30 No. 4
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Jan Heeres Awarded the 2008 IUPAC-Richter Prize
On 18 June, the 2008 IUPAC-Richter Prize in Medicinal Chemistry was awarded to Jan Heeres at the American Chemical Society 31st National Medicinal Chemistry Symposium in Pittsburgh, Pennsylvania, USA. Heeres, formerly of the Centrum for Molecular Design and Janssen Pharmaceutica, Beerse, Belgium, received a check for USD 10 000 and a plaque signed by Jung-Il Jin, president of IUPAC; Erik Bogsch, chief executive officer of Gedeon Richter Plc.; and Robin Ganellin, chair of the IUPAC-Richter Prize selection committee.
Heeres received the award in recognition of his outstanding medicinal chemistry contributions to new drug discovery while at Janssen Pharmaceutica. In particular, he was recognized for the discovery of ketoconazole, the first orally active broad-spectrum imidazole antimycotic, and for 20 years of discovering other important antifungal azole drugs, such as econazole, miconazole, isoconazole, carnidazole, azanocazole, parconazole, terconazole, propiconazole, itraconazole, and saperconazole.
|Jan Heeres (center) accepts the 2008 IUPAC-Richter Prize from Robin Ganellin (left) and Janos Fischer.
Heeres studied chemistry at the State University of Gröningen, The Netherlands, and received a Master’s degree in 1965. He then joined the team of E.F. Godefroi at Janssen Pharmaceutica 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.
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 USA. Meanwhile, rilpivirine has successfully completed phase II clinical trials.
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 Research Fellow.
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