EFMC-ISMC 2018

XXV EFMC International Symposium on Medicinal Chemistry

 Ljubljana, Slovenia    September 2-6, 2018

Programme Schedule


13:30

Registration

16:00

Opening Ceremony

Prof. Marko ANDERLUH
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia

16:20

Chair

Prof. Marko ANDERLUH
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia

Zika Virus: An Old Virus with a New Face

Prof. Tatjana AVSIC-ZUPANC
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia

16:50

Chair

Dr Yves P. AUBERSON
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland

It’s a Small-Molecule World: Medicinal Chemistry Challenges and Opportunities for the Next Decade

Dr Bayard HUCK
MERCK BIOPHARMA, Darmstadt, Germany

17:20

Award Ceremony

Dr Yves P. AUBERSON
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland

17:40

Chair

Prof. Henk TIMMERMAN
VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands

NAUTA AWARD FOR PHARMACOCHEMISTRY
Tools and Drugs for Purine Targets - Important Players in Inflammation and Cancer

Prof. Christa MÜLLER
UNIVERSITY OF BONN, Bonn, Germany

18:25

Chair

Prof. Hans Ulrich STILZ
NOVO NORDISK, Cambridge, United States

Synthetic Glycoconjugate Vaccines against Bacterial Infections

Prof. Peter H. SEEBERGER
MAX PLANCK INSTITUTE OF COLLOIDS AND INTERFACES, Berlin, Germany

19:10

Welcome Reception

20:30

End of the Day

08:30

Chair

Dr Laurent PROVINS
UCB, Braine-l'Alleud, Belgium

UCB-EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
How Best to Discover Bioactive Small Molecules?

Prof. Adam NELSON
UNIVERSITY OF LEEDS, Leeds, United Kingdom

09:15

Chair

Prof. Roberto DI SANTO
SAPIENZA UNIVERSITY OF ROME, Rome, Italy

The Therapeutic Challenge of the New Era: Developing and Making Available Life Changing Treatment to Patients with Rare Diseases

Dr Diego ARDIGO
CHIESI GROUP, PARMA, Italy

10:00

Exhibition & Coffee

10:30

Start of sessions

Session 1 'Technologies'

Artificial Intelligence Applications in Medicinal Chemistry
Session 2 'Therapeutic Areas'

Immuno-Oncology: Novel Therapeutic Opportunities
Session 3 'Chemical Biology'

Glycans in Medicinal Chemistry: Carbohydrate-Based Vaccines
(EuChemS Session)
Session 1 'Technologies'

Artificial Intelligence Applications in Medicinal Chemistry
10:30
Session Chair
Dr Jonas BOSTRÖM
ASTRAZENECA, Mölndal, Sweden
10:35
Artificial Intelligence. Not Just Another Name for in Silico Design
Dr David E. LEAHY
THE DISCOVERY BUS LTD, Macclesfield, United Kingdom
11:15
Re-Energising Small Molecule Drug Discovery
Dr Willem VAN HOORN
EXSCIENTIA, Dundee, United Kingdom
11:35
Computer-Aided Synthesis Planning
Mr Marwin SEGLER
BENEVOLENTAI, London, United Kingdom
11:55
Potency and Patents, New Arenas for Matched Molecular Pair Analysis in the AI World
Dr Al DOSSETTER
MEDCHEMICA LIMITED, Macclesfield, United Kingdom
Session 2 'Therapeutic Areas'

Immuno-Oncology: Novel Therapeutic Opportunities
10:30
Session Chair
Dr Luc VAN HIJFTE
MERCACHEMSYNCOM, Nijmegen, The Netherlands
10:35
Small Molecule Immune Checkpoint Antagonists for Cancer Therapy
Dr Murali RAMACHANDRA
AURIGENE DISCOVERY TECHNOLOGIES LTD, Bangalore, India
11:15
Tankyrase Inhibitor Development: Evidence for Potential in Cancer Immune Therapy
Prof. Stefan KRAUSS
UNIVERSITY OF OSLO, Oslo, Norway
11:35
Small Molecules Inhibiting PD1-PDL1 Immune Checkpoint
Dr Shabnam SHAABANI
UNIVERSITY OF GRONINGEN, Groningen, The Netherlands
11:55
New Small-Molecule Immune Checkpoint Inhibitors: A Step Forward in Cancer Immunotherapy
Ms Ana Rita DE CARVALHO ACURCIO
UNIVERSITY OF LISBON, Lisbon, Portugal
Session 3 'Chemical Biology'

