408365-87-7Relevant articles and documents
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR INHIBITORS
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, (2014/12/09)
Compounds of formula (Ι') that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
P2 pyridine N-oxide thrombin inhibitors: A novel peptidomimetic scaffold
Nantermet, Philippe G.,Burgey, Christopher S.,Robinson, Kyle A.,Pellicore, Janetta M.,Newton, Christina L.,Deng, James Z.,Selnick, Harold G.,Lewis, S. Dale,Lucas, Bobby J.,Krueger, Julie A.,Miller-Stein, Cynthia,White, Rebecca B.,Wong, Bradley,McMasters, Daniel R.,Wallace, Audrey A.,Lynch Jr., Joseph J.,Yan, Youwei,Chen, Zhongguo,Kuo, Lawrence,Gardell, Stephen J.,Shafer, Jules A.,Vacca, Joseph P.,Lyle, Terry A.
, p. 2771 - 2775 (2007/10/03)
In this study, we have demonstrated that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by a 2-aminopyridine N-oxide. As this peptidomimetic core is more resistant toward oxidative metabolism, it also overcomes the metabolic liability associated with the pyrazinones. An optimization study of the P 1 benzylamide delivered the potent thrombin inhibitor 21 (K i = 3.2 nM, 2xaPTT = 360 nM), which exhibited good plasma levels and half-life after oral dosing in the dog (Cmax = 2.6 μM, t 1/2 = 4.5 h).
