46èmes

www.medchem.fr

InternationalConference on

Medicinal Chemistry

RICT 2010RENCON TRES I N TERN AT ION ALES DE

CHIMIE THERAPEUTIQUEOrganisées par la Société de Chimie Thérapeutique (SCT)

Interfacing Chemical Biology and Drug DiscoveryReims - France,June 30 – July 2, 2010

Under the Auspices of:

SCT - Société de Chimie Thérapeutique, FranceUniversité de Reims (URCA)

Organising Committee

Local Organising Committee

Dr C. DENHEZDr S. GERARDProf. D. GUILLAUMEDr M. LARONZE-COCHARDProf. J. SAPI(University of Reims Champagne-Ardenne, Reims, France)

Scientific Organising Committee

Dr E. DIFFERDING (UCB, Braine-l'Alleud, Belgium)Dr R. DODD (ICSN, Gif-Sur-Yvette, France)Dr L. HENNEQUIN (AstraZeneca, Reims, France)Dr J. MULLER (Sanofi-Aventis, Paris, France)Dr P. PITCHEN (Institut de Recherche Pierre Fabre, Labège Innopole,

France)Dr Y. ROLLAND (Société de Chimie Thérapeutique, Châtenay-

Malabry, France)Prof. J. SAPI (University of Reims Champagne-Ardenne, Reims,

France)Prof. A. TARTAR (University Lille 2, Lille, France)Dr L. VAN HIJFTE (Johnson & Johnson Pharmaceutical Research and

Development, Beerse, Belgium)

Supported by

WELCOME

University of Reims-Champagne-Ardenne, its Faculty of Pharmacy and the ‘Institut de Chimie Moléculaire de Reims (ICMR)’ have the honour of hosting the 46th International Conference on Medicinal Chemistry (RICT 2010) between 30th June and 2nd July 2010.

This prestigious scientific meeting covers the major aspects of medicinal chemistry with particular emphasis on the importance of chemical biology in modern drug discovery. The scientific programme, which will include over 20 plenary lectures by internationally well-known scientists, focuses on recent achievements in:

- Target Selection and Validation for Drug Discovery - Chemical Biology, - Hit-to-lead: Identification, Selection, Development, - Case-studies: from Bench to Bedside, - Physico-Chemical Tools and Structural Studies,- Synthetic Chemistry: New Frontiers Impacting Drug Discovery.

The scientific committee ensures the high quality and diversity of the scientific programme together with the accessibility of the meeting to MSc and PhD students. For the latter, an advantageous registration fee will be proposed. Moreover, a special career session will be organised with industrial and academic participants.

During the meeting, the traditional prizes (P. Ehrlich Lecture Award and C. Mentzer Prize) of the ‘Société de Chimie Thérapeutique’ will be awarded to researchers or research teams for their outstanding contributions to medicinal chemistry. In addition, a poster session will provide the opportunity for all participants to present their current results. A “best poster” prize will also be attributed.

Looking forward to your active participation in Reims!

Prof. Janos SapiUniversity of Reims Champagne-Ardenne – Chairman of Local Organising Committee

AIM OF THE SYMPOSIUM

When looking back how drugs were discovered in the mid to late nineties, it becomes apparent that the role of chemists in this endeavor has dramatically changed. Where the role of the chemist mainly was to synthesize small organic molecules, aiming to opti-mize biological activity, it is clear that his role today goes largely beyond optimizing for primary biological activity.

Today, it is expected from the chemists to be multidisciplinary experts in the fields of biology, ADME-T, computer assisted drug de-sign, the use of various IT systems allowing to extract and visualize the data, patent space and law …, in order to be able to orches-trate the optimization of hit molecules to NMEs in a multi-factorial fashion. In addition, he is also expected to provide his organic chemistry skills to design tool compounds, imaging agents, PET ligands, solutions for diagnostic tools, etc …, enabling the biologists in the unravelling and understanding of the extremely complex biological systems. Finally, he is supposed to be able to propose alternative drug delivery technologies and/or prodrugs for improved systemic exposures. In summary, from being an expert in pure medicinal chemistry, the chemist’s role has now evolved to being an expert in chemical biology.

Since a number of years, the French Society for Medicinal Chemistry (Société de Chimie Thérapeutique – SCT) has paid full attention to this evolution, and this year again, the 46th International Conference on Medicinal Chemistry (RICT 2010) aims to bring together people concerned by the multiple aspects of Chemical Biology and Drug Discovery.