Glycans in Medicinal Chemistry: Carbohydrate-Based Vaccines
(EuChemS Session)
10:30
Session Chair
Dr Sonsoles MARTIN-SANTAMARIA
BIOLOGICAL RESEARCH CENTER, Madrid, Spain
10:35
Breaking the Limits in Analyzing Carbohydrate Recognition by NMR
Dr Jesus JIMENEZ-BARBERO
CIC BIOGUNE, Derio, Spain
11:15
Targeting of Cancer Specific Glycopeptide Epitopes
Prof. Hans WANDALL
UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
11:35
A Multidisciplinary Strategy to Synthetic Carbohydrate-Based Conjugates for Vaccination against Shigella: from Concept to First-in-Human Study
Dr Laurence MULARD
PASTEUR INSTITUTE, Paris, France
11:55
Glycoside Antagonists of Bacterial Lectins: New Treatment Options for Recurrent and Antibiotic Resistant UTI
Prof. James JANETKA
WASHINGTON UNIVERSITY IN SAINT LOUIS, Saint Louis, United States
12:15

Exhibition & Lunch

13:15

Start of sessions

Session 4 'Technologies'

Timing is Everything: Target Binding Kinetics and Pharmacokinetics
Session 5 'Therapeutic Areas'

Life Science at the Interface of Agro and Pharma
Session 6 'Chemical Biology'

Recent Advances in Targeted Protein Degradation
Session 4 'Technologies'

Timing is Everything: Target Binding Kinetics and Pharmacokinetics
13:15
Session Chair
Prof. Ad P. IJZERMAN
LEIDEN UNIVERSITY, Leiden, The Netherlands
13:20
"Micro-Pharmacokinetics”: How Local Drug Concentration Influences Observed Binding Kinetics
Prof. Steven CHARLTON
UNIVERSITY OF NOTTINGHAM, Nottingham, United Kingdom
14:00
Allosteric Modulation of the mGlu2 Receptor: from Structure-Kinetic Relationships to in vivo Efficacy
(2017 MedChemComm Emerging Investigator Lectureship)
Dr Laura HEITMAN
UNIVERSITY OF LEIDEN, Leiden, The Netherlands
14:20
Target Binding Kinetics and its Relevance in the in vivo Context
Dr Liesbeth DE LANGE
UNIVERSITY OF LEIDEN, Leiden, The Netherlands
14:40
Large-Scale Analysis of Kinase Inhibitors' Target Binding Kinetics and its Implications for Drug Discovery
Ms Victoria GEORGI
BAYER AG, Berlin, Germany
Session 5 'Therapeutic Areas'

Life Science at the Interface of Agro and Pharma
13:15
Session Chair
Dr Franz VON NUSSBAUM
BAYER AG, Berlin, Germany
13:20
A New Target in Fungal Protein Biosynthesis: Shared Learnings for AgChem and MedChem
Dr Franz VON NUSSBAUM
BAYER AG, Berlin, Germany
14:00
Natural Products as Leads in Agrochemistry
Dr Joachim RHEINHEIMER
BASF, Ludwigshafen am Rhein, Germany
14:20
Synthesis and Fungicidal Activity of a New Family of Oxysterol Binding Protein Inhibitors
Dr Laura QUARANTA
SYNGENTA AG, Basel, Switzerland
14:40
Targeting Non Essential Bacterial Targets as a Novel Route to Counteract Bacterial Resistance
Prof. Gabriele COSTANTINO
UNIVERSITY OF PARMA, Parma, Italy
Session 6 'Chemical Biology'

Recent Advances in Targeted Protein Degradation
13:15
Session Chair
Dr Gregory HOLLINGWORTH
NOVARTIS PHARMA AG, Basel, Switzerland
13:20
Recent Advances in Bifunctional Degrader Molecules (e.g. SNIPER) for Targeted Protein Degradation via the Ubiquitin Proteasome System; Status and Outlook
Dr Mikihiko NAITO
NATIONAL INSTITUTE OF HEALTH SCIENCES, Tokyo, Japan
14:00
Targeting 'Undruggable' Transcription and Translation Factors for Degradation with Low Molecular Weight Cereblon Modulators
Dr Philip CHAMBERLAIN
CELGENE, San Diego, United States
14:20
The Zinc-Degrome
Dr Nicolas THOMÄ
FRIEDRICH MIESCHER INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland
14:40
Drugging the Fbw7 E3 Ligase with a Combined Computational and Biophysical Approach
Dr Carles GALDEANO
UNIVERSITY OF BARCELONA, Barcelona, Spain
15:00

