Yearbook 2018

 

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Yearbook 2018

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Editorial 1 EFMC YEARBOOK 20187 Dear colleagues, It is a great honour and privilege to assume the presidency of the EFMC as of January 2018. I am very grateful to the EFMC Council members and to the Executive Committee for their trust and support, and for the opportunity to serve our extended community. Thank you. With you, I want to build on what has been achieved to date and further develop EFMC’s influence, ensuring that our Federation adapts to its changing environment and best represents all aspects of our community. As time passes, the definition of medicinal chemistry evolves: Medicinal chemists are no longer expected to just provide innovative drug candidates, but also to develop tools to facilitate the study of cellular pathways and the evaluation of novel clinical candidates. These are high expectations, which led our community to foray beyond its original core competences in drug optimization, into the areas of chemical biology and molecular imaging. In parallel, the fundamental principles of our discipline evolve, as well as the way we communicate, present and teach it. None of this could be achieved without a high scientific level, which the EFMC will continue supporting through the organization of courses and congresses, including cutting-edge science and novel technological developments. With your help, I want to ensure close contacts and mutually supportive interactions between national organizations and the EFMC. Finally, I will support the implementation of an expanded communication strategy, including the use of social media, to better reach our extended community and main stakeholders. It is with great appreciation that I acknowledge Prof. Koen Augustyns for three remarkable years under his presidency. Koen has not only guaranteed the good functioning of the EFMC, which as such is already a significant achievement, but also developed its international network and influence. Over the last three years, EFMC has signed agreements with medicinal chemistry associations in Brazil, South Africa, India, and most recently with the Chinese Pharmacological Association. This materialized in enhanced interactions, shared sessions at scientific events, and the opportunity to increase the world-wide visibility of the European medicinal chemistry community. He also supported the initiation of a series of workshops at the European Parliament, in collaboration with EuCheMS, following up on the wish for EFMC to increase its influence on scientific directions and funding at European level. It has been both a great pleasure and a wonderful learning opportunity to work with him, and I look forward to continued interactions in his role as Past President. I am also looking forward to working with the team of the Executive Committee (EC), whose energy, support and valuable advice are always greatly appreciated: The EC is composed of Koen Augustyns (Past President) Anders Karlén (Secretary), Pascal George (Treasurer), Rui Moreira (EC Member), Toni Torrens (EC Member), Matt Tozer (EC Member) and Henk Timmerman (EFMC Advisor). Before providing an overview of the most important events of 2017 and of the activities planned by our Federation in 2018, I would also like to sincerely thank Miroslav Gasic, Raphaël Nudelman, Erhan Palaska and Janos Wölfling for their year-long contributions to the EFMC Council. Their successors are Ayla Balkan (Turkey), György Miklós Keseru (Hungary), Igor Opsenica (Serbia) and Eylon Yavin (Israel). Welcome. A review of 2017 Our main event was the 7th edition of the EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMCASMC’17), which took place in Vienna (Austria) on August 27-31st.

