864972-26-9

Upstream product

• 1037168-91-4 C₂₄H₂₁F₂N₃O₄S 
• 349-88-2 4-Fluorobenzenesulfonyl chloride 
• 1361345-29-0 (R)-1-(4-fluoro-phenyl)-4a-hydroxymethyl-1,4,4a,5,7,8-hexahydro-1,2,6-triaza-cyclopenta[b]naphthalene-6-carboxylic acid tert-butyl ester 
• 864972-21-4 6-tert-butyl 4a-methyl (4aR)-1-(4-fluorophenyl)-4a,5,7,8-tetrahydro-1H-pyrazolo[3,4-g]isoquinoline-4a,6(4H)-dicarboxylate 

Downstream Products

• 1018679-87-2 C₂₃H₁₉F₂N₃O₃S 

Relevant academic research and scientific papers

HETEROARYL-ETHER FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS

The present invention provides heteroaryl ether fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.

1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity

Addition of the 4-fluorophenylpyrazole group to the previously described 2-azadecalin glucocorticoid receptor (GR) antagonist 1 resulted in significantly enhanced functional activity. SAR of the bridgehead substituent indicated that whereas groups as small as methyl afforded high GR binding, GR functional activity was enhanced by larger groups such as benzyl, substituted ethers, and aminoalkyl derivatives. GR antagonists with binding and functional activity comparable to mifepristone were discovered (e.g., 52: GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM) and found to be highly selective over other steroid receptors. Analogues 43 and 45 had >50% oral bioavailability in the dog.

FUSED RING AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS

The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.