Exhibition & Coffee

15:30

Start of sessions

Session 7

First Time Disclosures
Session 7

First Time Disclosures
15:30
Session Chair
Dr Emmanuel PINARD
F. HOFFMANN-LA ROCHE, Basel, Switzerland
15:35
Discovery of RG7916, a Selective SMN2 Splicing Modifier for the Treatment of Spinal Muscular Atrophy
Dr Hasane RATNI
F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland
16:05
Discovery of LOU064, a Covalent BTK Inhibitor with Best in Class Selectivity
Dr Robert PULZ
NOVARTIS PHARMA, Basel, Switzerland
16:35
Discovery of a Novel Oral NO- and Heme-Independent sGC Activator BAY 1101042
Dr Michael G. HAHN
BAYER HEALTHCARE, Wuppertal, Germany
17:05
First Time Disclosure of BI 409306, a First in Class PDE9 Inhibitor for the Treatment of CNS Diseases
Dr Riccardo GIOVANNINI
BOEHRINGER INGELHEIM, Biberach, Germany
17:35

Poster Session 1 (even numbers) & Networking

19:30

End of the Day

08:30

Chair

Dr Josep Jr. PROUS
PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain

PROUS INSTITUTE-OVERTON AND MEYER AWARD FOR NEW TECHNOLOGIES IN DRUG DISCOVERY
Activity-Based Proteomics - Protein and Ligand Discovery on a Global Scale

Prof. Benjamin CRAVATT
THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States

09:15

Chair

Dr Phil JONES
BIOASCENT, Glasgow, United Kingdom

Sugars & Proteins: Glycomimetics to Target Infectious Disease

Prof. Benjamin DAVIS
OXFORD UNIVERSITY, Oxford, United Kingdom

10:00

Exhibition & Coffee

10:30

Start of sessions

Session 8 'Technologies'

New Chemical Modalities in Medicinal Chemistry
Session 9 'Therapeutic Areas'

Targeting Aggregated Proteins in Neurodegenerative Diseases with Small Molecules
Sessions 10 'Chemical Biology'

Targeting the STING Pathway (Stimulator of Interferon Genes)
Session 8 'Technologies'

New Chemical Modalities in Medicinal Chemistry
10:30
Session Chair
Dr Eric VALEUR
ASTRAZENECA, IMED BIOTECH UNIT, Cambridge, United States
10:35
New Modalities for Complex and Unprecedented Biological Targets
Dr Eric VALEUR
ASTRAZENECA, IMED BIOTECH UNIT, Cambridge, United States
11:15
Cell Permeability with Beyond ‘Rule of 5’ Modalities – Do We Understand How This Works?
Dr Nick TERRETT
MERCK SHARP & DOHME RESEARCH GMBH (MSD), Kriens, Switzerland
11:35
Novel Hybrid Macrocyclic Modalities for Structure-Based Protein Mimetics
Dr Stephanie GUERET
ASTRAZENECA-MAX PLANCK INSTITUTE SATELLITE UNIT, Mölndal, Sweden
11:55
Small-Molecule Stabilization of Protein-Protein Interactions by Natural Products, Supramolecular Ligands, Fragments and Macrocycles
Dr Christian OTTMANN
EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands
Session 9 'Therapeutic Areas'

Targeting Aggregated Proteins in Neurodegenerative Diseases with Small Molecules
10:30
Session Chair
Dr Laurent PROVINS
UCB, Braine-l'Alleud, Belgium
10:35
Understanding Aggregation Inhibition of Alpha-Synuclein and Tau by Small Molecules
Prof. Markus ZWECKSTETTER
MAX PLANCK INSTITUTE FOR BIOPHYSICAL CHEMISTRY, Göttingen, Germany
11:15
Discovery of Peptidomimetics Targeting Protein-Protein Interactions of Alpha-Synuclein
Dr Wolfgang WRASIDLO
UNIVERSITY OF CALIFORNIA SAN DIEGO, La Jolla, United States
11:35
Targeting the Monomeric Intrinsically Disordered Structural State of Tau and Alpha-Synuclein by Small Molecules as a Potential Therapeutic Strategy for Alzheimer's and Parkinson’s Disease
Dr Gergely TOTH
CANTABIO PHARMACEUTICALS INC., Sunnyvale, United States
11:55
Brain-Penetrant Autophagy Modulators for Treating Neurodegenerative Diseases
Dr Steve ANDREWS
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
Sessions 10 'Chemical Biology'

