EFMC-ISMC 2010

21st International Symposium on Medicinal Chemistry

 Brussels, Belgium    September 5-9, 2010

17:00

Opening Ceremony

17:20

Innovative Medicines Initiative - Europe and Biopharmaceutical Innovation

Michel GOLDMAN
INNOVATIVE MEDICINES INITITATIVE JOINT UNDERTAKING, Brussels, Belgium

17:35

EFMC Award Ceremony

Chair

Gerhard ECKER
EFMC, UNIVERSITY OF VIENNA, Vienna, Austria

18:00

The NAUTA AWARD for Pharmacochemistry Lecture

Camille G. WERMUTH
PRESTWICK CHEMICAL, ILLKIRCH, France

Chair

Henk TIMMERMAN
VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands

18:35

Plenary Lecture
Genomes, Structural Biology and Drug Discovery: New Challenges from Difficult Targets and Neglected Diseases

Tom BLUNDELL
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom

Chair

Edmond DIFFERDING
DIFFERDING CONSULTING, Louvain-la-Neuve, Belgium

19:20

Welcome Reception

08:30

Plenary Lecture
A Chemical Approach to Controlling Cell Fate

Sheng DING
THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States

Chair

Rasmus Praetorius CLAUSEN
DANISH UNIVERSITY OF PHARMACEUTICAL SCIENCES, Copenhagen, Denmark

09:15

Exhibition & Coffee

10:00

Start of sessions

1. Chemical Strategies for Functional Proteomics - Activity-Based Protein Profiling
2. Hot Topics in Cardiovascular Diseases
3. Knowledge Enabled Drug Design
1. Chemical Strategies for Functional Proteomics - Activity-Based Protein Profiling
11:25
Development Of Chemical Probes For The Study Of The Cb1 And Cb2 Cannabinoid Receptors
Silvia ORTEGA GUTIERREZ
UNIVERSIDAD COMPLUTENSE DE MADRID, Madrid, Spain
2. Hot Topics in Cardiovascular Diseases
10:05
Canosimibe - Lowering of Atherogenic LDL by a Non-Systemic Cholesterol Absorption Inhibitor
Heiner GLOMBIK
SANOFI AVENTIS, Frankfurt, Germany
3. Knowledge Enabled Drug Design
11:25
Better Compounds Faster – The Development And Exploitation Of A Desktop Predictive Chemistry Toolkit
John CUMMING
ASTRAZENECA, Macclesfield, United Kingdom
11:45

Start of sessions

11:45
Poster Session 1 - Lunch
12:00
ACCELRYS WORKSHOP
Staying Ahead Of Your Medicinal Chemistry Project Data
13:45

Start of sessions

4. Chemical Approaches to Stem Cell Biology
5. Molecular Therapies for Iinflammatory and Autoimmune Diseases: Ongoing Clinical Trials and Future Prospects
6. Virtual Screening and Profiling
4. Chemical Approaches to Stem Cell Biology
15:10
Phenotypic Screening using Human Neural Precursor Cells as a Translational in vitro Model to explore the Process of Neurogenesis
Ravi JAGASIA
HOFFMANN - LA ROCHE, Basel, Switzerland
5. Molecular Therapies for Iinflammatory and Autoimmune Diseases: Ongoing Clinical Trials and Future Prospects
15:10
Optimisation Of The Diaminopyrimidine Carboxamide Series Leading To Highly Potent, Selective And Orally Bioavailable Syk Inhibitors
Neil GARTON
GLAXOSMITHKLINE, Stevenage, United Kingdom
6. Virtual Screening and Profiling
14:50
Cinderella’s Shoe For Virtual Drug Discovery, Screening And Design
Vladimir POTEMKIN
CHELYABINSK STATE MEDICAL ACADEMY, Chelyabinsk, Russia
15:30

Exhibition & Coffee

16:15

Start of sessions

7. Targeting Pathways
8. Hot Topics in CNS Diseases
9. Toxicity Challenges in Drug Design and Structure-Toxicity Relationships
7. Targeting Pathways
17:40
Phenotypic Drug Discovery at Lilly: Merging Images, Informatics and Chemistry to Enable SAR
Thomas ENGLER
ELI LILLY AND COMPANY, Indianapolis, United States
8. Hot Topics in CNS Diseases
16:20
Identification of a PDE9 Clinical Candidate for the Treatment of Alzheimer's Disease utilizing Prospective Design and Novel Protocol Development
Patrick Robert VERHOEST
PFIZER GLOBAL RESEARCH, Groton, United States
9. Toxicity Challenges in Drug Design and Structure-Toxicity Relationships
17:40
Systems Chemical Biology and Toxicogenomics
Karine AUDOUZE
CENTER FOR BIOLOGICAL SEQUENCE ANALYSIS -DTU, Lyngby, Denmark
18:20