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2 Editorial Jointly organised by the EFMC, the medicinal chemistry section of the Austrian Chemical Society (GÖCH) and ChemBridge Corporation, EFMC-ASMC’17 brought together more than 500 scientists from 40 different nations. This biennial symposium is unique in combining talks on synthetic and medicinal chemistry, bringing together chemists from industry, academia and start-up companies from around the world. It was an enriching opportunity to discuss the most recent advances in synthetic methodology, their application to medicinal chemistry and drug discovery, and to network broadly. This very successful edition was led by Karin Briner (Novartis, US) and Erick Carreira (ETH Zürich, CH), to whom I would like to renew my thanks for putting together such a high-quality scientific program. The symposium was followed by the twoday long EFMC Young Medicinal Chemist Symposium (EFMC-YMCS’17). This edition was the most successful since the series began in 2014, gathering more than 160 young chemists at the University of Vienna. This talented and highly participating audience contributed to making the symposium a lively networking event. I am grateful to Thierry Langer and his committee for having put together a really interesting meeting, and for creating the right conditions for these dynamic exchanges. The 13th EFMC Short Course took place in April 2017 and was entitled “A Kinetic Perspective on Drug-Target Interactions”. I am thankful to Ad Ijzerman, Laura Heitman and Henk Timmerman (all three from the Netherlands) for organizing this course and Henk Timmermann for organizing this course and helping the EFMC fulfil its training and networking objectives. This series will continue with a course on peptide therapeutics. It is scheduled for April 22-25, 2018 and will be organised by Bart de Spiegeleer (Belgium). Detailed information can be found at www. efmcshortcourses.org In 2017, EFMC started preparing a STOA workshop at the European Parliament with EuCheMS. This event will focus on neurodegenerative diseases, especially Parkinson’s disease, to discuss research needs and the important role of medicinal chemistry in developing new therapies. Such workshops provide reference material for members of the parliament, and reinforce the visibility of EFMC and medicinal chemistry as a discipline at European level. EFMC also collaborated with several Federations beyond Europe to increase the visibility of European medicinal chemistry, and reinforce interactions with our partners: Koen Augustyns organized an EFMC session on Computer-Aided Drug Discovery at AIMECS 2017, the annual meeting of the Asian Federation of Medicinal Chemistry (AFMC). Henk Timmerman represented the EFMC at the annual meeting of the Chinese Pharmaceutical Association (CPA), the Chinese Academic Conference on Medicinal Chemistry, where Alessio Ciulli (UK) organized and chaired the EFMC session on “Promoting protein degradation as new drug discovery strategy”. The EFMC also co-organized the 2017 ACSMEDI-EFMC Medicinal Chemistry Frontiers meeting in Philadelphia, on June 25-28, with the Medicinal Chemistry Division of the American Chemical Society. Finally, what I believe to be a milestone in the future of our Federation has been reached this year when the Council unanimously agreed to formally recognize chemical biology as being in the scope of the EFMC. In practice, chemical biology is already included, as illustrated by the fact that many national organizations regroup both medicinal chemistry and chemical biology, and that our symposia also include chemical biology sessions. This message however needs to be reinforced, and the chemical biology community made more aware that EFMC also represents their interests in Europe. I am pleased by this development and look forward to the advancement of this initiative.

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Editorial 3 EFMC YEARBOOK 2018 Eyes on the future Our flagship meeting, the XXV EFMC International Symposium on Medicinal Chemistry, will be organised by the Section for Medicinal Chemistry of the Slovenian Pharmaceutical Society (SFD) and will take place in Ljubljana – Slovenia on September 2-6, 2018. In addition to plenary lectures and sessions on first disclosures, recent highlights and artificial intelligence in drug discovery, the symposium will be divided in three streams: Chemical Biology, Drug Discovery, and Medicinal Chemistry Related Technologies. Ljubljana is a great city and the scientific program will be exciting: EFMC-ISMC’18 is an event that shouldn’t be missed. It will be followed by the 5th edition of the EFMC Young Medicinal Chemist Symposium, on September 6-7. Judging by the success of the preceding edition, it will be a meeting worthwhile attending too, and I hope to welcome many of you there. To recognize scientific excellence, EFMC will confer three awards in 2018: The Nauta Award for Pharmacochemistry, the UCBEhrlich Award for Excellence in Medicinal Chemistry, and the Prous Institute-Overton and Meyer Award for New Technologies in Drug Discovery. The ceremonies will take place at the EFMC-ISMC’18. In addition, the EFMC Prizes for Young Medicinal Chemists in Academia and Industry will acknowledge the scientific accomplishments of two rising stars. The call for the 2018 Awards and Prizes are open, and I encourage you to submit nominations before the deadline of January 31. Over the coming year we will continuously provide updates on EFMC activities through our monthly newsletter MedChemWatch, via the EFMC LinkedIn group, via Twitter and on our regularly updated website www. efmc.info, which also offers a meeting calendar and a job portal. The EFMC is now also present on Facebook – with a page that will be managed, like all social media of the Federation, by a new Communication Team composed of young volunteers. Furthermore, I encourage you to submit contributions to MedChemComm, the EFMC journal, published monthly in collaboration with RSC. Let me close by wishing you all the best for a successful and happy 2018, both in your professional and personal life. With my very best personal regards, Yves P. Auberson EFMC President

