Jan Heeres is Awarded
the 2008 IUPAC-Richter Prize
2008 IUPAC-Richter Prize in Medicinal Chemistry has been awarded to
Jan Heeres, formerly of the Centrum for Molecular Design and
Janssen Pharmaceutica, Beerse, Belgium.
Heeres received this award in recognition of his outstanding medicinal
chemistry contributions to new drug discovery while at Janssen Pharmaceutica.
In particular for the discovery of ketoconazole, the first orally active
broad-spectrum imidazole antimycotic, and for various other very important
antifungal azole drugs over a period of twenty years, such as econazole,
miconazole, isoconazole, carnidazole, azanocazole, parconazole, terconazole,
propiconazole, itraconazole and saperconazole.
He has continued to invent new drugs. One of them is mitratapide, an
inhibitor of MTP (the microsomal triglyceride transfer protein) so that
it is useful as a lipid lowering agent. The compound was derived from
itraconazole and is now in use for the treatment of obese dogs.
The IUPAC-Richter Prize comprising a plaque and a cheque for USD 10,000,
will be presented on 18 June 2008 at the American Chemical Society 31st
National Medicinal Chemistry Symposium in Pittsburgh, Pennsylvania,
USA. The plaque is signed by Professor Jung-Il Jin, President of IUPAC,
Erik Bogsch, Chief Executive Officer of Gedeon Richter Plc. and Prof.
Robin Ganellin, Chair of the IUPAC-Richter Prize selection committee.
Jan Heeres studied chemistry in the State University of Gröningen,
Gröningen, The Netherlands, and received a Master's degree in 1965,
supervised by Dr. (now Prof.) A.M. Van Leusen in the department of Profs.
H. Wijnberg and J. Strating. He then joined the team of Dr E.F. Godefroi
at Janssen Pharmaceutica, Beerse, Belgium, to work on azole chemistry.
During the next two years this work produced the first of the substituted-imidazole
antifungal drugs, miconazole and econazole. From 1971 onwards Jan Heeres
was responsible for elaborating on these structures, incorporating the
dioxolane ring and introducing a variety of side chains. This work led
to ketoconazole, and was followed by various other improved drugs as
listed above over the following 10 years.
His research continued in various areas such as anticancer agents,
anti-epileptics, lipid-lowering agents and, in 1996, he joined Paul
Janssen's Centrum for Molecular Design. Here he was involved in structure-assisted
drug design for antiviral drugs against HIV. This work produced dapivirine,
etravirine and rilpivirine, non-nucleoside reverse transcriptase inhibitors.
Etravirine has recently been approved by the FDA and has been launched
by Tibotec (a subsidiary of Johnson and Johnson) in the US marketplace.
Meanwhile rilpivirine has successfully completed phase II clinical trials.
In 1982 Jan Heeres was awarded the J&J medal in recognition of
his role in the discovery of ketoconazole and in 2002 was made Distinguished
> Back to IUPAC-Richter
<prize announcement published in
2008, p. 20 >