Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia
The discovery of novel 4-hydroxy-2-(heterocyclic)pyrimidine-5-carboxamide inhibitors of hypoxia-inducible factor (HIF) prolyl hydroxylases (PHD) is described. These are potent, selective, orally bioavailable across several species, and active in stimulati
Debenham, John S.,Madsen-Duggan, Christina,Clements, Matthew J.,Walsh, Thomas F.,Kuethe, Jeffrey T.,Reibarkh, Mikhail,Salowe, Scott P.,Sonatore, Lisa M.,Hajdu, Richard,Milligan, James A.,Visco, Denise M.,Zhou, Dan,Lingham, Russell B.,Stickens, Dominique,Demartino, Julie A.,Tong, Xinchun,Wolff, Michael,Pang, Jianmei,Miller, Randy R.,Sherer, Edward C.,Hale, Jeffrey J.
p. 11039 - 11049
(2016/12/30)
Substituted 4-Hydroxypyrimidine-5-Carboxamides
The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
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Page/Page column 25
(2009/10/01)
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