Targeting the STING Pathway (Stimulator of Interferon Genes)
10:30
Session Chair
Dr Thorsten OOST
BOEHRINGER INGELHEIM, Biberach, Germany
10:35
Intracellular DNA Sensing in Health and Disease
Prof. Andrea ABLASSER
EPFL, Lausanne, Switzerland
11:15
Modification of Cyclic Dinucleotides to Enhance Modulation of the Innate Immune Response
Dr Diane COE
GLAXOSMITHKLINE, Stevenage, United Kingdom
11:35
Use of Cyclic Dinucleotides (CDNs) to Induce Stimulator of Interferon Genes (STING)-Dependent Antitumor Immunity
Dr Cedric BOULARAN
INVIVOGEN, Toulouse, France
11:55
In vivo Anti-Viral and -Tumor Effect Of 3’3’-cAIMP STING Activation
Dr Martin K. THOMSEN
AARHUS UNIVERSITY, Aarhus C, Denmark
12:15

Exhibition & Lunch

12:15

Chemical Computing Group Workshop
MOEsaic: The application of Matched Molecular Pair Analysis to SAR Exploration

13:15

Start of sessions

Flash Posters 1
Flash Posters 2
Flash Posters 3
Flash Posters 1
Chair
Prof. Lucija PETERLIN MASIC
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
13:15
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here
Flash Posters 2
Chair
Dr Ziga JAKOPIN
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
13:15
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here
Flash Posters 3
Chair
Dr Tihomir TOMASIC
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
13:15
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here
13:45

Start of sessions

Session 11 'Technologies'

Expanding Medicinal Chemists’ Synthetic Toolbox
Session 12 'Therapeutic Areas'

Breakthroughs in Polypharmacology Towards Neurological Disorders
(ACS Session)
Session 13 'Chemical Biology'

Chemical Biology Approaches to Target Identification
Session 11 'Technologies'

Expanding Medicinal Chemists’ Synthetic Toolbox
13:45
Session Chair
Prof. Gyorgy KESERU
HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary
13:50
Capturing Biological Activity in Natural Product Fragments by Chemical Synthesis
Prof. Karl GADEMANN
UNIVERSITY OF ZÜRICH, Zürich, Switzerland
14:30
Stuck in a Rut with Old Chemistry
Dr Jonas BOSTRÖM
ASTRAZENECA, Mölndal, Sweden
14:50
New Chemical Libraries in Exploration of Chemical Space
Prof. Jurij SVETE
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
15:10
Integrated System for the Expedited Generation and Characterization of Drug-Like Libraries for Hit-to-Lead Explorations
Prof. Antimo GIOIELLO
UNIVERSITY OF PERUGIA, Perugia, Italy
Session 12 'Therapeutic Areas'

Breakthroughs in Polypharmacology Towards Neurological Disorders
(ACS Session)
13:45
Session Chair
Prof. Maria Laura BOLOGNESI
UNIVERSITY OF BOLOGNA, Bologna, Italy
13:50
Multi-Functional Treatments for Multi-Factorial Neurodegenerative Disorders: the Challenge of Alzheimer's Disease
Dr Mark J. MILLAN
INSTITUT DE RECHERCHES SERVIER, Croissy-sur-Seine, France
14:30
Beyond Single-Target Activities: Using Polypharmacology and Systems Readouts for Compound Selection and Mode-of-Action Analysis
Prof. Andreas BENDER
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
14:50
In silico Polypolpharmacology
Dr Giovanni BOTTEGONI
HEPTARES THERAPEUTICS, Welwyn Garden City, United Kingdom
15:10
Metabotropic Glutamate Receptor Type 2 Positive Allosteric Modulators (mGlu2 Receptor PAMS) as a Transformational Epilepsy Treatment
Dr Jose CID
JANSSEN R&D, Toledo, Spain
Session 13 'Chemical Biology'

