MedChemWatch
Monthly Newsletter September 2015

IN MEMORIAM Professor Camille-Georges WERMUTH

Professor Camille-Georges WERMUTH passed away in Strasbourg (France) at the age of 82 years on Tuesday, September 22nd 2015.

Camille-Georges Wermuth was Emeritus Professor of organic and medicinal chemistry at the Faculty of Pharmacy of Strasbourg University and Founder of Prestwick Chemical, a medium-size company established in Illkirch (France).

C.G Wermuth studied pharmacy and later specialized in chemistry at the Strasbourg University (with Professors J. Schreiber and G. Ourisson); he obtained his PhD in organic chemistry entitled "Directed aldol condensation between enolisable aldehydes and alpha-ketocarboxylic acids" (1964). He became interested in medicinal chemistry during his two-year military service in the Research Center of the French Navy (“Centre d'Études Physiobiologiques Appliquées à la Marine") in Toulon, directed by Dr Henri Laborit, the inventor of artificial hibernation and of chlorpromazine. Dr Wermuth has been Professor of organic chemistry and medicinal chemistry at the Faculty of Pharmacy, Strasbourg University for more than 33 years (1969-2002) and in parallel has been the Director of the “Molecular Pharmacochemistry CNRS Research Unit” for 27 years. The research activity of his CNRS group, gathering skilled collaborators in synthetic organic chemistry, medicinal chemistry and computer modeling, focused on neuro-psychiatric pathologies leading to the development of a new psychotropic drug, minaprine (Cantor®) marketed in Europe since 1980.

Professor Wermuth’s main research themes concerned the chemistry and pharmacology of pyridazine derivatives. He was interested in the 3-aminopyridazine pharmacophore possessing an impressive variety of biological activities: such as antidepressant and anticonvulsant derivatives; inhibitors of enzymes (mono-amine-oxidases, phosphodiesterases and acetylcholinesterase) or neuroreceptor ligands (GABA-A antagonists, 5-HT3 antagonists, dopaminergic and muscarinic agonists). In collaboration with the pharmaceutical company Sanofi, he developed potent antagonists of the 41 amino-acid neuropeptide CRF (corticotrophin-releasing factor) which regulates the release of ACTH and thus the synthesis of corticoids in the adrenal glands. He successfully developed selective ligands of the newly discovered dopamine D3 receptor. After a three-year exploratory phase, this research has led to nanomolar partial agonists for the treatment of the cocaine-withdrawal syndrome.

Professor Wermuth was a prolific scientific author with more than 250 scientific papers and 60 patents. He is co-author or editor of several book-chapters, and books. His famous book, entitled "The Practice of Medicinal Chemistry", originated from the acknowledge that the majority of medicinal chemists working in pharmaceutical industry has strong organic synthetic chemistry background with little experience in medicinal chemistry. This manual considered « The Bible » by many medicinal chemists has a great success, it was translated into several languages wherof Japanese, and the 4th improved edition was just released.

The outstanding scientific career of Professor Wermuth has been recognized by a couple of awards, and prizes. He obtained the Charles Mentzer Prize of the Société de Chimie Thérapeutique (SCT) in 1984, the Léon Velluz Prize of the French Academy of Science (1995), the Prix de l’Ordre des Pharmaciens (1998) from the French Academy of Pharmacy and the Carl Mannich Prize of the German Pharmaceutical Society in 2000. The European Federation for Medicinal Chemistry (EFMC) acknowledged and recognized Professor  Wermuth’s  accomplishments  in  the  field   of   medicinal chemistry   by   attributing   him The Nauta Award for Pharmacochemistry in 2010.

Professor Wermuth has been President of the Medicinal Chemistry Section of the International Union of Pure and Applied Chemistry (IUPAC) from 1988 to 1992 and from January 1998 to January 2000 he was President of the IUPAC Division on Chemistry and Human Health.

Professor Wermuth will long be remembered as an outstanding medicinal chemist, an excellent mentor, a highly appreciated teacher, a wonderful colleague and friend.