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Reflection 4 Reflection on 2015-2017 Dear colleagues, It has been a great honour to serve the European Federation for Medicinal Chemistry (EFMC) as President for the past three years (2015-2017). On this occasion, I was asked to share with you some personal reflections on this period to facilitate the work of future EFMC history writers. The organisation of symposia is one of the major activities of EFMC to contribute to the advancement of the science of medicinal chemistry. The EFMC-ISMC is our flagship meeting and I experienced from many contacts worldwide that it is considered as THE best international symposium on medicinal chemistry. We should cherish this and work hard to keep it at this high level. In 2016 we had an outstanding EFMC-ISMC in Manchester from which I will always remember new and successful initiatives such as the plenary first-time disclosure lectures and the organisation of a public event. A new and in my opinion important initiative was the decision to increase the impact of the EFMC council on the EFMCISMC program. In Manchester, the council members proposed and selected 5 sessions that will be part of the EFMC-ISMC 2018 in Ljubljana. I have full confidence that the future symposia which were selected to be in Ljubljana (2018), Basel (2020) and Nice (2022) will reach and even exceed the standards we are used to. After an initial and highly successful round of Advances in Synthetic and Medicinal Chemistry symposia in Russia and Ukraine, we decided to start traveling across Europe in collaboration with Chembridge, the local NAO and LDOrganisation. This took a very promising start at the Weizmann Institute in Rehovot in 2015 and turned into a big success in Vienna in 2017. Participants unanimously informed me that they appreciate the mix of high level organic and medicinal chemistry, and I would recommend to keep this special focus for the future EFMCASMC’s. We decided to change the name of our Frontiers symposium to the ACSMEDI-EFMC Medicinal Chemistry Frontiers symposium to avoid confusion with another existing symposium. This symposium took place in Antwerp in 2015 and Philadelphia in 2017 and focuses alternatingly on the science of a certain region in Europe and the USA. It was very rewarding to me that the Frontiers 2015, hosted at my university in Antwerp, a joint organisation between the NAO’s from Belgium and the Netherlands, turned into a successful event both in terms of quality of the program and a record number of participants. The decision to start with a Young Medicinal Chemist Symposium in 2014 in Lisbon was certainly one of the best decisions of the recent past. I participated in the EFMC-YMCS symposia in Antwerp (2015), Manchester (2016) and Vienna (2017) and experienced a vibrant, passionate, young community bringing their scientific achievements and building networks. This gives me full trust in a brilliant future for our scientific discipline. A bit less young in age but with the same enthusiasm, Henk Timmerman organises each year a highly focused short course in Oegstgeest, which is always extremely well perceived by all participants. The field of medicinal chemistry has always been international, and certainly with the rapid increasing international mobility of researchers and companies, a strong embedding of EFMC in the international environment is very important. In the recent past, we reinforced existing collaborations and established novel collaborations with sister societies worldwide by signing agreements. Our longstanding and strong collaboration with the medicinal chemistry division of the American Chemical Society (ACSMEDI) was formalised by signing a memorandum in 2015. Next to a fruitful collaboration with the Asian Federation for Medicinal Chemistry (AFMC), we entered into a new agreement with the Chinese Pharmaceutical Association in 2016. We also signed MoU’s with South Africa, Brazil and India. Obviously, we were also working to strengthen the position of EFMC in Europe. The council unanimously approved in 2016 to become a supporting member of EuCheMS. This decision ensures that EFMC is an important partner in the broad field of chemistry in Europe and gives us a much better access to the European Parliament and Commission to influence science policy. A first result of this was the organisation of a STOA

