14th Swiss Course on Medicinal Chemistry 2022
Leysin Switzerland
9-14. October 2022, Alpine Classic Hotel
Program Overview
Sunday, October 9, 2022
16.00
Course check in
18.00
Welcome and Conference Opening Dinner
20.00
Welcome, housekeeping
Introduction into program and tutorials
Intro lecture by Gerhard Müller
Introduction into program and tutorials
Intro lecture by Gerhard Müller
20.15
Gerhard Müller, Anavo Therapeutics
«Medicinal Chemistry, a personal View»
«Medicinal Chemistry, a personal View»
21.00
End of official program
Monday, October 10, 2022
08.00
Klaus Urbahns, Merck
«Medicinal Chemistry of the Future: Trends, Targets and Technologies»
«Medicinal Chemistry of the Future: Trends, Targets and Technologies»
09.00
Werngard Czechtizky, AstraZeneca
«Medicinal Chemistry to Validate Novel Biological Targets»
«Medicinal Chemistry to Validate Novel Biological Targets»
10.00
Coffee Break
10.30
Jean-Louis Reymond, University of Bern
«Chemical Space for Drug Discovery»
«Chemical Space for Drug Discovery»
11.30
Karl-Heinz Altmann, ETH Zurich
«Natural Product - Based Drug Discovery»
«Natural Product - Based Drug Discovery»
12.30
Lunch
14.00
Didier Roche, Edelris
«New Paradigms in Hit Generation»
«New Paradigms in Hit Generation»
15.15
C. Commandeur, Symeres / M. Carneiro, ZoBio
«Biophysics meets MedChem: Discovery and Optimization of Bromodomain Inhibitors»
L. van Berkom, Symeres /K. Ritter, University of Tübingen
«FXa Inhibitors - Interrupted Case Studies»
«Biophysics meets MedChem: Discovery and Optimization of Bromodomain Inhibitors»
L. van Berkom, Symeres /K. Ritter, University of Tübingen
«FXa Inhibitors - Interrupted Case Studies»
A.Mortlock, Astra Zeneca
«The development of a lead»
N. Meanwell, BMS / G. Commandeur, Symeres
«Some Applications of Bioisosteres in Drug Design»
«The development of a lead»
N. Meanwell, BMS / G. Commandeur, Symeres
«Some Applications of Bioisosteres in Drug Design»
M. Whittaker, Ebryl Ltd. / M. Mazanetz, Novadata Solutions Ltd.
«Fragment based Lead Generation»
J. Viklund, Astra Zeneca / G. La Sala, Astra Zeneca
«Fragment- and Structure-based Design»
«Fragment based Lead Generation»
J. Viklund, Astra Zeneca / G. La Sala, Astra Zeneca
«Fragment- and Structure-based Design»
18.00
Debora Dumont, Bioqube Ventures
«Drug Discovery and Development: The Venture Capital Perspective»
«Drug Discovery and Development: The Venture Capital Perspective»
19.00
Dinner
20.30
Nicholas Meanwell, Bristol-Myers Squibb
«The Discovery of HCV NS5A Replication Complex Inhibitors Leading to Daclatasvir»
«The Discovery of HCV NS5A Replication Complex Inhibitors Leading to Daclatasvir»
21.30
End of Program
Tuesday, October 11, 2022
08.00
Peter Tonge, Stony Brook University
«Widening the Therapeutic Window: Kinetic Selectivity and Target Vulnerability»
«Widening the Therapeutic Window: Kinetic Selectivity and Target Vulnerability»
09.00
Gerhard Klebe, Philipps University Marbug
«What Thermodynamics Can Help to Understand Protein-Ligand Binding in Medicinal Chemistry»
«What Thermodynamics Can Help to Understand Protein-Ligand Binding in Medicinal Chemistry»
10.00
Coffee Break
10.30
Lars van der Veen, IOnctura
«PI3K inhibitors: be ready to get what you are screening for»
«PI3K inhibitors: be ready to get what you are screening for»
11.30
Gerhard Mueller, Anavo Therapeutics
«tba.»
«tba.»