Dr Luc Van HijfteResearch Director Janssen-Cilag and Head Medicinal Chemistry Europe Johnson & Johnson Pharmaceutical R&D

Symposium Secretariat

RICT 2010 - 46èmes Rencontres internationales de Chimie thérapeutiqueLD OrganisationScientific Conference ProducersRue Michel de Ghelderode 33/2 B – 1348 Louvain-la-Neuve, BelgiumTel: +32 10 45 47 77 - Fax: +32 10 45 97 19secretariat@LDOrganisation.com - www.medchem.fr

© Photo: Office de Tourisme de Reims - Julien Thomas

PROGRAMMESESSION TOPICS:

- Target Selection and Validation for Drug Discovery - Chemical Biology,

- Hit-to-lead: Identification, Selection, Development,

- Case-studies: from Bench to Bedside,

- Physico-Chemical Tools and Structural Studies,

- Synthetic Chemistry: New Frontiers Impacting Drug Discovery.

CONFIRMED SPEAKERS:

Discovery of Inhibitors of MAPKAPK5, a Novel Target for Rheumatoid ArthritisDr Martin ANDREWS (GALAPAGOS, Mechelen, Belgium)

Topically Bioavailable and Systemically Safe PPARg Agonists as Sebum Modulators Dr Jean-Guy Boiteau (GALDERMA R&D, Sophia-Antipolis,France)

Pyrrolopyrimidine-Based P2X3 Antagonists for the Treatment of PainDr Louis-David CANTIN (ASTRAZENECA R&D, Montréal, Canada)

New Methods for Peptide SynthesisProf. David CRICH (ICSN, Gif-sur-Yvette, France)

Binding of the Macrocyclic Noncovalent Inhibitor TMC435 to its HCV NS3/NS4A Protease TargetDr Max CUMMINGS (TIBOTEC, Mechelen, Belgium)

Sugars and ProteinsProf. Ben DAVIS (OXFORD UNIVERSITY, Oxford, United Kingdom)

Hybrids, Natural Products with Neurotrophin ActivityDr Bruno FIGADERE (UNIVERSITY PARIS-SUD, Chatenay-Malabry, France)

Telbivudine, a Potent and Specific Anti-HBV Nucleoside Analogue: From the Bench to its Marketing Approvals (Tyzeka®, Sebivo®)Dr Gilles GOSSELIN (IDENIX, Montpellier, France)

Peptidomimetic Foldamers: Connecting Structure to FunctionDr Gilles GUICHARD (IECB, Bordeaux, France)

The First NO- and Heam-independent Activator of Soluble Guanylate Cyclase for the IV Treatment of Acute Heart FailureDr Michael G. HAHN (BAYER HEALTHCARE, Wuppertal, Germany)

Two Stimulating Concepts in Natural Substances Synthesis: the NEO Cascade and the CIM StrategyProf. Arnaud HAUDRECHY (UNIVERSITY OF REIMS CHAMPAGNE-ARDENNE, Reims, France)

Identification of Functionally Selective Alpha2C-AR Agonists as Potential New Drugs for Treatment of PainDr Eric JNOFF (UCB PHARMA, Braine-l'Alleud, Belgium)

Virtual Screening in Drug Discovery: Overview and ApplicationsDr Romano KROEMER (SANOFI AVENTIS, Vitry sur Seine, France)

Inhibitors of PKC-beta and GSK-3beta: A Tale of Two KinasesDr Bruce MARYANOFF (SCRIPPS, San Diego, California, United States)

Active Pharmaceutical Ingredients in Convergent Technologies: How Are They ChosenDr Cynthia MARYANOFF (CORDIS, A JOHNSON AND JOHNSON COMPANY, Spring House, Pennsylvania, United States)

Fragment-based Design of Small RNA BindersDr Laurent MICOUIN (UNIVERSITY PARIS DESCARTES, Paris, France)

A Single Synthetic Peptide for Immunomodulating Lupus, a Complex Autoimmune Disease.Dr Sylviane MULLER (IBMC-CNRS, Strasbourg, France)

Prodrug Approaches for Enhancing the Bioavailability of DrugsProf. Christa MÜLLER (UNIVERSITY OF BONN, Bonn, Germany)

Vascular Tumor TargetingProf. Dario NERI (ETH, Zurich, Switzerland)

Functional Assays as Multifaceted Tools for HTSDr Olivier NOSJEAN (SERVIER RESEARCH INSTITUTE, Croissy-sur-Seine, France)

