683813-75-4Relevant academic research and scientific papers
An efficient synthesis of Ecopladib
Li, Wei,Li, Jianchang,DeVincentis, Dianne,Mansour, Tarek S.
, p. 7871 - 7876 (2008)
An efficient synthesis of Ecopladib, an indole inhibitor of cytosolic phospholipase A2α, is described. A new reaction involving indole C3 reductive alkylation using an acetal in the absence of water and a novel transformation of the C2 methyl t
Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
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Page/Page column 12, (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.
Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α
Lee, Katherine L.,Foley, Megan A.,Chen, Lihren,Behnke, Mark L.,Lovering, Frank E.,Kirincich, Steven J.,Wang, Weiheng,Shim, Jaechul,Tam, Steve,Shen, Marina W. H.,Khor, SooPeang,Xu, Xin,Goodwin, Debra G.,Ramarao, Manjunath K.,Nickerson-Nutter, Cheryl,Donahue, Frances,Ku, M. Sherry,Clark, James D.,McKew, John C.
, p. 1380 - 1400 (2008/02/01)
The synthesis and structure-activity relationship of a series of indole inhibitors of cytosolic phospholipase A2α (cPLA 2α, type IVA phospholipase) are described. Inhibitors of cPLA2α are predicted to be efficacious in treating asthma as well as the signs and symptoms of osteoarthritis, rheumatoid arthritis, and pain. The introduction of a benzyl sulfonamide substituent at C2 was found to impart improved potency of these inhibitors, and the SAR of these sulfonamide analogues is disclosed. Compound 123 (Ecopladib) is a submicromolar inhibitor of cPLA2α in the GLU micelle and rat whole blood assays. Compound 123 displayed oral efficacy in the rat carrageenan air pouch and rat carrageenan-induced paw edema models.