Société de Chimie Thérapeutique (SCT)


ACADEMIC DRUG DISCOVERY, REPORT ON A PANEL DISCUSSION

At the Lisbon EFMC-ISMC a discussion on the issue of the position of medicinal chemistry in academia emerged. There was insufficient time to discuss the topic thoroughly so a session on “Academic Drug Discovery” was organized during the Frontiers in Medicinal Chemistry Symposium held in Antwerp in September 2015. Here we report on this special event.

Two initial lectures exemplified the success of recent medicinal chemistry programmes in academia. The first by Professor Roberto Pellicciari (University of Perugia) described the successful transfer of an academic finding towards therapeutic use: the application of obeticholic acid for the treatment of primary liver cirrhosis. Next Professor Iwan de Esch (VU University Amsterdam) focused his lecture on public-private partnerships and explained his personal experience combining entrepreneurial initiatives such as the foundation of a spin-off company with the inherent demands of an academic position. He put an emphasis on the rapidly changing landscape in the pharmaceutical sciences, changes which have important consequences for academic research teams.

Subsequently the two lecturers joined the discussion panel which was completed with Professor Christa Müller (University of Bonn) and Professor Chas Bountra (University of Oxford) and was chaired by Professor Henk Timmerman (VU University Amsterdam). All four panellists  were asked to briefly present their opinion on the following questions: ‘Is there a place for medicinal chemistry at universities? And if not, why not? If the answer is yes, what would such a place be like?’ He also invited the panellists to discuss the question “what would then be the contribution of academic scientists?”.

The four panellists agreed that there is definitely a place and an important role for medicinal chemistry at universities. Bountra was quite firm: ‘the need for more medicinal chemistry in academia will increase substantially’. The question about the objective of medicinal chemistry in academia generated more discussion. Müller strongly defended that academic and industrial drug research should not remain separated worlds, there should be extensive exchange and mutual fertilisation. The panellists agreed on the importance of teaching and training new medicinal chemists, which consumes a substantial amount of time. As for the topic ’which type of research?’ all panellists agreed that basic research should be a first priority. Bountra was more precise stating that target finding should be at the top of the list. Finally, it was noted that nowadays most academic institutions are involved in private-public partnerships, and this situation leads naturally to the inclusion of applied research into the academic programmes.

The session was well attended and though it was placed at the end of the day, almost all participants remained as an active audience till the conclusion of the session. There was a general opinion that the remarks at the Lisbon meeting which led to the current exchange of views, had not been justified at all. Clearly medicinal chemistry as defined in the recently published position paper of the EFMC has a solid position in academia and there are several good reasons to further strengthen it.

 

NEWS FROM THE SECTION OF MEDICINAL CHEMISTRY, ROYAL NETHERLANDS CHEMICAL SOCIETY (KNCV)

- Prof. Dr Roland Pieters becomes the new President
- Dr Peter Molenveld follows up Prof. Dr Henk Timmerman in EFMC Council

  • Prof. Dr. Roland Pieters as New President

End of March 2015, Prof. Dr. Roland Pieters of Utrecht University was installed as new president of the Section Medicinal Chemistry of the Royal Netherlands Chemical Society (KNCV). He succeeds Prof. Dr. Ad IJzerman of Leiden University, who chaired the committee for 8 years. Roland Pieters was already member of the committee as of 2012 and was a board member of the Dutch organic chemistry section as well. He is heading the department Medicinal Chemistry & Chemical Biology where his research is focusing on the design and synthesis of multivalent bioactive compounds, in particular carbohydrates, and on protein-carbohydrate interactions

  • Dr Peter Molenveld Follows Up Prof. Dr Henk Timmerman in EFMC Council

Last month, Prof. Dr Henk Timmerman stopped as the Dutch representative in the EFMC Council. Henk Timmerman has served many (inter)national positions, amongst them the president of the Royal Netherlands Chemical Society, the Netherlands Society for Pharmaceutical Research and the EFMC, respectively. After his retirement from the Free University Amsterdam in 2002 he remained active in the field and in the EFMC in particular. He will continue as advisor of the Section Medicinal Chemistry of the Royal Netherlands Chemical Society and the EFMC as well. Dr Peter Molenveld, the secretary of the Section Medicinal Chemistry as of 2012, is the new Dutch representative in the EFMC Council. He is an organic chemist by education and is employed as Director of Chemistry at the CRO Mercachem in Nijmegen

