Fused pyrimidine derivativesFused pyrimidine derivatives R 0515 Design and Synthesis of Potent, Orally Bioavailable Dihydroquinazolinone Inhibitors of p38 MAP Kinase. -A variety of new dihydroquinazoline inhibitors of p38 MAP kinase [cf. (VII) and (X)] are synthesized. Optimization of the C-5 aryl and C-7 piperidinyl substituents results in the identification of compound (X), which gives excellent suppression of TNF-α production and good oral exposure in rats. -(STELMACH*, J. E.; et al.; Bioorg. Med. Chem. Lett. 13 (2003) 2, 277-280; Dep. Med. Chem., Merck Res. Lab., Rahway, NJ 07065, USA; Eng.) -M. Schroeter 19-153
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