- SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-A]PYRAZIN-1 (2H)-ONE DERIVATIVES AS KINASE INHIBITORS
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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.
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Page/Page column 173
(2016/10/31)
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- PYRIMIDINYLPYRAZOLES AS TGF-BETA INHIBITORS
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The invention is based on the discovery that compounds of formula (I) possess high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. The invention feat
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Page/Page column 29-30
(2010/10/20)
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- Pyrimidinylimidazole inhibitors of CSBP/P38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes
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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.
- 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.
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p. 3111 - 3116
(2007/10/03)
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