Chemical Biology Approaches to Target Identification
13:45
Session Chair
Prof. Herbert WALDMANN
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany
13:50
Activity-Based Glycosidase Profiling in Biomedicine and Biotechnology
Prof. Hermen OVERKLEEFT
LEIDEN UNIVERSITY, Leiden, The Netherlands
14:30
An Iron Hand over Cancer Stem Cells
Dr Raphaël RODRIGUEZ
INSTITUT CURIE, Paris, France
14:50
Charting the Structure-Resistance Landscape of Novel Antibiotics
Mr Tamas REVESZ
BIOLOGICAL RESEARCH CENTRE, HUNGARIAN ACADEMY OF SCIENCES, Szeged, Hungary
15:10
Buruli Ulcer and the mTOR Pathway: Total Synthesis, Structure-Activity and Target Elucidation Studies of Mycolactones
Prof. Matthias GEHRINGER
UNIVERSITY OF TUEBINGEN, Tuebingen, Germany
15:30

Exhibition & Coffee

16:00

Start of sessions

Flash Posters 4
Flash Posters 5
Flash Posters 6
Flash Posters 4
Chair
Prof. Danijel KIKELJ
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
16:00
Opportunity for 15 young scientists to present a summary of their poster

Discover the presenters here
Flash Posters 5
Chair
Prof. Jurij SVETE
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
16:00
Opportunity for 15 young scientists to present a summary of their poster

Discover the presenters here
Flash Posters 6
Chair
Prof. Janez ILAS
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
16:00
Opportunity for 15 young scientists to present a summary of their poster

Discover the presenters here
16:45

Poster Session 2 (odd numbers) & Networking

18:45

End of Poster Session

20:00

Concert

08:30

Chair

Dr Jürgen MACK
BOEHRINGER INGELHEIM, Biberach an der Riss, Germany

Development of Non-Nucleosidic Compounds against DNA Viruses of the Herpes Group. The Era After Nucleosides: Letermovir and Pritelivir

Dr Helga RÜBSAMEN-SCHAEFF
AICURIS GMBH & CO. KG, Wuppertal, Germany

09:15

EFMC Prize Ceremony

Dr Matthew TOZER
CONSULTANT, Cambridge, United Kingdom
Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal

09:20

EFMC Prize for a Young Medicinal Chemist in Industry
The Challenges of Restoring Programmed Cell Death Through MCL1 Inhibition

Dr Marton CSEKEI
SERVIER RESEARCH INSTITUTE OF MEDICINAL CHEMISTRY, Budapest, Hungary

09:40

EFMC Prize for a Young Medicinal Chemist in Academia
Carbohydrate-binding Proteins as Targets for Anti-Infectives and Diagnostics: ESKAPE pathogen Pseudomonas aeruginosa and its Lectins

Dr Alexander TITZ
HELMHOLTZ INSTITUTE FOR PHARMACEUTICAL SCIENCES, Saarbrücken, Germany

10:00

Exhibition & Coffee

10:30

Start of sessions

Session 14 'Technologies'

Development of New Synthetic Methodologies for Drug Discovery
(CPA Session)
Session 15 'Therapeutic Areas'

Upcoming Treatments for NASH and Other Fibrotic Diseases
Session 16 'Chemical Biology'

Recent Developments in Kinase Inhibitors
Session 14 'Technologies'

Development of New Synthetic Methodologies for Drug Discovery
(CPA Session)
10:30
Session Chair
Dr Ming-Qiang ZHANG
AMGEN, Shanghai City, China
10:35
Tricyclic Peptides via Templated Tandem CLIPS/CUAAC Cyclizations
Prof. Peter TIMMERMAN
PEPSCAN THERAPEUTICS, Lelystad, The Netherlands
11:15
Asymmetric Synthesis of Statin API as the Hypolipidemic Agents: The Evolution from the Chemical Kinetic Resolution to the Asymmetric Catalytic Technology (An Odessy)
Prof. Fener CHEN
FUDAN UNIVERSITY, Shanghai Shi, China
11:35
Practical Asymmetric Hydrogenation
Prof. Xumu ZHANG
SOUTHERN UNIVERSITY OF SCIENCE AND TECHNOLOGY, Guangdong, China
11:55
Synthesis of MedChem-Relevant Gem-Difluorocycloalkane Building Blocks
Prof. Dmytro VOLOCHNYUK
ENAMINE LTD, Kyiv, Ukraine
Session 15 'Therapeutic Areas'

