Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases
The design, synthesis and structure-activity relationships of a novel series of 2,4-diamino-5-cyclopropyl pyrimidines is described. Starting from BX795, originally reported to be a potent inhibitor of PDK1, we have developed compounds with improved selectivity and drug-like properties. These compounds have been evaluated in a range of cellular and in vivo assays, enabling us to probe the putative role of the TBK1/IKKε pathway in inflammatory diseases.
McIver, Edward G.,Bryans, Justin,Birchall, Kristian,Chugh, Jasveen,Drake, Thomas,Lewis, Stephen J.,Osborne, Joanne,Smiljanic-Hurley, Ela,Tsang, William,Kamal, Ahmad,Levy, Alison,Newman, Michelle,Taylor, Debra,Arthur, J. Simon C.,Clark, Kristopher,Cohen, Philip
p. 7169 - 7173,5
(2012/12/12)
CHK-, PDK- AND AKT-INHIBITORY PYRIMIDINES, THEIR PRODUCTION AND USE AS PHARMACEUTICAL AGENTS
This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.
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Page 158; 228
(2008/06/13)
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