1042170-76-2Relevant academic research and scientific papers
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor
Han, Yongxin,Belley, Michel,Bayly, Christopher I.,Colucci, John,Dufresne, Claude,Giroux, Andre,Lau, Cheuk K.,Leblanc, Yves,McKay, Daniel,Therien, Michel,Wilson, Marie-Claire,Skorey, Kathryn,Chan, Chi-Chung,Scapin, Giovana,Kennedy, Brian P.
, p. 3200 - 3205 (2008)
A series of quinoline/naphthalene-difluoromethylphosphonates were prepared and were found to be potent PTP1B inhibitors. Most of these compounds bearing polar functionalities or large lipophilic residues did not show appreciable oral bioavailability in rodents while small and less polar analogs displayed moderate to good oral bioavailability. The title compound was found to have the best overall potency and pharmacokinetic profile and was found to be efficacious in animal models of diabetes and cancer.
FUSED AROMATIC PTP-1B INHIBITORS
-
Page/Page column 31; 33, (2008/12/07)
The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
