875415-00-2Relevant academic research and scientific papers
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.
, 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.
