- Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase
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Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38α kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position leading to analogs that were potent in human whole blood based cell assay as well as in a number of animal efficacy models for rheumatoid arthritis. Ultimately, we identified a clinical candidate from this substrate; SD-0006.
- Walker, John K.,Selness, Shaun R.,Devraj, Rajesh V.,Hepperle, Michael E.,Naing, Win,Shieh, Huey,Kurambail, Ravi,Yang, Syaulan,Flynn, Daniel L.,Benson, Alan G.,Messing, Dean M.,Dice, Tom,Kim, Tina,Lindmark,Monahan, Joseph B.,Portanova, Joseph
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scheme or table
p. 2634 - 2638
(2010/07/13)
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- Process for making substituted pyrazoles
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This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R3A, R3B, R3C, Y1, Y2, Y3, Y4, and Y5 are as defined in the specification.
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