Start of sessions

10. Sunset Session: Careers in Medicinal Chemistry
10. Sunset Session: Careers in Medicinal Chemistry
18:50
Career Evolution in the Med Chem Department of a Small Drug Discovery Company
Riccardo ZANALETTI
SIENA BIOTECH, Siena, Italy
20:30

Concert

08:30

2010 IUPAC-RICHTER Prize Lecture
Behind the Design of Darunavir for HIV/AIDS and β-Secretase Inhibitors for Alzheimer's Disease

Arun K. GHOSH
PURDUE UNIVERSITY, West Lafayette, United States

Chair

Robin GANELLIN
UNIVERSITY COLLEGE LONDON, London, United Kingdom

09:15

EFMC Prize for a Young Medicinal Chemist in Industry

Antonio NARDI
GRÜNENTHAL, Aachen, Germany

Chair

Mark BUNNAGE
PFIZER, Boston, United States

09:40

EFMC Prize for a Young Medicinal Chemist in Academia

Andreas BENDER
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom

Chair

Danijel KIKELJ
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia

10:00

Exhibition & Coffee

10:35

Start of sessions

11. Emerging Technologies
12. Novel Treatments for Obesity and Metabolic Disorders
13. Successful Strategies in Lead Discovery
11. Emerging Technologies
11:55
Nanotools for Biomedical Targets – Nanobodies Stabilize Active State of G-Protein Coupled Receptors
Jan STEYAERT
VUB-VIB, Brussels, Belgium
12. Novel Treatments for Obesity and Metabolic Disorders
11:35
Discovery of a Novel Gut-Targeted Microsomal Triglyceride Transfer Protein Inhibitor (JNJ-16269110) to Treat Obesity: Proof of Concept
Lieven MEERPOEL
JOHNSON & JOHNSON PRD, Beerse, Belgium
13. Successful Strategies in Lead Discovery
11:35
Ensemblins: A New Class of Therapeutic Macrocycles
Nick TERRETT
ENSEMBLE THERAPEUTICS CORPORATION, Kriens, Switzerland
12:15

Start of sessions

12:15
Poster Session 2 - Lunch
12:15
BIOSOLVEIT WORKSHOP
Fragment Based Ligand Design for Medicinal Chemists
13:45

Start of sessions

14. Innovative Drug Delivery Systems and Nanotechnologies - EUFEPS Session
15. Oncology Case Studies
16. Natural Products in Drug Discovery - Beyond Cytotoxics and Antiinfectives
14. Innovative Drug Delivery Systems and Nanotechnologies - EUFEPS Session
15:10
Thiomer Micro- and Nanoparticles in Drug Delivery
Andreas BERNKOP-SCHNÜRCH
LEOPOLD-FRANZENS UNIVERSITY, Innsbruck, Austria
15. Oncology Case Studies
14:55
Discovery of a Potent and Selective SMO Inhibitor
Stefan PEUKERT
NOVARTIS, Cambridge MA, United States
16. Natural Products in Drug Discovery - Beyond Cytotoxics and Antiinfectives
15:10
Antibiotic Clusters
Pal HERCZEGH
UNIVERSITY OF DEBRECEN, Debrecen, Hungary
15:30

Exhibition & Coffee

16:15

Start of sessions

17. Imaging Biomarkers
18. Hot Topics in Anti-Infectives
19. Covalent Inhibitors in Drug Discovery
17. Imaging Biomarkers
16:50
The Next Generation of PET Cardiac Imaging Agents: Discovery of Flurpiridaz F 18 for Detection of Coronary Disease and LMI1195 for Sympathetic Neuronal Imaging
Simon ROBINSON
LANTHEUS MEDICAL IMAGING, North Billerica, United States
18. Hot Topics in Anti-Infectives
16:20
Advances in Bacterial Fatty Acid Synthesis Inhibitors for Use against Toxoplasma gondii and Bacillus anthracis
Alan KOZIKOWSKI
UNIVERSITY OF ILLINOIS, Chicago, United States
19. Covalent Inhibitors in Drug Discovery
16:15
Session Chair
Tjeerd BARF
MERCK, Oss, The Netherlands
18:55

Start of sessions

20. Sunset Session: Academic curricula and industrial careers
20. Sunset Session: Academic curricula and industrial careers
18:40
Gary TRESADERN
JOHNSON & JOHNSON PHARMACEUTICAL R&D, Toledo, Spain
08:30

