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| Keynote Speakers |
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| Monday January 24, 2022 |
| Methodologies to Understand Cellular Target Interaction |
| Session Chair |
Prof. Per ARTURSSON
(UPPSALA UNIVERSITY, Uppsala, Sweden) |
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| 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) |
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| 13:30 | IL01 - Intracellular Oligonucleotide Distribution and Protein Binding |
Dr Alice GHIDINI
(ASTRAZENECA, Gothenburg, Sweden) |
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| 13:50 | IL02 - Monitoring Drug Selectivity and Target Engagement Across Systems – Thermal Shift Assay in Drug Discovery |
Dr Anna RUTKOWSKA-KLUTE
(GSK, Heidelberg, Germany) |
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| 14:25 | IL03 - Molecular Chameleonicity and Cell Permeability of Drugs and PROTACs in the bRo5 Space |
Prof. Jan KIHLBERG
(UPPSALA UNIVERSITY, Uppsala, Sweden) |
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| 14:45 | IL04 - Lessons in Transcellular Membrane Permeability Re-Learned |
Dr Mike HANN
(GSK MEDICINES RESEARCH CENTRE, Stevenage, United Kingdom) |
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| Targeting Unstructured Proteins |
| Session Chair |
Dr Hasane RATNI
(F. HOFFMANN-LA ROCHE LTD, Basel , Switzerland) |
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| 16:00 | IL05 - Innovative Strategies to Target Non-Coding RNAs with Synthetic Ligands |
Dr Maria DUCA
(UNIVERSITY OF CÔTE D'AZUR, Nice, France) |
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| 16:20 | IL06 - Targeting Transcription Factors for Treating Human Cancers and Auto Immune and Inflammatory Diseases |
Dr Doriano FABBRO
(CELLESTIA BIOTECH AG, arlesheim, Switzerland) |
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| 16:55 | IL07 - Drugging RNA – A Structure-based Approach |
Dr Jacques DUMAS
(ARRAKIS THERAPEUTICS, Boston, United States) |
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| 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) |
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| 17:35 | KL01 - Attenuating Oncogenic Transcription with Small Molecules |
(SANOFI-AVENTIS DEUTSCHLAND GMBH)
Prof. Angela KOEHLER (MIT KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH, Cambridge, United States) |
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| Tuesday January 25, 2022 |
Poster Session I - Odd Numbers
Networking & Exhibition |
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| Automation and Machine Learning Applications for Medicinal Chemistry |
| Session Chair
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Dr Michael WLEKLINSKI
(MERCK & CO., INC., Kenilworth, United States) |
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| 13:20 | IL09 - Enabling Fragment-based Drug Discovery (FBDD) with Automated Synthesis Technologies |
Dr Rachel GRAINGER
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom) |
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| 13:40 | IL10 - Rapid Development of Robust Reactions and Multi-Step Syntheses |
Prof. Alexei LAPKIN
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom) |
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| 14:15 | IL11 - High-Throughput Experimentation Capabilities to Accelerate Discovery Chemistry |
Dr Iulia STRAMBEANU
(JOHNSON AND JOHNSON, King of Prussia, United States) |
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| Increasing sp3 Fragment Options: Advances in the Synthesis of Small Ring Systems |
| Session Chair |
Dr James MOUSSEAU
(HALDA THERAPEUTICS, New Haven, United States) |
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| 15:30 | IL12 - Exploring and exploiting propellanes |
Prof. Ed ANDERSON
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
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| 15:50 | IL13 - The Next Generation of BCPs: Exploring Substitutions on the Bridge |
Dr Xiaoshen MA
(MERCK & CO., INC, Boston, United States) |
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| 16:25 | IL14 - Synthesis and Functionalization of Cyclopropane Derivatives |
Dr Sophie ROUSSEAUX
(UNIVERSITY OF TORONTO, Toronto, Canada) |
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| 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) |
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| Wednesday January 26, 2022 |
| Understanding PK and PK/PD relationships in drug discovery - Target Mediated Drug Disposition |
| Session Chair |
Dr Stephanie HARLFINGER
(ASTRAZENECA, Cambridge, United Kingdom) |
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| 13:20 | IL16 - General Introduction to TMDD |
Dr David FAIRMAN
(GSK, Cambridge, United Kingdom) |
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| 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) |
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| 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) |
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| 14:35 | IL19 - Importance of Mechanistic Models in AHD Prediction (IL) |
Dr Birgit SCHOEBERL
(NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Cambridge, MA, United States) |
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| Drug Discovery Tales (I) |
| Session Chair |
Dr Nadia M. AHMAD
(CHARLES RIVER LABORATORIES, Harlow, United Kingdom) |
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| 15:50 | OC01 - Design and Synthesis of Novel RNA Binders for Therapeutic Applications |
Dr Maurinne BONNET
(ICN, Nice, France) |
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| 16:10 | OC02 - Is Resistance Futile? Discovery of Clinical Candidate AZD3229, A Pan-Mutant C-KIT Inhibitor
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Dr James SMITH
(ASTRAZENECA, Cambridge, United Kingdom) |
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| 16:45 | KL02 - Drug Discovery: Where are we Headed? |
Dr Wendy YOUNG
(MPM CAPITAL, Brisbane, CA, United States) |
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| Thursday January 27, 2022 |
Poster Session II - Even Numbers
Networking & Exhibition |
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| Drug Discovery Tales (II) |
| Session Chair |
Dr Nadia M. AHMAD
(CHARLES RIVER LABORATORIES, Harlow, United Kingdom) |
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| 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) |
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| 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) |
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| 14:15 | OC05 - Rational Design of Light-Controlled Bioactive Compounds for Photopharmacology |
Mr Piermichele KOBAURI
(UNIVERSITY OF GRONINGEN FSSC, Groningen, The Netherlands) |
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| 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) |
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| Covalent Targeting: Innovating for the Future |
| Session Chair |
Dr Vishal VERMA
(GENENTECH, INC., South San Francisco, United States) |
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| 15:50 | IL20 - Lysine-Targeting Covalent Inhibitors |
Dr Matthew CHEESEMAN
(THE INSTITUTE OF CANCER RESEARCH, Sutton, United Kingdom) |
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| 16:10 | IL21 - Reversible-covalent Inhibitors of the Kinase Activity of FGFR4 |
Dr Robin FAIRHURST
(NOVARTIS, Basel, Switzerland) |
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| 16:45 | IL22 - Studies with Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors |
Dr Agustin CASIMIRO-GARCIA
(PFIZER, United States) |
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| Friday January 28, 2022 |
| The "Catalytic Cycle" of Complex Molecule Synthesis and Methodology Development |
| Session Chair |
Prof. Tanja GAICH
(UNIVERSITY OF KONSTANZ, Konstanz, Germany) |
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| 13:05 | IL23 - Flow-based Methods for Chemical Peptide and Protein Synthesis". |
Prof. Nina HARTRAMPF
(UNIVERSITY OF ZURICH, Zürich, Switzerland) |
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| 13:25 | IL24 - Prins Cyclization in Natural Product Synthesis |
Prof. Ang LI
(SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, Shanghai, China) |
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| 14:00 | IL25 - Taming Multifaceted Nickel Catalysts: An Academic Fascination
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Prof. Ruben MARTIN
(INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA, Tarragona, Spain) |
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| 14:20 | IL26 - Computationally Augmented Total Synthesis |
Dr Timothy NEWHOUSE
(YALE UNIVERSITY, New Haven, United States) |
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| 16:00 | End of Alpine Winter Conference 2022 |
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