug Selectivity and Target Engagement Across Systems – Thermal Shift Assay in Drug Discovery
Dr Anna RUTKOWSKA-KLUTE
(GSK, Heidelberg, Germany)
14:10Break
14:25IL03 - Molecular Chameleonicity and Cell Permeability of Drugs and PROTACs in the bRo5 Space
Prof. Jan KIHLBERG
(UPPSALA UNIVERSITY, Uppsala, Sweden)
14:45IL04 - Lessons in Transcellular Membrane Permeability Re-Learned
Dr Mike HANN
(GSK MEDICINES RESEARCH CENTRE, Stevenage, United Kingdom)
15:05Session Discussion
15:25End of Session
Networking & Exhibition
Targeting Unstructured Proteins
Session Chair
Dr Hasane RATNI
(F. HOFFMANN-LA ROCHE LTD, Basel , Switzerland)
15:55Introduction
16:00IL05 - Innovative Strategies to Target Non-Coding RNAs with Synthetic Ligands
Dr Maria DUCA
(UNIVERSITY OF CÔTE D'AZUR, Nice, France)
16:20IL06 - Targeting Transcription Factors for Treating Human Cancers and Auto Immune and Inflammatory Diseases
Dr Doriano FABBRO
(CELLESTIA BIOTECH AG, Basel , Switzerland)
16:40Break
16:55IL07 - Drugging RNA – A Structure-based Approach
Dr Jacques DUMAS
(ARRAKIS THERAPEUTICS, Boston, United States)
17:15IL08 - Design of Zotatifin (eFT226), a First-in-Class Inhibitor of the RNA Helicase eIF4A
Dr Christian NILEWSKI
(GENENTECH, South San Francisco, United States)
17:35KL01 - Attenuating Oncogenic Transcription with Small Molecules
 (SANOFI-AVENTIS DEUTSCHLAND GMBH)
Prof. Angela KOEHLER (MIT KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH, Cambridge, United States)
18:15Session Discussion
18:45End of the Day
Tuesday 25/01/2022
Poster Session I - Odd Numbers
Networking & Exhibition
Automation and Machine Learning Applications for Medicinal Chemistry
Session Chair
Dr Michael WLEKLINSKI
(MERCK & CO., INC., Kenilworth, United States)
13:15Introduction
13:20IL09 - Enabling Fragment-based Drug Discovery (FBDD) with Automated Synthesis Technologies
Dr Rachel GRAINGER
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom)
13:40IL10 - Rapid Development of Robust Reactions and Multi-Step Syntheses
Prof. Alexei LAPKIN
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
14:00Break
14:15IL11 - High-Throughput Experimentation Capabilities to Accelerate Discovery Chemistry
Dr Iulia STRAMBEANU
(JOHNSON AND JOHNSON, King of Prussia, United States)
14:35Session discussion
14:55End of Session
Networking & Exhibition
Increasing sp3 Fragment Options: Advances in the Synthesis of Small Ring Systems
Session Chair
Dr James MOUSSEAU
(HALDA THERAPEUTICS, New Haven, United States)
15:25Introduction
15:30IL12 - Exploring and exploiting propellanes
Prof. Ed ANDERSON
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
15:50IL13 - The Next Generation of BCPs: Exploring Substitutions on the Bridge
Dr Xiaoshen MA
(MERCK & CO., INC, Boston, United States)
16:10Break
16:25IL14 - Synthesis and Functionalization of Cyclopropane Derivatives
Dr Sophie ROUSSEAUX
(UNIVERSITY OF TORONTO, Toronto, Canada)
16:45IL15 - No Strain, No Gain: Advances in the Synthesis and Design of New Classes of Building Blocks
Prof. Kevin BROWN
(INDIANA UNIVERSITY, Bloomington, United States)
17:05Session Discussion
17:25End of the Day
Wednesday 26/01/2022
Understanding PK and PK/PD relationships in drug discovery - Target Mediated Drug Disposition
Session Chair
Dr Stephanie HARLFINGER
(ASTRAZENECA, Cambridge, United Kingdom)
13:15Introduction
13:20IL16 - General Introduction to TMDD
Dr David FAIRMAN
(GSK, Cambridge, United Kingdom)
13:40IL17 - 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)
14:00Break
14:15IL18 - Understanding the PKPD and ADME of PF-07059013: An Allosteric Modulator of a High Abundance Target
Dr Kevin BEAUMONT
(ASTRAZENECA, Cambridge, United Kingdom)
14:35IL19 - Importance of Mechanistic Models in AHD Prediction (IL)
Dr Birgit SCHOEBERL
(NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Cambridge, MA, United States)
14:55Session Discussion
15:15End of Session
Networking & Exhibition
Drug Discovery Tales (I)
Session Chair
Dr Nadia M. AHMAD
(CHARLES RIVER LABORATORIES, Harlow, United Kingdom)
15:45Introduction
15:50OC01 - Design and Synthesis of Novel RNA Binders for Therapeutic Applications
Ms Maurinne BONNET
(ICN, NICE, France)
16:10OC02 - Is Resistance Futile? Discovery of Clinical Candidate AZD3229, A Pan-Mutant C-KIT Inhibitor
Dr James SMITH
(ASTRAZENECA, Cambridge, United Kingdom)
16:30Break
16:45KL02 - Drug Discovery: Where are we Headed?