Upcoming Treatments for NASH and Other Fibrotic Diseases
10:30
Session Chair
Prof. Roberto PELLICCIARI
TES PHARMA SRL, Corciano, Italy
10:35
Obeticholic Acid, Leading in the NASH Race. History and Perspectives
Prof. Roberto PELLICCIARI
TES PHARMA SRL, Corciano, Italy
11:15
Discovery of LJN452 (Tropifexor), a Highly Potent, Non-Bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and NASH
Dr David TULLY
NOVARTIS, Emeryville, United States
11:35
The First Class of Orally Available Mono-Saccharide Galectin-3 Inhibitors for Treatment of Fibrosis (NASH) and Cancer
Dr Fredrik ZETTERBERG
GALECTO BIOTECH, Gothenburg, Sweden
11:55
Development of Small-Molecule Inhibitors of Adipose Triglyceride Lipase (ATGL)
Ms Anna MIGGLAUTSCH
TU GRAZ, Graz, Austria
Session 16 'Chemical Biology'

Recent Developments in Kinase Inhibitors
10:30
Session chair
Prof. Stefan LAUFER
UNIVERSITY OF TÜBINGEN, Tübingen, Germany
10:35
EGFR Triple Mutant L858R_T790M_ C797S Recent Set-Backs and New Hope in Fighting Mutant Non-Small Cell Lung Cancer
Prof. Stefan LAUFER
UNIVERSITY OF TÜBINGEN, Tübingen, Germany
11:15
Design and Rationale for Exquisite Selectivity of Preclinical and Clinical Kinase Inhibitors
Dr Laurent SCHIO
SANOFI, Vitry sur Seine, France
11:35
Chemical Probes for New Therapeutic Concept Discovery
Dr Peter ETTMAYER
BOEHRINGER-INGELHEIM, Vienna, Austria
11:55
Discovery of the TYK2 Selective Inhibitor PF-6826647 for the Treatment of Crohn’s Disease, and Other Autoimmune Conditions
Dr Brian GERSTENBERGER
PFIZER, Cambridge, United States
12:15

Exhibition & Lunch

12:15

Schrödinger Workshop
Data Driven Drug Design – Using LiveDesign

13:15

Start of sessions

Session 17

Emerging Topics
Session 18 'Therapeutic Areas'

Addressing Infectious Diseases in the Developing Countries
(AFMC Session)
Session 19 'Chemical Biology'

The Sphingosine-1-Phosphate Axis: Therapeutic Potential in Inflammation, Cancer, and More
(ACS Session)
Session 17

Emerging Topics
13:15
Session Chair
Prof. Gabriele COSTANTINO
UNIVERSITY OF PARMA, Parma, Italy
13:20
Development of Potent, Selective, CNS Penetrant Small Molecule Inhibitors of Notum to Potentiate Wnt Signaling for the Maintainance of Synaptic Function in Alzheimer’s Disease
Prof. Paul FISH
ARUK UCL DRUG DISCOVERY INSTITUTE, London, United Kingdom
13:40
Synthetic Small-Molecule RNA Ligands: Scope and Therapeutic Applications
Dr Maria DUCA
UNIVERSITÉ CÔTE D'AZUR, Nice, France
14:00
Discovery of First-in Class, Selective and Noncovalent Small Molecule Inhibitors of DNMT1
Dr Allan JORDAN
CANCER RESEARCH UK MANCHESTER INSTITUTE, Manchester, United Kingdom
14:40
IUPAC-Richter Prize Lecture
Discovery of CFTR Modulators For The Treatment of Cystic Fibrosis
Dr Peter GROOTENHUIS
VERTEX PHARMACEUTICALS, San Diego, United States
Session 18 'Therapeutic Areas'

Addressing Infectious Diseases in the Developing Countries
(AFMC Session)
13:15
Session Chair
Dr Renate GRIFFITH
UNIVERSITY OF NEW SOUTH WALES, UNSW Sydney, Australia
13:20
All Bugs are Shallow: Open Source Drug Discovery
Prof. Matthew TODD
UNIVERSITY COLLEGE LONDON, London, United Kingdom
14:00
Towards the Development of Novel Inhibitors for Chikungunya Virus Infection: Approaches in Structure-Activity-Metabolism Relationship (SAMR) Studies
Prof. Christina CHAI
NATIONAL UNIVERSITY OF SINGAPORE, Singapore, Singapore
14:20
Identification of New Antimalarial GSK607: An Example of Adaptive and Differentiated Early Drug Development
Dr Esther FERNANDEZ
GLAXOSMITHKLINE, Tres Cantos, Spain
14:40
Mechanisms of HIV-1 Nucleocapsid Protein Inhibition by Small Molecules Targeting RNA
Dr Alice SOSIC
UNIVERSITY OF PADOVA, Padova, Italy
Session 19 'Chemical Biology'

