EFMC-ASMC 2023

OC05 - Discovery of A Potent, Selective and Metabolically Stable mTOR Kinase Inhibitor Exploiting Morpholine Isosters

Dr Chiara BORSARI

UNIVERSITY OF MILAN, Milan, Italy

EFMC Prize Winner EFMC-YMCS 2022

Ms Floriane ESHAK

UNIVERSITY PARIS CITÉ, Paris, France

OC07 - Direct Access to Unnatural Drug-Like Molecules by Photocatalytic Late-Stage Functionalization

Prof. Olga GARCIA MANCHENO

UNIVERSITY OF MÜNSTER, Münster, Germany
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Prof. Olga GARCIA MANCHENO

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Prof. Dr. Olga García Mancheño is professor for organic chemistry at the University of Münster (WWU). She obtained her PhD in Chemistry in 2005 at the University Autonomous of Madrid under the supervision of Prof. J.C. Carretero. After her postdoc in the group of Prof. C. Bolm at RWTH Aachen, she carried out her habilitation at the WWU Münster. In 2013, she was appointed as professor for organic chemistry at the University of Regensburg and, in 2017, to her current position at the University of Münster. Her research aims at developing new, efficient synthetic methodologies in organic chemistry, with especial focus on the design of novel catalytic systems and their application in catalysis, including photocatalysis and asymmetric anion-binding catalysis, and late-stage functionalization towards valuable small and drug building-blocks.

Selected Awards: International Isotope Society IIS-CED Prize 2022, ORCHEM EJOC Lecture Award 2022, ERC Consolidator Grant (2017), ORCHEM Prize 2016, Young Researcher Award WWU Münster (2013), Thieme Chemistry Journal Award 2012, Extraordinary Doctorate-Award 2006 (U.A.M.), Lilly Investigation Award, Spanish II Edition (2004).

OC02 - Isolation and Biological Activities of Natural Products and Analogues from the Adriatic Coral Eunicella Cavolini

OC04 - High-Throughput Protac Synthesis and Direct to Biology Assaying for Rapidly Evaluating Targeted Protein Degradation

OC03 - Design and Optimization of High Performance KSPi ADCs With Increased Tumor Selectivity: Enhancing the Therapeutic Window by Legumain-Mediated ADC Activation

OC06 - Discovery of Imidazo[1,2-a]Pyridine Carboxamide BAY 1165747, a Long-Acting Soluble Guanylate Cyclase Stimulator for Resistant Hypertension

OC08 - Cocktails For 19F NMR Fragment Screening: From Theory to Applications Using Enamine’s Stock Chemical Space

Prof. Dmytro VOLOCHNYUK

ENAMINE LTD, Kyiv, Ukraine
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Prof. Dmytro VOLOCHNYUK

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Prof. Dmitriy Volochnyuk at present shares his time as senior scientific advisor of ENAMINE LTD, Head of Medicinal Chemistry Department at the Institute of Organic Chemistry NAS of Ukraine and Professor of Chemistry at the Institute of High Technologies of Taras Shevchenko National University of Kyiv. He received his PhD in Organic Chemistry in 2005 and Dr.Sci in Organic and Organomettalic Chemistry in 2011. Having been previously working at the key positions in CRO industry (2006–2010: Director of Chemistry at Enamine Ltd; 2010–2014: Executive Director at Curplyx–Macrochem; 2014 – 2017: New business development director at Life Chemicals), Prof. Volochnyuk has over 15-year experience in managing chemical outsourcing projects and is an expert in fluoroorganic, organophosphorus, heterocyclic, combinatorial and medicinal chemistry as well as in cheminformatics. He is an author of more than 180 scientific publications and 3 monograph chapters.

