21849-89-8Relevant articles and documents
AMPK ACTIVATORS
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Paragraph 00231; 00236, (2021/11/26)
This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Cameron, Kimberly O.,Kung, Daniel W.,Kalgutkar, Amit S.,Kurumbail, Ravi G.,Miller, Russell,Salatto, Christopher T.,Ward, Jessica,Withka, Jane M.,Bhattacharya, Samit K.,Boehm, Markus,Borzilleri, Kris A.,Brown, Janice A.,Calabrese, Matthew,Caspers, Nicole L.,Cokorinos, Emily,Conn, Edward L.,Dowling, Matthew S.,Edmonds, David J.,Eng, Heather,Fernando, Dilinie P.,Frisbie, Richard,Hepworth, David,Landro, James,Mao, Yuxia,Rajamohan, Francis,Reyes, Allan R.,Rose, Colin R.,Ryder, Tim,Shavnya, Andre,Smith, Aaron C.,Tu, Meihua,Wolford, Angela C.,Xiao, Jun
, p. 8068 - 8081 (2016/10/30)
Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the treatment of diabetic nephropathy. Identification of an indazole amide high throughput screening (HTS) hit followed by truncation to its minimal pharmacophore provided an indazole acid lead compound. Optimization of the core and aryl appendage improved oral absorption and culminated in the identification of indole acid, PF-06409577 (7). Compound 7 was advanced to first-in-human trials for the treatment of diabetic nephropathy.
CYCLIC PEROXIDE OXIDATION OF AROMATIC COMPOUND PRODUCTION AND USE THEREOF
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Page/Page column 9; 10, (2014/10/15)
The present invention provides a method for converting an aromatic hydrocarbon to a phenol by providing an aromatic hydrocarbon comprising one or more aromatic C-H bonds and one or more activated C-H bonds in a solvent; adding a phthaloyl peroxide to the solvent; converting the phthaloyl peroxide to a di-radical; contacting the di-radical with the one or more aromatic C-H bonds; oxidizing selectively one of the one or more aromatic C-H bonds in preference to the one or more activated C-H bonds; adding a hydroxyl group to the one of the one or more aromatic C-H bonds to form one or more phenols; and purifying the one or more phenols.