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5 EFMC YEARBOOK 2018 working breakfast on solving antimicrobial resistance at the European Parliament in Brussels on April 28, 2016. By inviting Prof. Klaus Bock, vicepresident of the European Research Council (ERC) to the EFMC-ISMC 2016 in Manchester, I was able to discuss with him the absence of medicinal chemistry in the panel structure of ERC. In future ERC programmes, medicinal chemistry will now be visible which should ensure better access of medicinal chemists to ERC grant money. Another objective was to raise the visibility and recognition of medicinal chemistry, both within our community and the general public. We organised press conferences in Antwerp (2015) and Manchester (2016), but we must admit with limited success. Attracting the general press to a medicinal chemistry event seems not to be easy, and we therefore decided to stop this initiative. On the other hand, the public event in Manchester and the video competition on “Why Medicinal Chemistry?” were quite successful. We reshaped our communication strategy and converted the newsletter MedChemWatch to an electronic version. EFMC also became active on social media. A Twitter account and LinkedIn group were established and recently also a Facebook group was started. All these initiatives generated quite some interest in the medicinal chemistry field, but it is now important that a group of young and highly motivated volunteers will start feeding and maturing our social media efforts. The three major EFMC Awards continue to reward well established scientists, but as importantly the Prizes for Young Medicinal Chemists in Academia and Industry are now well consolidated. Several prize winners told me that this recognition made a significant difference and boosted their careers, demonstrating the importance of this initiative. Last but not least, I am convinced that history will learn that the decision taken in Vienna in 2017 to integrate chemical biology within the scope of EFMC is extremely important. We had long discussions on the fact if there is a difference between medicinal chemistry and chemical biology, and whether it was necessary that a new field such as chemical biology was established. But many scientists call themselves chemical biologists, new chemical biology journals were started and many universities and pharma companies have research groups on chemical biology. So, we cannot deny that the field is there. The only possible conclusion that EFMC could make is that medicinal chemists and chemical biologists share much more than what differentiates them. We all design and synthesize novel chemical molecules to influence biological, physiological and pathophysiological systems. Some are used as tool compounds in chemical biology, others will eventually lead to drug candidates and drugs on the market. It is my personal belief that EFMC should approach the field of chemical biology such that they feel included and comfortable in our federation. If EFMC does this well, it will offer new opportunities, but if it is done wrong, it might pose a threat to our society. Finally, I would like to take a moment to thank all the people that I collaborated with during the past years. Many of you became good colleagues and even friends. I hope to see many of you in the coming years at one or another EFMC event. I would like to thank especially all executive committee, working group and council members. Of course, I collaborated more intensively with a smaller group of people during the past 9 years. Starting in 2009 as EFMC Secretary and continuing the last three years as President, we had weekly Skype calls on Wednesday morning to discuss and organize the daily EFMC business. This was always done in an open and constructive spirit with a high level of engagement. Therefore, a special word of thanks to Gerhard Ecker, Uli Stilz, Jordi Gracia, Anders Karlén, Yves Auberson, Ly Differding, Nele Coulier and Brieuc Matagne. I have full trust that our beautiful federation is in good hands with Yves as next President and I wish him and all of you the very best for the coming years. I served EFMC with enormous pleasure and will always cherish the many great memories. With my very best personal regards, Koen Augustyns EFMC Past President December 2017

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EFMC YEARBOOK 2018 Table of Contents EFMC Presentation Editorial Reflection on 2015-2017 Table of Contents Sponsors Corporate Members Executive Committee Council Advisory Board EFMC Framework MedChemWatch - Website - Social Media EFMC Objectives Report EFMC-ASMC 2017 Report EFMC-YMCS 2017 EFMC Awards EFMC Prizes Calendar of Events EFMC Short Course National Adhering Organisations Austria Belgium Croatia Denmark Finland France Germany Greece Hungary Israel Italy Latvia The Netherlands Poland Portugal Russia Serbia Slovenia Spain Sweden Switzerland Turkey United Kingdom Directory of Companies Directory of Companies 1 4 7 8 8 9 10 11 12 14 15 17 21 22 24 28 39 41 42 44 45 46 47 48 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 65 69 7 Medicinal Chemistry in Europe, the Yearbook of the European Federation for Medicinal Chemistry is published by: LD Organisation sprl Scientific Conference Producers Rue Michel de Ghelderode 33/2 - BE-1348 Louvain-la-Neuve, Belgium Tel: +32 10 45 47 77 - Fax: +32 10 45 97 19 administration@efmc.info Reproduction: All items published in this directory are protected by copyright. Reproduction by reprint, photocopy, microfilm or any other process is not allowed without the prior written permission of the publisher. www.efmc.info

