Novel Inhibitors of Inosine Monophosphate Dehydrogenase as Potential Anti-Cancer Drugs: A Patent Review (2002-2014)
Pp. 37-102 (66)
Riccardo Petrelli, Ilaria Torquati, Krzysztof Felczak, Daniel J. Wilson and Loredana Cappellacci
Inosine monophosphate dehydrogenase (IMPDH), an NAD-dependent
enzyme that controls de novo synthesis of guanine nucleotides, has received
considerable interest in recent years as an important target enzyme, not only for the
discovery of anticancer drugs, but also for antiviral, antiparasitic, and
immunosuppressive chemotherapy. The field of IMPDH inhibitor research is highly
important for providing potential therapeutics against a validated target for disease
intervention. This patent chapter examines the chemical structures and biological
activities of recently reported IMPDH inhibitors. Patent databases SciFinder and
Espacenet and Delphion were used to locate patent applications that were published
between January 2002 and November 2013, claiming chemical structures for use as
IMPDH inhibitors. From 2002 to 2014, around 64 primary patent applications have
claimed IMPDH inhibitors, which we analyzed by target and applicant. The level of
newly published patent applications covering IMPDH inhibitors remains high and a
diverse range of scaffolds has been claimed.
Anticancer, antimicrobial, anti-tubercular, antiviral, benzamide
riboside, chemotherapy, EICAR, immunosuppression, IMP-dehydrogenase,
IMPDH, inhibitor design, merimepodib (VX-497), mizoribine, mycophenolic
acid, mycophenolic mofetil, NAD analogs, NAD-based therapeutics, nicotinamide
adenine dinucleotide, ribavirin, tiazofurin.
School of Pharmacy, University of Camerino, via S. Agostino 1, 62032 Camerino (MC), Italy.