THE EXPANDING TOOLBOX OF MEDICINAL CHEMISTRY: FROM CHEMICAL BIOLOGY TO CLINICAL APPLICATIONS. DIJON, FRANCE - OCTOBER 16, 2015

This symposium, jointly organised by the Société de Chimie Thérapeutique (SCT) and the Division of Medicinal Chemistry & Chemical Biology (DMCCB) of the Swiss Chemical Society, will discuss significant advances that are part of the expanding scope of Medicinal Chemistry. A panel of experts will highlight these developments in the areas of chemical biology, metabolite pattern optimization, analytics and clinical imaging tracers with specific examples.

Until recently, Medicinal Chemistry has mostly focused on the exploration of biologically active molecules and their optimization towards pharmaceutical applications. There is, however, an increasing need for medicinal chemists to contribute to the drug discovery and development process more broadly, in order to enable the development of truly improved medicines. This includes providing tools for therapeutic target identification and validation, to explore therapeutic and pathological mechanisms, or even support clinical trials.

Find out more on www.sct-dmccb2015.org

NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (UK)

BMCS invites nominations for the sixth Capps Green Zomaya Memorial Award in medicinal or computational chemistry and announces:
- the 1st RSC/SCI Symposium on Fibrosis Disease and Medicinal Chemistry on November 10th in Slough, UK
- the 3rd RSC/SCI Symposium on Continuous Flow Technology on 14th to 16th March 2016 in Cambridge, UK

THE CAPPS GREEN ZOMAYA MEMORIAL AWARD 2016 – OPEN TO INTERNATIONAL NOMINATIONS:  

The Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is pleased to invite nominations for the sixth Capps Green Zomaya Memorial Award in medicinal or computational chemistry. The Award will be given to the individual judged to have made an important contribution to the discovery or development of new medicines. Nominations are invited for candidates, up to the age of 40, working in UK or international laboratories (candidates over the age of 40, who have taken career breaks, will be considered). A Royal Society of Chemistry commemorative medal and certificate will be awarded to accompany the prize of £2000.

Nominations should be submitted no later than 31st October 2015 and sent to Maggi Churchouse at RSC-BMCS Secretariat, 3 East Barn, Market Weston Road, Thelnetham, Diss IP22 1JJ, UK or maggi@maggichurchouseevents.co.uk

FIND FIBROSIS FASCINATING? WHY NOT COME TO THE 1ST RSC / SCI SYMPOSIUM ON FIBROSIS DISEASE AND MEDICINAL CHEMISTRY: ON 10TH NOVEMBER 2015 AT THE UCB SITE IN SLOUGH, UK

Fibrosis disease is the result of a dysregulated wound healing process and is responsible for considerable patient mortality affecting multiple organs in diseases such as idiopathic pulmonary fibrosis (IPF), diabetic nephropathy, steatohepatitis and systemic sclerosis. Fibrosis disease pathology is often complex and this inaugural symposium on fibrosis will provide mechanistic insight and progress in medicinal chemistry and drug discovery from experts across the world

Late fees apply from 8th October

Websites:  www.maggichurchouseevents.co.uk/bmcs

http://www.rsc.org/events/detail/18629/1st-rsc-sci-symposium-on-fibrosis-disease-medicinal-chemistry-progress-from-biological-target-to-the-clinic

GO WITH THE FLOW? JOIN US AT THE THIRD RSC / SCI SYMPOSIUM ON CONTINUOUS FLOW TECHNOLOGY ON 14TH TO 16TH MARCH 2016, CAMBRIDGE, UK

This three-day Conference on Continuous Flow Technology is organised by both SCI and RSC, combining previously successful 1 and 2 day symposia. This reflects the advances made with continuous flow technology over recent years and the impact it is making right across the chemicals industry spanning discovery applications, process development advances and value for commercial manufacture of fine and speciality chemicals. To reflect the mix of interests and applications across the chemistry community, the symposium is structured as two back to back events with options for attending two consecutive days or all three