Dr Wendy YOUNG
(MPM CAPITAL, Brisbane, CA, United States)
17:25Session Discussion
17:45End of the Day
Thursday 27/01/2022
Poster Session II - Even Numbers
Networking & Exhibition
Drug Discovery Tales (II)
Session Chair
Dr Nadia M. AHMAD
(CHARLES RIVER LABORATORIES, Harlow, United Kingdom)
13:15Introduction
13:20OC03 - Discovery of a Selective ALK2 Kinase Inhibitor for the Treatment of a Rare Genetic Bone Disease
Dr Thomas ULLRICH
(NOVARTIS PHARMA AG, Basel, Switzerland)
13:40OC04 - 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)
14:00Break
14:15OC05 - Rational Design of Light-Controlled Bioactive Compounds for Photopharmacology
Mr Piermichele KOBAURI
(UNIVERSITY OF GRONINGEN FSSC, Groningen, The Netherlands)
14:35OC06 - Towards the Design of Cell Division Cycle 25 Phosphatases Inhibitors as Anticancer Agents
Dr Carmen CERCHIA
(UNIVERSITY OF NAPLES FEDERICO II, Naples, Italy)
14:55Session Discussion
15:15End of Session
Networking & Exhibition
Covalent Targeting: Innovating for the Future
Session Chair
Dr Vishal VERMA
(GENENTECH, INC., South San Francisco, United States)
15:45Introduction
15:50IL20 - Lysine-Targeting Covalent Inhibitors
Dr Matthew CHEESEMAN
(THE INSTITUTE OF CANCER RESEARCH, Sutton, United Kingdom)
16:10IL21 - Reversible-covalent Inhibitors of the Kinase Activity of FGFR4
Dr Robin FAIRHURST
(NOVARTIS, Basel, Switzerland)
16:30Break
16:45IL22 - Studies with Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors
Dr Agustin CASIMIRO-GARCIA
(PFIZER, United States)
17:05Session Discussion
17:25End of the Day
Friday 28/01/2022
The "Catalytic Cycle" of Complex Molecule Synthesis and Methodology Development
Session Chair
Prof. Tanja GAICH
(UNIVERSITY OF KONSTANZ, Konstanz, Germany)
13:00Introduction
13:05IL23 - Flow-based Methods for Chemical Peptide and Protein Synthesis".
Prof. Nina HARTRAMPF
(UNIVERSITY OF ZURICH, Zürich, Switzerland)
13:25IL24 - Prins Cyclization in Natural Product Synthesis
Prof. Ang LI
(SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, Shanghai, China)
13:45Break
14:00IL25 - Taming Multifaceted Nickel Catalysts: An Academic Fascination
Prof. Ruben MARTIN
(INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA, Tarragona, Spain)
14:20IL26 - Computationally Augmented Total Synthesis
Dr Timothy NEWHOUSE
(YALE UNIVERSITY, New Haven, United States)
14:40KL03 - Functionalization of N-Heterocycles using Li, Mg, and Zn Organometallics
Prof. Paul KNOCHEL
(LUDWIG MAXIMILIANS UNIVERSITY, Munich, Germany)
15:20Session Discussion
15:50Closing Ceremony
16:00End of Alpine Winter Conference 2022

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