1028458-64-1

Upstream product

• 492-41-1 (1R,2S)-norephedrine 
• 146137-76-0 2-Fluoro-5-iodo-benzaldehyde 
• 139631-62-2 cyclopropanesulfonyl chloride 
• 1025762-98-4 1-(4-fluorophenyl)-5-iodo-1H-indazole 
• 1028459-20-2 (1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenyl-propan-2-amine 

Relevant academic research and scientific papers

Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators

A structure-based design approach led to the identification of a novel class of indazole ether based, non-steroidal glucocorticoid receptor (GR) modulators. Several examples were identified that displayed cell potency in the picomolar range, inhibiting LPS-induced TNF-α release by primary peripheral blood mononuclear cells (PBMCs). Additionally, an improved steroid hormone receptor binding selectivity profile, compared to classical steroidal GR agonists, was demonstrated. The indazole ether core tolerated a broad range of substituents allowing for modulation of the physiochemical parameters. A small sub-set of indazole ethers, with pharmacokinetic properties suitable for oral administration, was investigated in a rat antigen-induced joint inflammation model and demonstrated excellent anti-inflammatory efficacy.

INDOZALYL SULPHONAMIDE DERIVATIVES USEFUL AS GLUCOCORTICOID MODULATORS

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).