OC01 - Divergent Synthesis as an Emergent Tool for Drug Discovery

Opening Lecture
Synthetic and Medicinal Chemistry for Biologics

Prof. Jeffrey BODE

ETH ZURICH, Zürich, Switzerland
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Prof. Jeffrey BODE

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http://www.bode.ethz.ch

The explosion of biological molecules as therapeutic modalities is transition to a new generation of modified proteins, antibodies, capsids, and bioconjugates through combinations of recombinantly produced biologics and synthetic molecules. This frontier requires new synthetic methods suitable for preparing and modifying homogeneous, folded biomolecule molecules. To achieve this, we are developing new chemical and chemoenzymatic reactions that offer the chemoselectivty, rapid reaction kinetics, and compatibility with physiological conditions required for advancing the field. These efforts have led to new platforms for chemical protein synthesis, modification and bioconjugation of commercial antibodies, and site specific modification and elaboration of recombinant proteins. Together, these new synthetic methods blur the lines between synthetic and biological molecules and open a plethora of new therapeutic approaches.

Synthesis of Fluorinated Molecules Using Modern Synthetic Tools

Dr Tatiana BESSET

INSA OF ROUEN, Mont-Saint-Aignan, France
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Dr Tatiana BESSET

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Different synthetic approaches for the synthesis of original fluorinated molecules will be presented including new tools based on transition metal catalyzed C-H bond functionalization and the design of original reagents.

MicroCycle: A Machine Learning Driven, Automated and Integrated Platform for Drug Discovery

Dr Cara BROCKLEHURST

NOVARTIS, Basel, Switzerland
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Dr Cara BROCKLEHURST

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"MicroCycle: A Machine Learning Driven, Automated and Integrated Platform for Drug Discovery"

What if we could develop an integrated drug discovery platform to accelerate drug discovery, which utilises micro-scale chemistry, real-time biological and physicochemical characterisation and machine learning driven compound design? At NIBR this is a reality! Our automated medicinal chemistry ‘design-make-test-analyse’ cycle is powered by machine learning, enables sequential multi-parameter optimisation and generates knowledge in a timeframe never before possible. We have built MicroCycle; a modular technology platform which benefits from recent advances in plate based micro-scale chemistry, micropurification,[1]in-situ quantification and machine learning thus ensuring rapid access to high quality chemical matter already formatted for assay. Furthermore, by reorienting existing high throughput assay technology we can generate a full package of relevant data on each set of compounds in every learning cycle.

Next Generation Design-Make-Test-Analysis-Cycles

Dr Clara CHRIST

BAYER, Berlin, Germany
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Dr Clara CHRIST

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"Next Generation Design-Make-Test-Analysis-Cycles"

Digital tools are changing the way scientists are working in drug discovery projects. We will show examples how scientists can profit from the recent advances in machine learning and physics-based computational approaches. Examples from our research will be given.

Making Difficult-to-Make Molecules: Photochemistry as an Enabling Tool

Dr Susannah COOTE

UNIVERSITY OF BATH, Bath, United Kingdom
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Dr Susannah COOTE

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"Making Difficult-to-Make Molecules: Photochemistry as an Enabling Tool"

Application of photochemical transformations in creative synthetic approaches to interesting strained products, especially four-membered rings.

Why Chemputers Will Dream of Electric Drugs

Prof. Leroy CRONIN

UNIVERSITY OF GLASGOW, Glasgow, United Kingdom
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Prof. Leroy CRONIN

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"Why Chemputers Will Dream of Electric Drugs"

Can chemputers, robots that can potentially make any molecule, take AI-designs of drugs and make them in the lab? In this talk Lee Cronin will discuss chemputation, the process of turning code into molecules, the use of theory to design new makable molecules, and the concept of a chemical programming language to help all chemists around the world exchange reproducible laboratory protocols.

EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Industry

New Catalytic Approaches for Simplifying Complex Amine Synthesis

Prof. Darren J. DIXON

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Darren J. DIXON

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In this presentation, new “synthesis inspired” user-friendly broad scope catalytic strategies for forging the key carbon-carbon bonds of key late stage synthetic intermediates en route to various complex alkaloid natural products will be described.

