The discovery of VX-745: A novel and selective p38α kinase inhibitor
The synthesis of novel, selective, orally active 2,5-disubstituted 6H-pyrimido[1,6-b]pyridazin-6-one p38α inhibitors is described. Application of structural information from enzyme-ligand complexes guided the selection of screening compounds, leading to t
Duffy, John P.,Harrington, Edmund M.,Salituro, Francesco G.,Cochran, John E.,Green, Jeremy,Gao, Huai,Bemis, Guy W.,Evindar, Ghotas,Galullo, Vincent P.,Ford, Pamella J.,Germann, Ursula A.,Wilson, Keith P.,Bellon, Steven F.,Chen, Guanging,Taslimi, Paul,Jones, Peter,Huang, Cassey,Pazhanisamy,Wang, Yow-Ming,Murcko, Mark A.,Su, Michael S.S.
supporting information; experimental part
p. 758 - 763
(2011/12/03)
An improved synthesis of 5-(2,6-dichlorophenyl)-2-(phenylthio)-6H- pyrimido[1,6-b]pyridazin-6-one (a VX-745 analog)
An improved procedure for the synthesis an analog of the p38 inhibitor compound VX-745 is reported.
Treu, Matthias,Jordis, Ulrich,Lee, Ving J.
p. 959 - 963
(2007/10/03)
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