1033909-28-2Relevant academic research and scientific papers
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase
Selness, Shaun R.,Devraj, Rajesh V.,Devadas, Balekudru,Walker, John K.,Boehm, Terri L.,Durley, Richard C.,Shieh, Huey,Xing, Li,Rucker, Paul V.,Jerome, Kevin D.,Benson, Alan G.,Marrufo, Laura D.,Madsen, Heather M.,Hitchcock, Jeff,Owen, Tom J.,Christie, Lance,Promo, Michele A.,Hickory, Brian S.,Alvira, Edgardo,Naing, Win,Blevis-Bal, Radhika,Messing, Dean,Yang, Jerry,Mao, Michael K.,Yalamanchili, Gopi,Vonder Embse, Richard,Hirsch, Jeffrey,Saabye, Matthew,Bonar, Sheri,Webb, Elizabeth,Anderson, Gary,Monahan, Joseph B.
, p. 4066 - 4071 (2011/08/02)
The synthesis and SAR studies of a novel N-aryl pyridinone class of p38 kinase inhibitors are described. Systematic structural modifications to the HTS lead, 5, led to the identification of (-)-4a as a clinical candidate for the treatment of inflammatory diseases. Additionally, the chiral synthesis and properties of (-)-4a are described.
PROCESSES FOR THE PREPARATION OF 3-(4-(2,4-DIFLUOROBENZYLOXY)-3-BROMO-6-METHYL-2-OXOPYRIDIN-1(2H)-YL)-N,4-DIMETHYLBENZAMIDE
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Page/Page column 31; 32; 34, (2008/12/06)
This invention is directed generally to processes for the preparation of compounds of Formula I: wherein R2, R3, R4, R5, X1, X2, X3, X4, X5, X6 a
PYRIDINONE PYRAZOLE UREA AND PYRIMIDINONE PYRAZOLE UREA DERIVATIVES
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Page/Page column 229, (2008/06/13)
This invention is directed generally to substituted pyridinone and pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygeπase activity. Such substituted pyridinone and pyrimidinone compounds include compounds generally corresponding in structure to the following formula: wherein Z, n, R1, R2a, R2b, R2c, R2d, R2e, R3a, R3b R3c, R3d, R4, R5, R6, R7a, R7b, R7c, R7d and R7e are as defined in this specification. This invention also is directed to compositions of such substituted pyridinones and pyrimidinones (particularly pharmaceutical compositions), and methods for treating disorders (typically pathological disorders) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