Closing date for oral abstracts is 30th September
Closing date for poster abstracts is 30th November

Website: http://www.rsc.org/events/detail/18985/continuous-flow-technology-iii

 

 

EFMC ORGANISED EVENTS

September 6-7, 2018
Ljubljana, Slovenia
5th EFMC Young Medicinal Chemist Symposium (EFMC-YMCS 2018)

EFMC SPONSORED EVENTS

January 28 - February 1, 2018
St Anton, Austria
1st Alpine Conference on Medicinal and Synthetic Chemistry

JOB PORTAL

Early Stage Researcher in Medicinal Chemistry, University of Basel (UNIBAS), University of Utrecht (UU), PamGene: Department of Pharmaceutical Sciences (UNIBAS), Department of Chemical Biology & Drug Discovery (UU), Basel, Utrecht, 's-Hertogenbosch, Switzerland
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Early Stage Researcher in Medicinal Chemistry, University of Ljubljana (UL), University of Utrecht (UU), PamGene: Faculty of Pharmacy, Chair of Pharmaceutical Chemistry (UL), Department of Chemical Biology & Drug Discovery (UU), Ljubljana, Utrecht, 's-Hertogenbosch, Slovenia
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Early Stage Researcher in Medicinal Chemistry, University of Utrecht (UU), University of Ljubljana (UL), PamGene: Department of Chemical Biology & Drug Discovery (UU), Faculty of Pharmacy, Chair of Pharmaceutical Chemistry (UL), Utrecht, Ljubljana, 's-Hertogenbosch, The Netherlands
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Early Stage Researcher in Medicinal Chemistry, University of Basel (UNIBAS), University of Ljubljana (UL): Department of Pharmaceutical Sciences (UNIBAS), Faculty of Pharmacy, Chair of Pharmaceutical Chemistry (UL), Basel, Ljubljana, Switzerland
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Early Stage Researcher in Medicinal Chemistry, University of Ljubljana (UL), Lund University (ULUND), SARomics, Red Glead: Faculty of Pharmacy, Chair of Pharmaceutical Chemistry (UL), Department of Chemistry (ULUND), Ljubljana, Slovenia
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Early Stage Researcher in Medicinal Chemistry, Università degli Studi di Milano (UMIL), Universiteit Utrecht (UU), PamGene: Chemistry (UMIL), Department of Chemical Biology & Drug Discovery (UU), Milano, Utrecht, 's-Hertogenbosch, Italy
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Early Stage Researcher in Medicinal Chemistry, Università degli Studi di Milano (UMIL), Université Grenoble Alpes (UGA), Centre national de la recherche scientifique (CNRS-Glycopedia): Chemistry (UMIL), CERMAV (UGA), Milano, Gières, Grenoble, Italy
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Early Stage Researcher in Medicinal Chemistry, Université Grenoble Alpes (UGA), Universiteit Utrecht (UU), PamGene: CERMAV (UGA), Department of Chenical Biology & Drug Discovery (UU), Gières, Utrecht, 's-Hertogenbosch, France
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Early Stage Researcher in Medicinal Chemistry, Universiteit Utrecht (UU), Université Grenoble Alpes (UGA), Centre national de la recherche scientifique (CNRS): Department of Chemical Biology & Drug Discovery (UU), CERMAV (UGA), Utrecht, Gières, Grenoble, The Netherlands 
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Early Stage Researcher in Medicinal Chemistry Université Grenoble Alpes (UGA), Università degli Studi di Milano (UMIL), Centre national de la recherche scientifique (CNRS) : CERMAV (UGA), Department of Chemistry (UMIL), Gières, Milano, Grenoble, France
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Research / Senior Scientist Medicinal Chemistry, UCB: Medicinal Chemistry, Braine-L'Alleud, Belgium
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Principal Scientist Medicinal Chemistry, UCB: Medicinal Chemistry, Braine-L'Alleud, Belgium
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Medicinal / Synthetic Organic Chemists, Concept Life Sciences: Drug Discovery, Sandwich, Kent, United Kingdom
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