1020153-96-1Relevant academic research and scientific papers
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity
Diallo, Hawa,Angell, Davina C.,Barnett, Heather A.,Biggadike, Keith,Coe, Diane M.,Cooper, Tony W.J.,Craven, Andy,Gray, James R.,House, David,Jack, Torquil I.,Keeling, Steve P.,MacDonald, Simon J.F.,McLay, Iain M.,Oliver, Samuel,Taylor, Simon J.,Uings, Iain J.,Wellaway, Natalie
scheme or table, p. 1126 - 1133 (2011/04/16)
A novel series of indazole non-steroidal glucocorticoid receptor agonist has been discovered. This series features a sulfonamide central core and meta amides which interact with the extended ligand binding domain. This series has produced some of the most potent and least lipophilic agonists of which we are aware such as 20a (NFκB pIC50 8.3 (100%), c log P 1.9). Certain analogues in this series also display evidence for modulated pharmacology.
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists
Biggadike, Keith,Caivano, Matilde,Clackers, Margaret,Coe, Diane M.,Hardy, George W.,Humphreys, Davina,Jones, Haydn T.,House, David,Miles-Williams, Annette,Skone, Philip A.,Uings, Iain,Weller, Vicki,McLay, Iain M.,Macdonald, Simon J.F.
scheme or table, p. 4846 - 4850 (2010/05/18)
Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFκB agonist activity was optimised in an iterative process from pIC50 7.5 (for 7), to pIC50 10.1 (for 38E1). An explanation for the SAR observed base
NOVEL COMPOUNDS
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Page/Page column 62-63, (2008/06/13)
The present invention provides glucocorticoid receptor agonists of formula (I), a process for their preparation, pharmaceutical compositions comprising the compounds and the preparation of said compositions, intermediates and use of the compounds for the