Making and Breaking of C-S Bonds Using Metal Catalysis

Dr Ivana FLEISCHER

UNIVERSITY OF TÜBINGEN, Tuebingen, Germany

Precision Molecule Editing (a Game of Bio and Chemo-catalysis)

Prof. Rebecca GOSS

UNIVERSITY OF ST ANDREWS, St Andrews, United Kingdom

Chemical Probes and their Relevance for Drug Discovery Programs – Examples from the Endocannabinoid System

Dr Uwe GRETHER

F. HOFFMANN-LA ROCHE, Basel, Switzerland
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Dr Uwe GRETHER

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"Chemical Probes and their Relevance for Drug Discovery Programs – Examples from the Endocannabinoid System"

Chemical probes are of utmost importance for bringing drugs from the laboratory through the clinic and ultimately to the market. Optionally, they can carry one or more additional reporter groups to meet specific application requirements. Chemical probes support and affect all research and discovery phases: target verification and validation; assay development; lead optimization; and biomarker engagement in the context of preclinical studies and human trials. On the example of the cannabinoid receptor type-2 (CB2R) and monoacylglycerol lipase (MAGL), two highly health-relevant targets of the endocannabinoid system, the design, synthesis and application of chemical probes in different research and development stages will be discussed.

Novel Modes of Enzyme Inhibition

Dr Anders JOHANSSON

ASTRAZENECA, Molndal, Sweden
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Dr Anders JOHANSSON

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"Novel Modes of Enzyme Inhibition"

Achieving good oral bioavailability and high potency can be a challenge, especially for intracellular protein targets. For certain enzymes, we have discovered a novel mode of inhibition, allowing for the optimization of permeability and bioavailability, but at the same time achieving high potency inhibitors of the target enzyme.

Multicomponent Alkene Cross-Coupling by Base Metal Catalysis

Dr Ming Joo KOH

NATIONAL UNIVERSITY OF SINGAPORE, Singapore, Singapore

Can Chemistry Generate Biological Questions?

Prof. Nuno MAULIDE

UNIVERSITY OF VIENNA, Vienna, Austria
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Prof. Nuno MAULIDE

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"Can Chemistry Generate Biological Questions?"

Can chemical curiosity be the driving force behind biology? In this talk we will address selected case studies from our own research which aim to showcase how chemical ingenuity and “blue skies curiosity” can be harnessed for valuable contributions to biological problems.

From BRD4 to KRAS: 12 Years of Oncology Small Molecules

Dr Darryl MCCONNELL

BOEHRINGER INGELHEIM, Vienna, Austria
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Dr Darryl MCCONNELL

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"From BRD4 to KRAS: 12 Years of Oncology Small Molecules"

Twelve years ago, one of the hottest oncology targets was the epigenetic reader protein BRD4 which contains a highly druggable pocket for small molecules. Now the field is focused on drugging KRAS which contains arguably the most difficult to drug pocket medicinal chemists have faced to date. The talk will replay the highlights and challenges of this twelve year journey at Boehringer Ingelheim.

Structure Based Identification of Novel Albumin Binders for Half-Life Extensions of Proteins and Peptides

Dr Maria MÉNDEZ PÉREZ

SANOFI GERMANY, Frankfurt, Germany
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Dr Maria MÉNDEZ PÉREZ

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Dr. María Méndez Pérez is currently the head of SMD Medicinal chemistry and global IDD portfolio coordinator at Sanofi. Her team focuses on supporting drug-discovery programs in the areas of immunology and neurological diseases, focusing thereby on the implementation of novel technologies and workflows with the aim to shorten the DMTA cycle. María obtained her Ph.D. in organic chemistry from the Universidad Autónoma of Madrid in 2001, followed by postdoctoral research in catalysis at the MPI in Mülheim an der Ruhr and in theoretical chemistry at the TU in Berlin. She started her industrial career at Sanofi in 2006, where as medicinal chemist, she has worked with several target classes, modalities and disease areas in all discovery phases. As project leader or co-leader, she has contributed to the delivery of clinical candidates in the areas of diabetes and neuroscience.