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Sponsors 8 PCroermpiourmateSpSopnosnosrors CHEMBRIDGE CORPORATION Corporate Members Premium Sponsors are CROs, Service Providers, Publishers that directly sponsor EFMC activities through major financial contributions. Their contribution helps the EFMC towards its main objective of developing a strong Medicinal Chemistry community in Europe that is wellequipped for the challenges of the future and enables the discovery of innovative new medicines for patients. EFMC offers any company involved in life sciences the opportunity to become an official corporate member. Corporate membership will help EFMC with its objective of advancing the science of medicinal chemistry and can be achieved in several ways: - By sponsoring an EFMC International Symposium with a minimum of €10 000 - By sponsoring an official EFMC Award - By paying an annual fee of € 2 000 to EFMC Companies interested in becoming a corporate member should contact the Administrative Secretariat at administration@efmc.info BAYER NAUTA FOUNDATION F.HOFFMANN-LA ROCHE BOEHRINGER INGELHEIM NOVARTIS SERVIER JANSSEN R&D PFIZER UCB MERCK PROUS INSTITUTE

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EC Executive Committee 9 EFMC YEARBOOK 2018 The Executive Committee (EC) consists of seven members: the President, the President Elect or the Past President, the Secretary, the Treasurer and three additional members. All members of the EC, except the President and the Past President, are elected by secret ballot by the Council during a meeting of the Council. After a term of one year, the President Elect will automatically become President. The members of the EC are not delegates of their respective countries. All details about the election process can be found in the statutes of the EFMC on the EFMC official website: www.efmc.info President Past President Secretary Treasurer Member Member Dr Yves P. AUBERSON Novartis Global Discovery Chemistry, WKL-136.6.82 Klybeckstrasse 141 - Basel Switzerland Tel: +41-795939101 Email: yves.auberson@novartis.com Prof. Dr Koen AUGUSTYNS University of Antwerp Medicinal Chemistry Campus Drie Eiken - Building A, Room 2.07 Universiteitsplein 1 - 2610 Antwerpen Belgium Tel: +32-3-265-27-17 - Fax: +32-3-265-27-39 Email: Koen.Augustyns@uantwerpen.be Prof. Dr Anders KARLÉN Uppsala University Department of Medicinal Chemistry BMC Box 574 – Uppsala Sweden Tel : +46-701679177 – Fax: +46-184714474 Email : anders.karlen@orgfarm.uu.se Dr Pascal GEORGE Independent Scientific Expert & Adviser 11, Route de Rochefort 78730 Longvilliers France Tel: +33 673683384 Email: george.pascal@wanadoo.fr Prof. Dr Rui MOREIRA University of Lisbon – Faculty of Pharmacy Av. Prof. Gama Pinto - 1649-019 Lisbon Portugal Tel : +351-217946477 – Fax : +351-217946470 Email : rmoreira@ff.ul.pt Dr Antoni TORRENS Esteve R&D Center Parc Científic de Barcelona, Baldiri i Reixach 4, Barcelona, Spain Tel : +34-934466000 Email : atorrens@esteve.es Member Activities Dr Matthew TOZER Consultant Cambridge United Kingdom Email : matttozer@hotmail.com The current affairs of the Federation are handled by the EC. Among its members, the EC will assign the responsibilities of International Liaison, Communication and Planning.

