271587-47-4Relevant academic research and scientific papers
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics
Riether, Doris,Harcken, Christian,Razavi, Hossein,Kuzmich, Daniel,Gilmore, Thomas,Bentzien, J?rg,Pack, Edward J.,Souza, Donald,Nelson, Richard M.,Kukulka, Alison,Fadra, Tazmeen N.,Zuvela-Jelaska, Ljiljana,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Nabozny, Gerald H.,Thomson, David S.
experimental part, p. 6681 - 6698 (2010/12/19)
Syntheses and structure-activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene trans
Discovery of quinolines as selective glucocorticoid receptor agonists
Jaroch, Stefan,Berger, Markus,Huwe, Christoph,Krolikiewicz, Konrad,Rehwinkel, Hartmut,Sch?cke, Heike,Schmees, Norbert,Skuballa, Werner
scheme or table, p. 5835 - 5838 (2010/11/19)
The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respec
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists
Regan, John,Lee, Thomas W.,Zindell, Renée M.,Bekkali, Younes,Bentzien, J?rg,Gilmore, Thomas,Hammach, Abdelhakim,Kirrane, Thomas M.,Kukulka, Alison J.,Kuzmich, Daniel,Nelson, Richard M.,Proudfoot, John R.,Ralph, Mark,Pelletier, Josephine,Souza, Donald,Zuvela-Jelaska, Lijiljana,Nabozny, Gerald,Thomson, David S.
, p. 7887 - 7896 (2007/10/03)
We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.
1-PROPANOL AND 1-PROPYLAMINE DERIVATIVES AND THEIR USE AS GLUCOCORTICOID LIGANDS
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Page 144-147, (2008/06/13)
Compounds of Formula (I) wherein R1, R2 R3, R4, R5, R6, and X are as defiend herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocoricoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
Nonsteroidal anti-inflammatory agents
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, (2008/06/13)
This invention describes the use of the compounds of general formula I in which A, B, A, Ar, R1, R2and R3have the meaning that is indicated in more detail in the description, for the production of pharmaceutical agents with anti-inflammatory action. The compounds of general formula I show a clear dissociation between anti-inflammatory and metabolic action.