The Sphingosine-1-Phosphate Axis: Therapeutic Potential in Inflammation, Cancer, and More
(ACS Session)
13:15
Session Chair
Dr Tony LEE
GILEAD SCIENCES, Seattle, United States
13:20
Unravelling the Mysteries of the Sphinx: Novel Targets and Small-Molecule Therapeutics from the Sphingolipid Synthesis and Signaling Pathway
Prof. Bernard FLYNN
MONASH UNIVERSITY, Parkville, Australia
14:00
Active Site Inhibitors of Sphingosine 1-Phosphate Lyase - Exploring Novel Biology with Tool Compounds
Dr Sven WEILER
BASILEA PHARMACEUTICA INTERNATIONAL LTD., Basel, Switzerland
14:20
Controlling Sphingosine-1-Phosphate Levels as a Therapeutic Strategy
Dr Webster L. SANTOS
VIRGINIA TECH, Blacksburg, United States
15:00

End of the Day

15:30

Excursions

20:00

Banquet

08:30

Start of sessions

Session 20 'Technologies'

Recent Developments in Nucleoside Medicinal Chemistry
Session 21 'Therapeutic Areas'

Inflammatory and Autoimmune Diseases
Session 22 'Chemical Biology'

Enzyme Activators and Positive Allosteric Modulators
Session 20 'Technologies'

Recent Developments in Nucleoside Medicinal Chemistry
08:30
Session Chair
Dr Jared CUMMING
MSD, Boston, United States
08:35
Cyclic Dinucleotide STING Agonists as Anti-Tumor Agents
Dr Wes TROTTER
MSD, Boston, United States
09:15
Discovery of JNJ-64619178 as a Potent and Selective PRMT5 Inhibitor for the Treatment of Lung and Hematologic Cancers
Dr Jan Willem THURING
JANSSEN PHARMACEUTICA NV, Beerse, Belgium
09:35
Design and Synthesis of Congerners of Cyclic ADP-Ribose, a Ca2+-Mobilizing Second Messenger, Toward Identification of the Target Protein
Prof. Satoshi SHUTO
HOKKAIDO UNIVERSITY, Sapporo, Japan
09:55
Development of Novel Sialyltransferase Inhibitors via Computer Aided Drug Design
Mr Andrew MONTGOMERY
UNIVERSITY OF WOLLONGONG, Wollongong, Australia
Session 21 'Therapeutic Areas'

Inflammatory and Autoimmune Diseases
08:30
Session Chair
Prof. Stanislav GOBEC
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
08:35
Nonpeptidic Selective Inhibitors of Immunoproteasome
Prof. Stanislav GOBEC
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
09:15
Small Molecule Immunomodulators that Target Toll-Like Receptors
Prof. Hang YIN
TSINGHUA UNIVERSITY, Beijing, China
09:35
A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase to Treat Non-Alcoholic Steatohepatitis
(EFMC-YMCS Presentation Prize)
Dr Daniel MERK
ETH ZÜRICH, Zürich, Switzerland
09:55
Discovery of SPL-707: A Potent, Selective, and Orally Bioavailable SPPL2a Inhibitor
Dr Juraj VELCICKY
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
Session 22 'Chemical Biology'

Enzyme Activators and Positive Allosteric Modulators
08:30
Session Chair
Prof. Joachim MITTENDORF
BAYER AG, Wuppertal, Germany
08:35
Design, Synthesis, and Mechanism of β-Glucocerebrosidase Activators for Gaucher’s and Parkinson’s Diseases
Prof. Richard B. SILVERMAN
NORTHWESTERN UNIVERSITY, Evanston, United States
09:15
Positive Allosteric Modulators of the GABA-B Receptor
Dr Sean C. TURNER
ABBVIE, Ludwigshafen am Rhein, Germany
09:35
The Value of Orthogonal Techniques for Elucidating Binding Site(s) of GPCR Allosteric Modulators: a Case Study With Positive Allosteric Modulators of Dopamine Receptors
Dr Anne VALADE
UCB, Braine-l'Alleud, Belgium
09:55
AMPA Receptor Positive Allosteric Modulators Based on New Scaffolds: Design, Synthesis, and Studies
Dr Vladimir A. PALYULIN
LOMONOSOV MOSCOW STATE UNIVERSITY, Moscow, Russia
10:15