Flow-enabled Synthesis of Fluorinated and Fluoroalkylated Moieties

Prof. Timothy NOËL

UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands

Synthesis of Glycosylated Natural Products or Analogues of Biological Interest

Dr Stéphanie NORSIKIAN

INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES, Gif-sur-Yvette, France

Phenotypic Screen to NLRP3 lead

Dr Daniel OEHLRICH

JOHNSON & JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT, Beerse, Belgium

Finerenone - A Novel Mineralo-Corticoid Receptor (MR) Antagonist

Dr Johannes PLATZEK

BAYER, Wuppertal, Germany
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Dr Johannes PLATZEK

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How to make an optically active & highly functionalized Dihydropyridine on ton scale?

Challenges and Opportunities in CNS Drug Discovery

Dr Frauke POHLKI

ABBVIE DEUTSCHLAND GMBH & CO.KG, Ludwigshafen, Germany

Covalent Chemical Biology with Natural Products and Novel Synthetic Warheads

Prof. Thomas POULSEN

AARHUS UNIVERSITY, Aarhus C, Denmark
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Prof. Thomas POULSEN

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Electrophiles are subject to strong interest within chemical biology and biomedicine. The discovery of novel, biologically relevant electrophiles can enable e.g. bioconjugation to native proteins for the preparation of biopharmaceuticals or provide new warhead-classes for targeted covalent inhibitors or fragments for screening. In my talk, I will provide examples from our most recent projects focused on electrophilic compounds, which span from fully synthetic constructs to natural products. I will discuss the different synthetic strategies involved and assessment of biological performance in biochemical and cellular contexts.

Enabling Technologies to Drive the MSD Portfolio

Dr Rebecca RUCK

MERCK, SHARP & DOHME, Rahway, United States
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Dr Rebecca RUCK

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"Enabling Technologies to Drive the MSD Portfolio"

The development and application of new enabling technologies is critical to the ideal preparation of our Active Pharmaceutical Ingredients. This talk will include how we think about these investments and recent utilization.

Novel Methods and Strategies for Rapid and Controlled Synthesis of Complex Antibiotics

Prof. David SARLAH

UNIVERSITY OF ILLINOIS, Urbana, United States
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Prof. David SARLAH

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This talk will cover recent synthetic efforts from Sarlah Lab, ranging from bottom-up synthesis of aminoglycosides to highly strained peptides.

Machine Learning to Accelerate Design-Make-Test Cycles

Dr Marwin SEGLER

MICROSOFT RESEARCH, Cambridge, United Kingdom

Natural Product Synthesis Through the Lens of Informatics

Prof. Ryan SHENVI

SCRIPPS RESEARCH, La Jolla, United States

Discovery of the First Orally Efficacious Small Molecules Disrupting the YAP-TEAD Interaction by Direct Competition

Dr Nicolas SOLDERMANN

NOVARTIS, Basel, Switzerland

Taking Molecular Glue Degraders to New Heights

Dr Owen WALLACE

MONTE ROSA THERAPEUTICS, Boston, United States
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Dr Owen WALLACE

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"Taking Molecular Glue Degraders to New Heights"

Targeted protein degradation has become a major focus for biotech and pharma over the last 5-10 years. Although molecular glue degraders (MGDs) have achieved significant clinical and commercial success, they have historically been discovered by serendipity. At Monte Rosa, we have established a platform, named QuEENTM (Quantitative and Engineered Elimination of Neosubstrates), that enables us to rationally discover and optimize molecular glue degraders. The QuEEN platform has generated a portfolio of programs across oncology, autoimmunity/inflammation and rare diseases which will be discussed.

EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Academia

Dr Georg WINTER

RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria