Ogoshi, Yosuke; Matsui, Takuya; Mitani, Ikuo; Yokota, Masahiro; Terashita, Masakazu; Motoda, Dai; Ueyama, Kazuhito; Hotta, Takahiro; Ito, Takashi; Hase, Yasunori; Fukui, Kenji; Deai, Katsuya; Yoshiuchi, Hiromi; Ito, Soichiro; Abe, Hiroyuki published the artcile< Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia>, Application In Synthesis of 112-63-0, the main research area is JTZ951 HIF prolyl hydroxylase inhibitor kidney anemia.
Inhibition of hypoxia inducible factor prolyl hydroxylase (PHD) represents a promising strategy for the discovery of a next generation treatment for renal anemia. We identified several 5,6-fused ring systems as novel scaffolds of the PHD inhibitor on the basis of pharmacophore anal. In particular, triazolopyridine derivatives showed potent PHD2 inhibitory activities. Examination of the predominance of the triazolopyridines in potency by electrostatic calculations suggested favorable π-π stacking interactions with Tyr310. Lead optimization to improve the efficacy of erythropoietin release in cells and in vivo by improving cell permeability led to the discovery of JTZ-951 (compound 14), with a 5-phenethyl substituent on the triazolopyridine group, which increased Hb levels with daily oral dosing in rats. Compound 14 was rapidly absorbed after oral administration and disappeared shortly thereafter, which could be advantageous in terms of safety. Compound 14 was selected as a clin. candidate.
ACS Medicinal Chemistry Letters published new progress about Hemoglobins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.
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