314298-15-2Relevant academic research and scientific papers
COMPOUNDS FOR INHIBITION OF ALPHA 4β7 INTEGRIN
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Paragraph 0422, (2020/05/29)
The present disclosure provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
Design and synthesis of highly potent and selective (2-arylcarbamoyl- phenoxy)-acetic acid inhibitors of aldose reductase for treatment of chronic diabetic complications
Van Zandt, Michael C.,Sibley, Evelyn O.,McCann, Erin E.,Combs, Kerry J.,Flam, Brenda,Sawicki, Diane R.,Sabetta, Al,Carrington, Anne,Sredy, Janet,Howard, Eduardo,Mitschler, Andre,Podjarny, Alberto D.
, p. 5661 - 5675 (2007/10/03)
Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective (2-arylcarbamoyl-phenoxy)-acetic acid aldose reductase inhibitors. The compound class features a core template that utilizes an intramolecular hydrogen bond to position the key structural elements of the pharmacophore in a conformation, which promotes a high binding affinity. The lead candidate, example 40, 5-fluoro-2-(4-bromo-2-fluoro-benzylthiocarbamoyl)-phenoxyacetic acid, inhibits aldose reductase with an IC50 of 30 nM, while being 1100 times less active against aldehyde reductase, a related enzyme involved in the detoxification of reactive aldehydes. In addition, example 40 lowers nerve sorbitol levels with an ED50 of 31 mg/kg/d po in the 4-day STZ-induced diabetic rat model.
Substituted phenoxyacetic acids
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, (2008/06/13)
Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.
