934987-46-9Relevant academic research and scientific papers
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation
Edman, Karl,Ahlgren, Ragnhild,Bengtsson, Malena,Bladh, Hakan,Baeckstroem, Stefan,Dahmen, Jan,Henriksson, Krister,Hillertz, Per,Hulikal, Vijakumar,Jerre, Anders,Kinchin, Liz,Kase, Charlotte,Lepistoe, Matti,Mile, Irene,Nilsson, Stinabritt,Smailagic, Amir,Taylor, John,Tjoernebo, Ann,Wissler, Lisa,Hansson, Thomas
, p. 2571 - 2577 (2014/05/20)
We report the discovery of highly potent and selective non-steroidal glucocorticoid receptor modulators with PK properties suitable for inhalation. A high throughput screen of the AstraZeneca compound collection identified sulfonamide 3 as a potent non-steroidal glucocorticoid receptor ligand. Further optimization of this lead generated indazoles 30 and 48 that were progressed to characterization in in vivo models. X-ray crystallography was used to gain further insight into the binding mode of selected ligands.
NOVEL BICYCLIC SULFONAMIDES FOR USE AS GLUCOCORTICOID RECEPTOR MODULATORS IN THE TREATMENT OF INFLAMMATORY DISEASES
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Page/Page column 55, (2008/06/13)
Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