The Identification of Selective p38 MAPK Inhibitors with High Blood Potency Suitable for Clinical Development: The Discovery of Losmapimod Dr Vipul K. PATEL (GLAXOSMITHKLINE, Stevenage, United Kingdom)

Novel Antagonists of Protease Activated Receptors 1: Unusual GPCRs Implicated in Cardio-vascular DiseasesDr Michel PEREZ (PIERRE FABRE RESEARCH INSTITUTE, Castres, France)

Indole-carboxylic Acid Amides as Novel CETP Inhibitors: From Hit to Clinical Candidate and Beyond.Dr Philippe PFLIEGER (F. HOFFMANN-LA ROCHE, Basel, Switzerland)

Carbonic Anhydrases: Novel Therapeutic Applications for Inhibitors and ActivatorsProf. Claudiu SUPURAN (UNIVERSITY OF FIRENZE, Sesto Fiorentino, Italy)

Novel Compound Classes as Calcilytics for the Treatment of OsteoporosisDr Leo WIDLER (NOVARTIS, Basel, Switzerland)

PROGRAMME SCHEDULE

Therapeutic Innovation: Vocations & CareersIn parallel to the scientific session on Thursday, July 1, a careers session will be organised by pharma companies and professional associations to show to young scientists, PhD and predoctoral students, the variety of possible jobs and career opportunities in pharmaceutical R&D. To make this session affordable to these students, the registration fee for access to the scientific programme on Thursday and the careers session will be 15 € (please refer to registration rates).

Poster SessionsAll participants are invited to submit abstracts of a poster which will be peer-reviewed by the Organising Committee. Participants wishing to contribute with a poster should submit their abstract via the online submission tool on the symposium website: www.medchem.fr where a template with further details is also available. Registration is requi-red to submit an abstract, but payment is not mandatory at this stage. However, accepted summaries will only be published in the book of abs-tracts of the symposium after full payment of the registration fee. In case of any questions, please do not hesitate to contact the symposium secretariat (secretariat@LDOrganisation.com).

Abstract Categories:- Target Selection and Validation for Drug Discovery - Chemical Biology, - Hit-to-lead: Identification, Selection, Development, - Case-studies: from Bench to Bedside, - Physico-Chemical Tools and Structural Studies,- Synthetic Chemistry: New Frontiers Impacting Drug Discovery.- Other

Deadline for abstract submission: May 25, 2010.

Commercial ExhibitionThe programme will also include a commercial exhibition which will form an integral part of the Symposium and will represent a unique opportunity for companies to present and promote their products to the numerous scientists involved in organic synthesis and medicinal che-mistry.

Wednesday June 30 Thursday July 1 Friday July 2

8:30 Registration Section A Section B

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9:30 Opening 9:00 Lecture 9:00 Lecture 9:00 Lecture

10:00 Lecture 9:45 Lecture 9:45 Lecture 9:45 Lecture

10:45 Coffee-break 10:30 Coffee-break 10:30 Coffee-break

11:15 Lecture 11:00 Lecture 11:00 Lecture 11:00 Lecture

12:00 Lecture 11:45 Lecture 11:45 Lecture 11:45 Lecture

12:45 LunchPoster session

12:30 LunchPoster session 12:15 Lecture

14:15 Lecture 14:00 Lecture 14:00 Lecture 13:00 End of Symposium

15:00 Lecture 14:45 Lecture 14:45 Lecture 13:00 Lunch

15:45 Coffee-breakPoster session 15:30 Coffee-break

16:30 Lecture 16:00 Lecture 16:00

17:15 Lecture 17:00 End of 2nd day

18:30 Poster sessionCocktail

17:30 - 18:30 Visit of the "Caves Taittinger"

20:00 Banquet

Optional banquet in the “Demeure des Comtes de Champagne” in Reims, Thursday, July 1

Optional banquet in the “Demeure des Comtes de Champagne” for not registered participant

Optional visit of the “Caves Taittinger”, Thursday July 1 - 17:30 (free of charge)

Profile (EUR) Price before 25/05/2010 Price after 25/05/2010

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*

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* SCT : Société de Chimie Thérapeutique (French Society for Medicinal Chemistry)

REIMS

Reims, one of the main gastronomic centres of France is eager to show you the

legacy of its glorious past and to lead you into a prestigious realm of the most

celebrated and festive of wines.

Proud of their traditions, the inhabitants of the Champagne region will gladly

introduce you to the making of their mythical wine by taking you on tours of

the wine cellars which were dug into the limestone, some of the more ancient

ones during the Gallo-Roman era.

