1025762-88-2Relevant academic research and scientific papers
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists
Sheppeck II, James E.,Gilmore, John L.,Xiao, Hai-Yun,Dhar, T.G. Murali,Nirschl, David,Doweyko, Arthur M.,Sack, Jack S.,Corbett, Martin J.,Malley, Mary F.,Gougoutas, Jack Z.,McKay, Lorraine,Cunningham, Mark D.,Habte, Sium F.,Dodd, John H.,Nadler, Steven G.,Somerville, John E.,Barrish, Joel C.
, p. 5442 - 5447 (2013/09/23)
Modification of a phenolic lead structure based on lessons learned from increasing the potency of steroidal glucocorticoid agonists lead to the discovery of exceptionally potent, nonsteroidal, indazole GR agonists. SAR was developed to achieve good selectivity against other nuclear hormone receptors with the ultimate goal of achieving a dissociated GR agonist as measured by human in vitro assays. The specific interactions by which this class of compounds inhibits GR was elucidated by solving an X-ray co-crystal structure.
MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF
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Page/Page column 90, (2008/12/05)
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