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Council 10 Council The Council consists of the members of the EC and one delegate of each Adhering Organisation. According to the statutes, the voting rights are allotted according to the following rules: members of the EC: 1 vote, countries with up to 99 members: 2 votes, countries with 100-199 members: 3 votes, countries with 200-399 members: 4 votes, countries with 400-599 members: 5 votes, countries with 600-899 members: 6 votes, countries with more than 899 members: 7 votes. As for countries with more than one Adhering Organisation, votes will be proportionally distributed among them, taking into a resulting number will be rounded off to the closest digit. Dr David ALKER David Alker Associates - The Biological and Medicinal Chemistry Sector (BMCS) of the Royal Society of Chemistry (RSC), United Kingdom Dr Yves P. Auberson Novartis Institutes for BioMedical Research, Switzerland – EFMC Executive Committee Prof. Dr Koen AUGUSTYNS University of Antwerp, Belgium - EFMC Executive Committee Prof. Dr Sergey BACHURIN Institute of Physiologically Active Compounds - The D.I. Mendeleev Russian Chemical Society, Medicinal Chemistry Section, Russia Prof. Dr Ayla BALKAN Hacettepe University, Turkish Association of Medicinal and Pharmaceutical Chemistry, Turkey Prof. Dr Bernd CLEMENT Kiel University - German Pharmaceutical Society, Section of Pharmaceutical/Medicinal Chemistry (DPhG), Germany Prof. Dr Gabriele COSTANTINO Università degli Studi di Parma Division of Medicinal Chemistry of the Italian Chemical Society, Italy Prof. Dr Gunars DUBURS Latvian Institute of Organic Synthesis - Latvian Association for Medicinal Chemistry, Latvia Dr Vesna GABELICA MARKOVIC Croatian Chemical Society, Medicinal Chemistry Section, Croatia Prof. Dr Pilar GOYA LAZA Instituto de Quimica Medica - Sociedad Española de Química Terapéutica, Spain Dr Pascal GEORGE Independent Scientific Expert & Adviser, France – EFMC Executive Committee Dr Georg JAESCHKE F. Hoffmann-La Roche - Division for Medicinal Chemistry & Chemical Biology (DMCCB), Switzerland Dr Annika JENMALM JENSEN Karolinska Institutet, Swedish Academy of Pharmaceutical Sciences, Sweden Prof. Dr Anders KARLÉN Uppsala University, Sweden - EFMC Executive Committee Prof. Dr György Miklós KESERU Hungarian Academy of Sciences, Organic and Medicinal Chemistry Division (OMCD) of the Hungarian Chemical Society (HCS), Hungary Prof. Dr Katarzyna KIEC-KONONOWICZ Jagiellonian University - Polish Society of Medicinal Chemistry, Poland Prof. Dr Danijel KIKELJ University of Ljubljana - Section for Medicinal Chemistry of the Slovenian Pharmaceutical Society, Slovenia Prof. Dr Thierry LANGER University of Vienna – Austrian Chemical Society, Medicinal Chemistry, Austria Dr Matilde MARQUES University of Lisbon - Division of Medicinal Chemistry of the Portuguese Chemical Society, Portugal Prof. Dr Emmanuel MIKROS Hellenic Society of Medicinal Chemistry, Greece Dr Peter MOLENVELD Mercachem - Section Medicinal Chemistry, Royal Netherlands Chemical Society (KNCV), The Netherlands Prof. Dr Rui MOREIRA University of Lisbon, Portugal - EFMC Executive Committee Prof. Dr Igor OPSENICA University of Belgrade, Division of Medicinal Chemistry of the Serbian Chemical Society, Serbia Dr Laurent PROVINS UCB, Société Royale de Chimie (SRC), Medicinal Chemistry Division, Belgium Prof. Dr Jarkko RAUTIO University of Eastern Finland, Finnish Pharmaceutical Society, Finland Prof. Dr Janos SAPI University of Reims-Champagne-Ardenne – French Medicinal Chemical Society, France Prof. Dr Trond ULVEN University of Southern Denmark - The Danish Society for Medicinal Chemistry and Chemical Biology, Denmark Dr Antoni TORRENS Esteve, Spain – EFMC Executive Committee Dr Matthew TOZER Consultant, United Kingdom – EFMC Executive Committee Prof. Dr Serge VAN CALENBERGH Ghent University - Medicinal and Bioorganic Chemistry Division of Royal Flemish Chemical Society (KVCV), Belgium Dr Franz VON NUSSBAUM Bayer Pharma AG - Division of Medicinal Chemistry of the German Chemical Society (GDCh), Germany Dr Eylon YAVIN The Hebrew University of Jerusalem, The Medicinal Chemistry Section of the Israel Chemical Society, Israel

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EFMC YEARBOOK 2018 AB Advisory Board 11 Current Board Membership: • Koen AUGUSTYNS – AB Chair University of Antwerp, Belgium • Annette G. BECK-SICKINGER Leipzig University, Germany • Karin BRINER Novartis, USA • Stuart CONWAY University of Oxford, United Kingdom • François DIEDERICH ETH Zurich, Switzerland • Frank LEEMHUIS Mercachem, The Netherlands • Ulrich SCHUBERT Vienna University of Technology, Austria The Advisory Board is an EFMC consulting body for the executive committee assisting in assessing the Federation’s strategic goals. The tasks of the AB consist of: - advising on EFMC policy related matters internally and externally - proposing novel scientific or political initiatives to the Executive Committee - proposing strategies how to increase awareness of Medicinal Chemistry and support of the community in Europe - proposing strategies how to affect and interact with stakeholders in Europe The Advisory Board is composed of eminent scientists in the life sciences and medicinal chemistry and is chaired by the past president.

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