706820-79-3Relevant academic research and scientific papers
Novel monocyclic amide-linked phenol derivatives without mitochondrial toxicity have potent uric acid-lowering activity
Uda, Junichiro,Kobashi, Seiichi,Ashizawa, Naoki,Matsumoto, Koji,Iwanaga, Takashi
supporting information, (2021/03/30)
Although benzbromarone (BBR) is a conventional, highly potent uricosuric drug, it is not a standard medicine because it causes rare but fatal fulminant hepatitis. We transformed the bis-aryl ketone structure of BBR to generate novel monocyclic amide-linked phenol derivatives that should possess uric acid excretion activity without adverse properties associated with BBR. The derivatives were synthesized and tested for uric acid uptake inhibition (UUI) in two assays using either urate transporter 1-expressing cells or primary human renal proximal tubule epithelial cells. We also evaluated their inhibitory activity against mitochondrial respiration as a critical mitochondrial toxicity parameter. Some derivatives with UUI activity had no mitochondrial toxicity, including compound 3f, which effectively lowered the plasma uric acid level in Cebus apella. Thus, 3f is a promising candidate for further development as a uricosuric agent.
Xanthine oxidase inhibitor and application thereof
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Paragraph 0083; 0085, (2017/08/26)
The invention discloses a xanthine oxidase inhibitor and application thereof. The xanthine oxidase inhibitor is a compound shown as a general formula (I) and is a pharmaceutically acceptable salt. The xanthine oxidase inhibitor, which is the compound and
2-'5-(5-CARBAMIMIDOYL-1H-HETEROARYL)-6-HYDROXYBIPHENYL-3-YL!- CARBOXYLIC ACID DERIVATIVES AS FACTOR VIIA INHIBITORS
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Page/Page column 35-36, (2010/02/07)
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS
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Page 71, (2008/06/13)
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
Optimization of a screening lead for factor VIIa/TF
Young, Wendy B,Kolesnikov, Aleksandr,Rai, Roopa,Sprengeler, Paul A,Leahy, Ellen M,Shrader, William D,Sangalang, Joan,Burgess-Henry, Jana,Spencer, Jeff,Elrod, Kyle,Cregar, Lynne
, p. 2253 - 2256 (2007/10/03)
The structure-based design and progression of a screening lead to a 3 nM factor VIIa/TF inhibitor with improved selectivity versus related enzymes is described.
