- Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors
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A series of pyrimidinopyridones has been designed, synthesized and shown to be potent and selective inhibitors of the FMS tyrosine kinase. Introduction of an amide substituent at the 6-position of the pyridone core resulted in a significant potency increase. Compound 24 effectively inhibited in vivo LPS-induced TNF in mice greater than 80%.
- Huang, Hui,Hutta, Daniel A.,Hu, Huaping,DesJarlais, Renee L.,Schubert, Carsten,Petrounia, Ioanna P.,Chaikin, Margery A.,Manthey, Carl L.,Player, Mark R.
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p. 2355 - 2361
(2008/09/20)
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- 5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase
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The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R101 and R200 are described in the specification.
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Page/Page column 68
(2010/11/26)
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