The UCB-EHRLICH AWARD for Excellence in Medicinal Chemistry Lecture
New HIV Therapies: the Discovery of Maraviroc and Lersivirine

Anthony WOOD
PFIZER, Waltham, United States

Chair

Christophe GENICOT
UCB SA, Bruxelles, Belgium

09:15

The PROUS INSTITUTE-OVERTON & MEYER Award for New Technologies in Drug Discovery Lecture
(R)Evolutions in Drug Discovery through Conceptual and Technological Innovations

Klaus MÜLLER
F. HOFFMANN-LA ROCHE, Switzerland

Chair

David PROUS
PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain

10:00

Exhibition & Coffee

10:30

Start of sessions

21. Process R&D and Scale-up: Chemistry, Crystals & More - Challenges and Success Stories
22. Emerging Drugs - Case Studies of Recently Disclosed New Medicines
23. The Challenges in Designing Multi-Targeted Ligands and Drugs - the Good, the Bad and the Ugly (ACS Session I)
21. Process R&D and Scale-up: Chemistry, Crystals & More - Challenges and Success Stories
11:55
Attrition Induced Grinding for the Synthesis of Some Commercial Drugs
Richard KELLOGG
SYNCOM B.V., Groningen, The Netherlands
22. Emerging Drugs - Case Studies of Recently Disclosed New Medicines
11:35
TMC 435, a Novel HCV Protease Inhibitor in Advanced Clinical Trials
Pierre RABOISSON
JANSSEN PHARMACEUTICAL COMPANIES
23. The Challenges in Designing Multi-Targeted Ligands and Drugs - the Good, the Bad and the Ugly (ACS Session I)
11:15
Serotonin/Noradrenaline Reuptake Inhibitors:A Case History in the Challenges of Multipharmacology Drug Discovery
Florian WAKENHUT
PFIZER CENTRAL RESEARCH, Kent, United Kingdom
12:15

Start of sessions

12:15
Poster Session 3 - Lunch
12:30
ELSEVIER WORKSHOP
REAXYS WORKSHOP: "GETTING TO KNOW REAXYS – ENHANCING YOUR CHEMISTRY RESEARCH"
15:00

Excursion

20:00

Gala Dinner

08:30

Start of sessions

24. G-Protein Coupled 7TM Receptors - New Insights into their Structure and Ligand Recognition
25. First Time Disclosures
26. Targeting Protein-Protein Interaction (AFMC Session)
24. G-Protein Coupled 7TM Receptors - New Insights into their Structure and Ligand Recognition
09:15
Activation Mechanism of class C GPCRs
Jean-Philippe PIN
CNRS-UNIVERSITY OF MONTPELLIER, Montpellier, France
25. First Time Disclosures
09:00
BGG492, a Competitive AMPA/kainate Antagonist in Clinical Development for the Treatment of Migraine and Epilepsy
Yves P. AUBERSON
NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland
26. Targeting Protein-Protein Interaction (AFMC Session)
08:30
Session Chair
Javier FERNANDEZ
JANSSEN R&D, Toledo, Spain
10:15

Exhibition & Coffee

10:45

Start of sessions

27. Finding the Right Binding Pockets: Allosteric Modulators of G-Protein Coupled Receptors for Non-CNS Diseases(ACS Session II)
28. Recent Case Studies in DD and Development
29. New Medicines Beyond Small Molecules - Novel Biologics
27. Finding the Right Binding Pockets: Allosteric Modulators of G-Protein Coupled Receptors for Non-CNS Diseases(ACS Session II)
12:10
Follicle Stimulating Hormone Receptor Negative Allosteric Modulators (Fshr Nam): Discovery And Development Of A New Series Of Orally Bioavailable Dimethoxy-Benzamides
Jean-Philippe ROCHER
ADDEX THERAPEUTICS, Plan-les-Ouates, Switzerland
28. Recent Case Studies in DD and Development
10:45
Session Chair
Gerhard ECKER
EFMC, UNIVERSITY OF VIENNA, Vienna, Austria
29. New Medicines Beyond Small Molecules - Novel Biologics
12:10
Engineered Protein Scaffolds as Next Generation Therapeutics
Arne SKERRA
TECHNICAL UNIVERSITY MUNICH, München, Germany
12:30

CLOSING LECTURE

Drugging the "Undruggable"

Gregory L. VERDINE
HARVARD UNIVERSITY, Cambridge, United States

Chair

André TARTAR
UNIVERSITY LILLE 2, Lille, France

13:15

Poster Prizes
Closing Remarks
Welcome to ISMC 2012