1004-17-7Relevant articles and documents
SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-A]PYRAZIN-1 (2H)-ONE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 173, (2016/10/31)
Compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 have any of the meanings defined hereinbefore in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cancer are disclosed.
Pyrimidinylimidazole inhibitors of CSBP/P38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes
Adams, Jerry L.,Boehm, Jeffrey C.,Kassis, Shouki,Gorycki, Peter D.,Webb, Edward F.,Hall, Ralph,Sorenson, Margaret,Lee, John C.,Ayrton, Andrew,Griswold, Don E.,Gallagher, Timothy F.
, p. 3111 - 3116 (2007/10/03)
Pyrimidine analogs of the pyridinylimidazole class of CSBP/p38 kinase inhibitors were prepared in an effort to reduce the potent inhibition of hepatic cytochrome P450 observed for the pyridinyl compounds. The substitution of pyrimidin-4-yl, 2-methoxypyrimidin-4-yl, or 2- methylaminopyrimidin-4-yl for pyridin-4-yl effectively dissociates CSBP/p38 kinase from P450 inhibition for this series and furthermore achieves an increase in oral activity.