12.30
Lunch
14.00
Andrew Mortlock, AstraZeneca
«The Development of PARP Inhibitors for the Treatment of Cancer»
«The Development of PARP Inhibitors for the Treatment of Cancer»
15.15
C. Commandeur, Symeres / M. Carneiro, ZoBio
«Biophysics meets MedChem: Discovery and Optimization of Bromodomain Inhibitors»
L. van Berkom, Symeres /K. Ritter, University of Tübingen
«FXa Inhibitors - Interrupted Case Studies»
«Biophysics meets MedChem: Discovery and Optimization of Bromodomain Inhibitors»
L. van Berkom, Symeres /K. Ritter, University of Tübingen
«FXa Inhibitors - Interrupted Case Studies»
A.Mortlock, Astra Zeneca
«The development of a lead»
N. Meanwell, BMS / G. Commandeur, Symeres
«Some Applications of Bioisosteres in Drug Design»
«The development of a lead»
N. Meanwell, BMS / G. Commandeur, Symeres
«Some Applications of Bioisosteres in Drug Design»
M. Whittaker, Ebryl Ltd. / M. Mazanetz, Novadata Solutions Ltd.
«Fragment based Lead Generation»
J. Viklund, Astra Zeneca / G. La Sala, Astra Zeneca
«Fragment- and Structure-based Design»
«Fragment based Lead Generation»
J. Viklund, Astra Zeneca / G. La Sala, Astra Zeneca
«Fragment- and Structure-based Design»
18.00
Special event: Wine tasting in the "Espace Nordique" in Les Mosses.
Course dinner
Course dinner
Wednesday, October 12, 2022
08.00
Gregg Siegal, ZoBio
«Application of Biophysics in Modern Drug Discovery: Fragments to Structure»
«Application of Biophysics in Modern Drug Discovery: Fragments to Structure»
09.00
Chun-Wa Chung, GlaxoSmithKline R&D UK
«tba.»
«tba.»
10.00
Coffee Break
10.30
Jenny Viklund, AstraZeneca
«Computational Chemistry - an Overview»
«Computational Chemistry - an Overview»
11.30
Andrea Decker, Novartis
«Drug Likeness: Physicochemical Properties in Small-Molecule Drug Discovery»
«Drug Likeness: Physicochemical Properties in Small-Molecule Drug Discovery»
12.30
Lunch
14.30
Special event: The heart of vineyards - Guided tour and wine tasting in Aigle Castle
Course dinner
Course dinner
Thursday, October 13, 2022
09.00
Andy Phillips, Aleksia Therapeutics
«Proximity-induced pharmacology: PROTACs, glues, and beyond»
«Proximity-induced pharmacology: PROTACs, glues, and beyond»
10.00
Simona Cotesta, Novartis
«JDQ443, a Structurally Novel Pyrazole-based Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors»
«JDQ443, a Structurally Novel Pyrazole-based Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors»
11.00
Coffee Break
11.30
Adrian Whitty, Boston University
«Macrocycles and other «beyond Rule-of-Five» Chemotypes»
«Macrocycles and other «beyond Rule-of-Five» Chemotypes»
12.30
Lunch
14.30
C. Commandeur, Symeres / M. Carneiro, ZoBio
«Biophysics meets MedChem: Discovery and Optimization of Bromodomain Inhibitors»
L. van Berkom, Symeres /K. Ritter, University of Tübingen
«FXa Inhibitors - Interrupted Case Studies»
«Biophysics meets MedChem: Discovery and Optimization of Bromodomain Inhibitors»
L. van Berkom, Symeres /K. Ritter, University of Tübingen
«FXa Inhibitors - Interrupted Case Studies»
A.Mortlock, Astra Zeneca
«The development of a lead»
N. Meanwell, BMS / G. Commandeur, Symeres
«Some Applications of Bioisosteres in Drug Design»
«The development of a lead»
N. Meanwell, BMS / G. Commandeur, Symeres
«Some Applications of Bioisosteres in Drug Design»
M. Whittaker, Ebryl Ltd. / M. Mazanetz, Novadata Solutions Ltd.
«Fragment based Lead Generation»
J. Viklund, Astra Zeneca / G. La Sala, Astra Zeneca
«Fragment- and Structure-based Design»
«Fragment based Lead Generation»
J. Viklund, Astra Zeneca / G. La Sala, Astra Zeneca
«Fragment- and Structure-based Design»
17.30
Chris Scarborough, Syngenta
«Lead Optimization in Crop Protection Research»
«Lead Optimization in Crop Protection Research»
19.30
Course Dinner: La Fromagerie (raclette or fondue)
Friday, October 14, 2022
09.00
Jonathan Mason, Sosei Heptares / Orexia Therapeutics
«Structure Based Drug Design for GPCR Targets: Lessons learnt and New Directions»
«Structure Based Drug Design for GPCR Targets: Lessons learnt and New Directions»
10.00
Yves Auberson, Novartis
«The Discovery of LML134, an H3R Inverse Agonists for Narcolepsy»
«The Discovery of LML134, an H3R Inverse Agonists for Narcolepsy»
11.00
Coffee Break
11.30
Gerhard Müller, Anavo Therapeutics
concluding remarks
concluding remarks
11.45
Lunch and End of the course