Beck, Hartmut; Jeske, Mario; Thede, Kai; Stoll, Friederike; Flamme, Ingo; Akbaba, Metin; Ergueden, Jens-Kerim; Karig, Gunter; Keldenich, Joerg; Oehme, Felix; Militzer, Hans-Christian; Hartung, Ingo V.; Thuss, Uwe published the artcile< Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia>, HPLC of Formula: 5018-38-2, the main research area is diheteroaryldihydropyrazolone preparation HIF prolyl hydroxylase inhibitor kidney disease anemia; molidustat BAY3934 preparation HIF prolyl hydroxylase inhibitor kidney anemia; BAY 85-3934; HIF-PH; inhibitors; metalloenzymes; molidustat.
Small-mol. inhibitors of hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) are currently under clin. development as novel treatment options for chronic kidney disease (CKD) associated anemia. Inhibition of HIF-PH mimics hypoxia and leads to increased erythropoietin (EPO) expression and subsequently increased erythropoiesis. Herein the authors describe the discovery, synthesis, structure-activity relationship (SAR), and proposed binding mode of novel 2,4-diheteroaryl-1,2-dihydro-3H-pyrazol-3-ones as orally bioavailable HIF-PH inhibitors for the treatment of anemia. High-throughput screening of the authors’ corporate compound library identified BAY-908 as a promising hit. The lead optimization program then resulted in the identification of molidustat (BAY 85-3934), a novel small-mol. oral HIF-PH inhibitor. Molidustat is currently being investigated in clin. phase III trials as molidustat sodium for the treatment of anemia in patients with CKD.
ChemMedChem published new progress about Anemia (chronic kidney disease associated). 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, HPLC of Formula: 5018-38-2.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia