540522-70-1Relevant academic research and scientific papers
Indole cytosolic phospholipase A2 α inhibitors: Discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4- dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl} benzoic acid, efipladib
McKew, John C.,Lee, Katherine L.,Shen, Marina W. H.,Thakker, Paresh,Foley, Megan A.,Behnke, Mark L.,Hu, Baihua,Sum, Fuk-Wah,Tam, Steve,Hu, Yonghan,Chen, Lihren,Kirincich, Steven J.,Michalak, Ronald,Thomason, Jennifer,Ipek, Manus,Wu, Kun,Wooder, Lane,Ramarao, Manjunath K.,Murphy, Elizabeth A.,Goodwin, Debra G.,Albert, Leo,Xu, Xin,Donahue, Frances,Ku, M. Sherry,Keith, James,Nickerson-Nutter, Cheryl L.,Abraham, William M.,Williams, Cara,Hegen, Martin,Clark, James D.
experimental part, p. 3388 - 3413 (2009/05/26)
The optimization of a class of indole cPLA2α inhibitors is described herein. The importance of the substituent at C3 and the substitution pattern of the phenylmethane sulfonamide region are highlighted. Optimization of these regions led to the
Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
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Page/Page column 19, (2010/11/29)
This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.
Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts
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Page/Page column 8, (2008/06/13)
The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar—(R)z—O2—X and sulfonamides of Formula Ar—(R)2—SO2—NR4R5, where the constituent varia
INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2
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Page/Page column 35, (2008/06/13)
This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLAα). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
Process for making an aldehyde
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Page 17, (2008/06/13)
A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.
