85070-67-3Relevant articles and documents
New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
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Page/Page column 23, (2011/06/10)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to pharmaceutical compositions comprising them, and to their use in therapy.
NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS AND METHODS OF USE
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Page/Page column 74, (2008/06/13)
The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
A fluorine scan of the phenylamidinium needle of tricyclic thrombin inhibitors: Effects of fluorine substitution on pKa and binding affinity and evidence for intermolecular C-F...CN interactions
Olsen, Jacob,Seiler, Paul,Wagner, Bjoern,Fischer, Holger,Tschopp, Thomas,Obst-Sander, Ulrike,Banner, David W.,Kansy, Manfred,Mueller, Klaus,Diederich, Francois
, p. 1339 - 1352 (2007/10/03)
The H-atoms of the phenylamidinium needle of tricyclic thrombin inhibitors, which interacts with Asp189 at the bottom of the selectivity pocket S1 of the enzyme, were systematically exchanged with F-atoms in an attempt to improve the pharmacokinetic prope