448956-58-9

Upstream product

• 459-57-4 4-fluorobenzaldehyde 
• 756869-45-1 [4-(4-allyloxy-phenoxy)-benzyl]-benzyl-(2-methyl-3-nitro-phenyl)-amine 
• 756869-43-9 [4-(4-allyloxy-phenoxy)-benzyl]-(2-methyl-3-nitro-phenyl)-amine 
• 448956-60-3 4-[4-(allyloxy)phenoxy]benzaldehyde 
• 123-31-9 hydroquinone 
• 100-39-0 benzyl bromide 
• 135054-68-1 (3R,5S)-6-<(methylsulfonyl)oxy>-3,5-O-isopropylidene-3,5-dihydroxyhexanoic acid tert-butyl ester 
• 448956-61-4 4-(4-{[benzyl-(2-methyl-3-nitro-phenyl)-amino]-methyl}-phenoxy)-phenol 

Downstream Products

• 756869-51-9 tert-butyl 6-O-(4-{4-[(benzyl{2-methyl-3-[(methylsulfonyl)amino]phenyl}amino)methyl]phenoxy}phenyl)-2,4-dideoxy-3,5-O-(1-methylethylidene)-D-erythro-hexonate 
• 756869-53-1 (3R,5S)-6-[4-(4-{[Benzyl-(3-methanesulfonylamino-2-methyl-phenyl)-amino]-methyl}-phenoxy)-phenoxy]-3,5-dihydroxy-hexanoic acid tert-butyl ester 

Relevant academic research and scientific papers

Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids

The synthesis, activity, metabolic stability, and pharmacokinetics of steroidal and nonsteroidal glucocorticoid receptor modulator-statin hybrids is reported. Potent steroidal antagonist-statin hybrids like 22 (h-GR binding IC50=7nM) and nonsteroidal modulator hybrids like 16 (h-GR binding IC50=2nM) were discovered. Appending a 'statin'-like diol-acid group to the modulators dramatically improved metabolic stability (and in some cases hepatocyte activity), but did not impart hepatoselectivity.

GLUCOCORTICOID RECEPTOR MODULATORS

Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.