4th Alpine Winter Conference on Medicinal and Synthetic Chemistry

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

Topics

For each of the below topics, a slot in the programme will be available for an oral communication to be selected out of the submitted abstracts.

 

  • Session 1 : Recent Developments in Synthetic Methodologies and their Impact
Session Chair : Dr Fabrice GALLOU, Novartis Pharma, Switzerland
 
Within the last decade, a variety of synthetic methodologies and technologies have significantly impacted the way to conduct chemistry. Most of these approaches, such bio- or chemo-catalysis, flow chemistry, photo-catalysis, chemistry in water, have been part of the toolbox of the chemists in the past. Recent developments have indeed made them reached high technology readiness, thus making them amenable for profound impact in almost all aspects of chemistry.
 
  • Session 2 : From Underground to Mainstream: Neglected and Novel, Emerging Functional Groups for Drug Discovery
Session Chair : Dr Ulrich LÜCKING, FoRx Therapeutics, Switzerland
 

Extension of the medicinal chemistry toolbox is in the vital interest of drug designers who are confronted with the task of finding molecular solutions for an ever-increasing biological target space in a timely manner. However, in the daily routine, medicinal chemists often tend to stick to the functional groups and structural elements they know and love.

This session intends to provide inspiration for the utilization of non-mainstream moieties in drug discovery to overcome optimization hurdles.

 
  • Session 3 : Human Dose Prediction in the Discovery Space
Session Chair : Dr Sherri DUDAL, F. Hoffmann-La Roche, Switzerland
 
Human dose prediction for small molecules is mainly based on physiologically-based pharmacokinetic modeling (PBPK) to ensure the right exposure for a safe and effective treatment.  This is typically done in late drug discovery before entry into human trials, but in recent years, simplified versions of human dose prediction are used for ranking lead optimization of compounds to judge the feasibility of a chemical series to reach the expected therapeutic dose, based on a limited number of molecular properties. In some cases, this is complemented with early PKPD modeling strategies to provide insights to the therapeutic window.  The focus of the session will provide an overview and discussion on the benefits and risks of pre clinically used human dose predictions.
 
  • Session 4 : Radical Intermediates in Complex Molecule Synthesis
Session Chair : Prof. Nina HARTRAMPF, University of Zurich, Switzerland
 
Reactions proceeding through radical intermediates, such as electrochemical and photochemical reactions, are becoming increasingly popular in organic chemistry. New synthetic methods have significantly improved the selectivity and efficiency of these reactions, making them valuable tools for the synthesis of natural products and other complex, highly functionalized molecules. This session intends to showcase state-of-the-art methods that enable novel disconnections in target molecule synthesis that were unattainable with classic methods.
 
  • Session 5 : Antiviral Drug Discovery
Session Chair : Dr Michael SOFIA, Arbutus Biopharma, United States
 

Viral diseases have had a profound impact on human health.  Since the beginning of the 21st century the World Health Organization has declared fourteen infectious disease related public health emergencies eight of which are viral in origin and include SARS, Influenza H1N1, Ebola, MERS, Zika, SARS-CoV-2 and Monkeypox.  In addition, chronic viral diseases such as HIV, HCV, HBV, HSV and HPV continue to burden both the developed and underdeveloped regions of the world.  To compound the situation, there is a growing concern around the emergence of resistant variants of known viral pathogens and the potential for the emergence of new viruses.  These heightened concerns are fueled by an increase in population density and urbanization, increases in global travel and migration and the impact of climate change.

To counter the continual threat of viral diseases, it is imperative that focus be maintained not only on the development of vaccines to control the emergence of viral diseases within a population but also on the development of novel antiviral drugs to combat these infections once they take hold within a population.  The success of antiviral drugs in combating global public health challenges can be seen in the treatments developed to combat HIV infection and the cures developed for HCV.  To achieve such success, required that all available tools in the drug discovery toolbox including genomics, structural biology, computational chemistry, high throughput screening and modern chemical synthetic methods be leveraged. This session on Antiviral Drug Discovery will highlight progress in the discovery of novel agents to treat viral infections, and the strategies and methods used to deliver these agents to the clinic.       

  • Session 6 : Latest Advances and Approaches in Bioconjugation Drug Discovery
Session Chair : Dr Natalia CHERNYAKMerck & Co. Inc., United States
 

Targeted therapies have expectation of broadened therapeutic window due to tumor-specific drug delivery. In the field of targetted therapies, the antibody drug conjugate (ADC) space is continuing to make major breakthroughs "from bench to clinic" and proving its potential as a safe, efficacious, and cost-effective treatment. Notable achievements in the field include ImmunoGen submitting a BLA for Mirvetuximab soravtansine, Enhertu showing efficacy in HER2-low breast cancer, and 16 new ADCs entering first in human studies. These recent successes are opening a new chapter in the story of antibody-drug conjugates, paving a well-defined pathway to change the future of oncology treatments. In this session we want to highlight recent developments in this field.

 
  • Session 7 : Drug Discovery Tales 1 & 2
Session Chair : To be confirmed
 
This session will be put together by selected proposals out of the abstract submissions.

  • Session 8 : Cryo-EM: Applications for Structure-Based Drug Discovery
Session Chair : Dr Katharina DÜRR, OMass Therapeutics, United Kingdom
 

In recent years, cryo-electron microscopy (cryo-EM) has become a key technology for the structure-based design of drugs targeting disease-relevant macromolecules. This has been particularly transformative for drug targets which are not suitable for other structural methods (X-ray crystallography or NMR), such as integral membrane proteins. Advances in detector technology and image processing software have made this technique now broadly applicable for routine high-resolution structure determination of GPCR/G protein complexes, ion channels, solute carriers and other challenging targets. 

In this session, speakers from academia and industry will present examples of how cryo-EM has contributed to small molecule design and how it can be even implemented for high-throughput approaches such as fragment-based screening pipelines.