250681-75-5Relevant academic research and scientific papers
PYRIMIDINE DERIVATIVES
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Page 26, (2010/02/10)
The invention concerns pyrimidine derivatives of Formula (I) wherein m is 0-3 and each Ris a group such as hydroxy, halogeno, trifluoromethyl and cyano; Ris hydrogen, halogeno or (1-6C)alkyl; n is 0-2 and each Ris a group such as hydroxy, halogeno, trifluoromethyl and cyano; p is 0-4; and Qis aryl or heteroaryl; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
Brown, Dearg S.,Belfield, Andrew J.,Brown, George R.,Campbell, Douglas,Foubister, Alan,Masters, David J.,Pike, Kurt G.,Snelson, Wendy L.,Wells, Stuart L.
, p. 5383 - 5387 (2007/10/03)
The discovery, rational analogue design, synthesis and SAR of a novel bisamide class of p38 MAP kinase inhibitor are reported. The activity in vitro is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues, such as 18. A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38α enzyme activity and lipopolysaccharide-induced tumour necrosis factor-α release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase
Cumming, John G.,McKenzie, Caroline L.,Bowden, Stuart G.,Campbell, Douglas,Masters, David J.,Breed, Jason,Jewsbury, Philip J.
, p. 5389 - 5394 (2007/10/03)
SAR studies led to the identification of 4-(3-benzoylamino-6-methyl- anilino)quinazolines as potent and selective inhibitors of p38 MAP kinase. Further optimisation led to the identification of a series of 4-(3-benzoylamino-6-methyl-anilino)pyrimidines as potent inhibitors of the p38 MAP kinase signalling pathway in vitro and in vivo. SAR studies led to the identification of 4-(3-benzoylamino-6-methyl-anilino)quinazolines as potent and selective inhibitors of p38 MAP kinase. Further optimisation led to the identification of a series of 4-(3-benzoylamino-6-methyl-anilino)pyrimidines as potent inhibitors of the p38 MAP kinase signalling pathway in vitro and in vivo.
