408365-87-7Relevant academic research and scientific papers
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR INHIBITORS
-
Page/Page column 62; 63, (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.
INHIBITORS OF 11ΒΕΤΑ-HYDROXY STEROID DEHYDROGENASE TYPE 1 (11BETA-HSD1)
-
Page/Page column 32; 39-40, (2010/11/30)
The invention relates to sulfonamide compounds of formula (I) wherein A, B, R1and X1 to X3 have the meaning as cited in the description and the claims. For example A is biphenyl, B is 2-morpholin-4-yl-2-oxo-ethyl, R1 is H and X1 to X3 are CH. Said compounds are useful as 11β-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament.
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).
