609849-80-1Relevant articles and documents
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate
Harcken, Christian,Riether, Doris,Liu, Pingrong,Razavi, Hossein,Patel, Usha,Lee, Thomas,Bosanac, Todd,Ward, Yancey,Ralph, Mark,Chen, Zhidong,Souza, Donald,Nelson, Richard M.,Kukulka, Alison,Fadra-Khan, Tazmeen N.,Zuvela-Jelaska, Ljiljana,Patel, Mita,Thomson, David S.,Nabozny, Gerald H.
supporting information, p. 1318 - 1323 (2015/01/09)
A series of nonsteroidal dissociated glucocorticoid receptor agonists was optimized for drug-like properties such as cytochrome P450 inhibition, metabolic stability, aqueous solubility, and hERG ion channel inhibition. This effort culminated in the identification of the clinical candidate compound (R)-39.
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects
Harcken, Christian,Riether, Doris,Kuzmich, Daniel,Liu, Pingrong,Betageri, Raj,Ralph, Mark,Emmanuel, Michel,Reeves, Jonathan T.,Berry, Angela,Souza, Donald,Nelson, Richard M.,Kukulka, Alison,Fadra, Tazmeen N.,Zuvela-Jelaska, Ljiljana,Dinallo, Roger,Bentzien, J?rg,Nabozny, Gerald H.,Thomson, David S.
, p. 1583 - 1598 (2014/03/21)
Synthesis and structure-activity relationship (SAR) of a series of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain "diazaindole" moieties and display different transcriptional regulatory profiles in vitro and are
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
GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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Page/Page column 64-65, (2009/12/28)
Compounds of Formula I wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid 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.
