271587-47-4Relevant academic research and scientific papers
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
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
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.
