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.
IMIDAZOPYRIDINONE COMPOUND
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Paragraph 0288, (2021/04/23)
The present invention aims to provide a novel compound which has prolyl hydroxylase (PHDs) inhibitory effect and which is useful for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. The present invention relates to a imidazopyridinone compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof which have prolyl hydroxylase inhibitory effect and, are useful as agents for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. In an embodiment, the present invention relates to a method for treating an inflammatory bowel disease
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
PHARMACEUTICAL COMPOSITION CONTAINING IMIDAZOPYRIDINONE COMPOUND
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Paragraph 0254, (2021/09/27)
PROBLEM TO BE SOLVED: To provide a compound useful as a treatment agent for inflammatory bowel diseases such as ulcerative colitis, and a pharmaceutical composition containing the same. SOLUTION: The present disclosure provides a pharmaceutical composition containing an imidazopyridinone compound of the following formula (I) or a pharmacologically acceptable salt thereof. 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.
Dynamic combinatorial chemistry employing boronic acids/boronate esters leads to potent oxygenase inhibitors
Demetriades, Marina,Leung, Ivanhoe K. H.,Chowdhury, Rasheduzzaman,Chan, Mun Chiang,McDonough, Michael A.,Yeoh, Kar Kheng,Tian, Ya-Min,Claridge, Timothy D. W.,Ratcliffe, Peter J.,Woon, Esther C. Y.,Schofield, Christopher J.
supporting information; experimental part, p. 6672 - 6675 (2012/09/22)
Dynamic duo: The reversible reaction of boronic acids with alcohols to form boronate esters, coupled to protein mass spectrometry analyses, was used to discover potent oxygenase inhibitors. This dynamic combinatorial mass spectrometry technique could potentially be applied to the identification of other protein inhibitors. Copyright
Design and synthesis of substituted pyridine derivatives as HIF-1α prolyl hydroxylase inhibitors
Warshakoon, Namal C.,Wu, Shengde,Boyer, Angelique,Kawamoto, Richard,Sheville, Justin,Bhatt, Ritu Tiku,Renock, Sean,Xu, Kevin,Pokross, Matthew,Zhou, Songtao,Walter, Richard,Mekel, Marlene,Evdokimov, Artem G.,East, Stephen
, p. 5616 - 5620 (2007/10/03)
Structure-guided de novo drug design led to the identification of a novel series of substituted pyridine derivatives as HIF-1α prolyl hydroxylase inhibitors. Pyridine carboxyamide derivatives bearing a substituted aryl group at the 5-position of the pyrid
