54884-19-4Relevant articles and documents
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4- oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases
Brown, Dearg S.,Cumming, John G.,Bethel, Paul,Finlayson, Jonathan,Gerhardt, Stefan,Nash, Ian,Pauptit, Richard A.,Pike, Kurt G.,Reid, Alan,Snelson, Wendy,Swallow, Steve,Thompson, Caroline
, p. 3879 - 3883 (2012/07/03)
A novel, potent and selective quinazolinone series of inhibitors of p38α MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clinical candidate N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin- 3(4H)-yl]benzamide (AZD6703). Optimisation was guided by understanding of the binding modes from X-ray crystallographic studies which showed a switch from DFG 'out' to DFG 'in' as the inhibitor size was reduced to improve overall properties.
PYRAZOLO-PYRIMIDINE ANILINE COMPOUNDS
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Page 35; 36, (2010/02/05)
Compounds having the formula (I), where all substituents are as defined herein, and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors.