915394-66-0Relevant articles and documents
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia
Wu, Yue,Jiang, Zhensheng,Li, Zhihong,Gu, Jing,You, Qidong,Zhang, Xiaojin
, p. 5332 - 5349 (2018)
As a gene associated with anemia, the erythropoiesis gene is physiologically expressed under hypoxia regulated by ?hypoxia-inducing factor-α (HIF-α). Thus, stabilizing HIF-α is a potent strategy to stimulate the expression and secretion of erythropoiesis. In this study, we applied click chemistry to the discovery of HIF prolyl hydroxylase 2 (HIF-PHD2) inhibitors for the first time, and a series of triazole compounds showed preferable inhibitory activity in fluorescence polarization assays. Of particular note was the orally active HIF-PHD inhibitor 15i (IC50 = 62.23 nM), which was almost ten times more active than the phase III drug FG-4592 (IC50 = 591.4 nM). Furthermore, it can upregulate the hemoglobin of cisplatin-induced anemia mice (120 g/L) to normal levels (160 g/L) with no apparent toxicity observed in vivo. These results confirm that triazole compound 15i is a promising candidate for the treatment of renal anemia.
METHOD FOR PRODUCING IMIDAZOPYRIDINONE COMPOUND
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Paragraph 0260, (2021/09/27)
PROBLEM TO BE SOLVED: To provide a novel production method of an imidazopyridinone compound useful as a treatment agent for inflammatory bowel diseases (IBDs). SOLUTION: The present disclosure provides a method for the synthesis of, for example, an imidazopyridinone compound shown below. The method includes a process of introducing a desired substituent into the 1st-position of 2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridine, having an N-protected 3-pyrrolidino group at the 3rd-position; then deprotecting a 3rd-position substituent; and further introducing a desired substituent into N of the pyrrolidino group. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
Pyridine derivative compound acting on prolyl hydroxylase
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Paragraph 0078; 0079; 0080, (2017/12/30)
The invention relates to a pyridine derivative compound for treating hypoxia-inducible factor mediated and/or hemopoietin related symptoms. The pyridine derivative compound adopts the structure as shown in the description.