1005326-26-0Relevant articles and documents
Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1)
Filipski, Kevin J.,Sammons, Matthew F.,Bhattacharya, Samit K.,Panteleev, Jane,Brown, Janice A.,Loria, Paula M.,Boehm, Markus,Smith, Aaron C.,Shavnya, Andre,Conn, Edward L.,Song, Kun,Weng, Yan,Facemire, Carie,Jüppner, Harald,Clerin, Valerie
supporting information, p. 440 - 445 (2018/05/23)
Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solute-carrier (SLC) transporter located in the kidney proximal tubule that reabsorbs glomerular-filtered phosphate. Inhibition of NaPi2a may enhance urinary phosphate excretion and correct maladaptive mineral and hormonal derangements associated with increased cardiovascular risk in chronic kidney disease-mineral and bone disorder (CKD-MBD). To date, only nonselective NaPi inhibitors have been described. Herein, we detail the discovery of the first series of selective NaPi2a inhibitors, resulting from optimization of a high-throughput screening hit. The oral PK profile of inhibitor PF-06869206 (6f) in rodents allows for the exploration of the pharmacology of selective NaPi2a inhibition.
Fused ring compound and use thereof
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Page/Page column 36-37, (2010/08/07)
The present invention provides a compound represented by the formula: wherein the symbols are as described in the specification, or a salt thereof, which is useful for preventing/treating eicosanoid-associated diseases such as atherosclerosis, diabetes, obesity, atherothrombosis, asthma, fever, pain, cancer, rheumatism, osteoarthritis and atopic dermatitis, and which has an excellent pharmacological action, physicochemical properties, etc.