Rich of traditions and centuries-old know-how, Reims has also become a mo-

dern and lively regional capital thanks to its location, at the crossroad of several

European routes, its economy and its first-rate teaching and research centre.

Three sites listed as UNESCO World Heritage, the refined atmosphere of the

Champagne Houses, a town centre which offers you both the elegance of its

Art Deco facades and its relaxed atmosphere which prevails in the streets and

on the café-terraces, a programme of many and varied cultural events, a green

environment where nature is queen…

The exhibition will take place from Wednesday, June 30 until Friday, July 2 and will be located centrally. Refreshment breaks will be held in the exhibition area to maximise attendance by delegates.

Please contact the symposium secretariat at secretariat@LDOrganisation.com for more detailed information about the exhibition and sponsoring opportunities.

AccommodationBlock of rooms in hotels of different price categories, with preferenti-al rates, have been blocked by WIP, the official hotel reservation cen-tre. In order to benefit from these rates, please make sure you book your room via the WIP online reservation system on www.medchem.fr www.medchem.fr. Furthermore, a limited number of student rooms will also be available at a very attractive price. More information will be available on the symposium website.

VenueFaculty of Pharmacy 51 rue Cognacq-Jay, 51096 Reims, FRANCE

LanguageThe official symposium language is English.

Symposium WebsiteFor more information about the Symposium and online registration please check the website www.medchem.fr All information will be updated regularly.

Important DeadlinesAbstract submission deadline: May 25, 2010Early registration deadline: May 25, 2010Hotel rooms – via WIP upon availabilities

Registration InformationYou have two easy ways to register:• online via www.medchem.fr• fill in the registration form and return it by mail or fax

to LD Organisation: Fax: +32-10-459719 e-mail: secretariat@LDOrganisation.com

The Registration Package Includes:• admission to all scientific sessions and exhibition• programme, abstract book• certificate of attendance• lunches and refreshment breaks• welcome cocktail

On Thursday July 1, you are invited (free of charge) for a visit of the famous “Caves Taittinger”. We will leave the Faculty around 17:15 and be back in Reims around 18:30. Places are limited so please register for the visit when registering for the Symposium. The banquet will then start at 20:00 in the "Demeure des Comtes de Champa-gne" in Reims.The banquet is optional for all registered participants with a contribution of 50 € . For the persons not registe-red for the symposium the price for the banquet is 80 €.

Registration and ConfirmationYou will always receive confirmation of your booking. An automatic reply will immediately follow any online regis-tration and a subsequent final confirmation will be sent by e-mail once your registration has been processed by our secretariat. If you do not receive these, please send an e-mail to secretariat@LDOrganisation.com to make sure that we have received your booking. Within two weeks from the confirmation, a pro-forma invoice for your participation will be sent by our accounting depart-ment. Please notify any corrections to your registration

immediately. Invoices with proof of payment will be sent after reception of the payment.All registrations which have been confirmed by LD Orga-nisation are considered valid registrations, unless cancel-led within two weeks from the registration date. After the indicated date, cancellation fees are due. Please note that only registered participants will have access to the social programme and all services provided by the sym-posium secretariat.

Liability and InsuranceNeither the Organisers nor LD Organisation will assume any responsibility whatsoever for any damage or injury to persons or property during the Symposium. Participants should make their own arrangements with respect to tra-vel and health insurance.

CancellationSubstitutions may be made at any time, but please advise the Symposium Secretariat of any change of name.In case of cancellation prior to June 1, 2010, by written notice, registration fees will be refunded, less 125 Euro processing charges. Unfortunately, after this date no other cancellations refunds can be given.In the unlikely event that the Organising Committee shall deem it necessary to cancel the symposium, all pre-paid registration fees will be reimbursed. Neither LD Organi-sation, nor the Organising Committee shall be liable for reimbursing travel costs or accommodation arrangements made by individual delegates.

PaymentIf possible, please use the online payment opportunity while registering online via the Symposium website www.medchem.fr

Otherwise, payments, net of all bank costs, should be made to the Symposium Secretariat by payment to ac-count n° 340-1813781-16IBAN: BE72 3401 8137 8116BIC: BBRUBEBBBank: ING - Rue des Wallons 2 - B-1348 Louvain-la-Neuvementioning "RICT 46", name and registration number of the participant

Collective remittances should be accompanied by a list of names. Within two weeks from the confirmation of your registration, a pro-forma invoice for your participation will be sent by our accounting department. Please notify any corrections to your registration immediately. Regis-trations are only final after full payment of the fees.

GENERAL INFORMATION