Exhibition & Coffee (brunch)

10:45

Start of sessions

Session 23 'Technologies'

PET Imaging as a Tool for in vivo Drug Evaluation and Development
(EANM Session)
Session 24

Late Breaking News
Session 25 'Therapeutic Areas'

Cardiometabolic Diseases
Session 23 'Technologies'

PET Imaging as a Tool for in vivo Drug Evaluation and Development
(EANM Session)
10:45
Session Chair
Prof. Antony GEE
KING'S COLLEGE LONDON, London, United Kingdom
10:50
PET Molecular Imaging – an Overview
Prof. Antony GEE
KING'S COLLEGE LONDON, London, United Kingdom
11:30
PET in Neuroscience Drug Discovery and Development
Dr Magnus SCHOU
KAROLINSKA INSTITUTE, Stockholm, Sweden
11:50
PET for Oncology Drug Discovery and Development
Prof. Bert WINDHORST
VU UNIVERSITY MEDICAL CENTER, Amsterdam, The Netherlands
12:10
Discovery of Candidates for PET Molecular Imaging of Pathological TDP-43 Aggregates in Frontotemporal Dementia and Amyotrophic Lateral Sclerosis Patients
Dr Vincent DARMENCY
AC IMMUNE SA, Lausanne, Switzerland
Session 24

Late Breaking News
10:45
Session Chair
Dr Anna KARAWAJCZYK
SELVITA, Krakow, Poland
10:50
First Disclosure of the Clinical Candidate BAY-840, a Potent And Selective hBradykinin B1 Antagonist for the Treatment of Chronic Inflammatory Diseases, Generated within the Bayer-Evotec Strategic Alliance
Dr Stefan BÄURLE
BAYER AG, Berlin, Germany
11:10
Discovery of GDC-0077: A Highly Selective Inhibitor and Degrader of Mutant PI3K-Alpha
Dr Jamie KNIGHT
CHARLES RIVER, Harlow, United Kingdom
11:30
Anti-HBV Drug Discovery Enabled by Structure-Based Drug Design and Phenotypic Screening
Dr Hong SHEN
ROCHE INNOVATION CENTER, Shanghai, China
11:50
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 that Enables Transient Target Engagement for the Treatment of Haematological Malignancies
Dr Bernard BARLAAM
ASTRAZENECA, Cambridge, United Kingdom
12:10
The Discovery of CNP520, an Amino-1,4-Oxazine BACE Inhibitor in Prevention Studies
Dr Rainer MACHAUER
NOVARTIS PHARMA AG, Basel, Switzerland
Session 25 'Therapeutic Areas'

Cardiometabolic Diseases
10:45
Session Chair
Dr Jesper LAU
NOVO NORDISK, Maaloev, Denmark
10:50
C-Natruiretic Peptide Agonists for Cardiovascular Disease
Prof. David SELWOOD
UNIVERSITY COLLEGE LONDON, London, United Kingdom
11:30
The Discovery of Semaglutide - A Journey from Ala Scan to Structural Design of GLP-1 Analogues
Dr Jesper LAU
NOVO NORDISK, Maaloev, Denmark
11:50
Discovery and Optimization of Non-Covalent, Selective, and Bioavailable Small Molecule Inhibitors of the KEAP1-Nrf2 Pathway
Dr Hauke SZILLAT
SANOFI, Frankfurt, Germany
12:10
Discovery and Clinical Evaluation of MK-8150, a Novel Nitric Oxide Donor with a Unique Mechanism of Nitric Oxide Release
Dr Amjad ALI
MERCK & CO. INC., Kenilworth, United States
12:30

Chair

Dr Cornelia ZUMBRUNN
IDORSIA PHARMACEUTICALS, Allschwil, Switzerland

Smart Chemical Probes: from Bromodomain Ligands to Natural Products

Prof. Cristina NEVADO
UNIVERSITY OF ZURICH, Zurich, Switzerland

13:15

Closing Remarks, Poster Prizes and Welcome to EFMC-ISMC 2020

Prof. Marko ANDERLUH
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
Dr Yves P. AUBERSON
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland


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