873055-66-4

Upstream product

• 10323-39-4 4-bromo-2-tert-butylphenol 
• 79-22-1 methyl chloroformate 
• 88-18-6 2-tert-Butylphenol 

Downstream Products

• 873055-77-7 1-tert-butyl-2-methoxy-5-(trifluoromethyl)-4-nitrobenzene 
• 873055-76-6 1-tert-butyl-2-methoxy-5-bromo-4-nitrobenzene 
• 873055-79-9 2-tert-butyl-4-bromo-5-aminophenol 
• 873055-78-8 1-tert-butyl-2-methoxy-5-(trifluoromethyl)-4-aminobenzene 
• 873055-73-3 2-tert-butyl-4-(2-ethoxyphenyl)-5-aminophenol 
• 873055-71-1 5-amino-2-tert-butyl-4-(trifluoromethyl)phenol 
• 873055-70-0 1-tert-butyl-2-(benzyloxy)-5-(trifluoromethyl)-4-nitrobenzene 
• 873055-69-7 1-tert-butyl-2-(benzyloxy)-5-bromo-4-nitrobenzene 
• 873052-80-3 N-(4-(tert-butyl)-5-hydroxy-2-(trifluoromethyl)phenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide 
• 873055-68-6 2-tert-butyl-4-bromo-5-nitrophenol 
• 873055-67-5 methyl (2-tert-butyl-4-bromo-5-nitrophenyl) carbonate 

Relevant academic research and scientific papers

COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY

The present disclosure features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of compounds disclosed herein.

SILICONE ATOMS CONTAINING IVACAFTOR ANALOGUES

The present disclosure is directed to disclosed compounds that modulate e.g., address underlying defects in cellular processing of CFTR activity.

Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

Discovery of N -(2,4-Di- tert -butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, Ivacaftor), a potent and orally bioavailable CFTR potentiator

Quinolinone-3-carboxamide 1, a novel CFTR potentiator, was discovered using high-throughput screening in NIH-3T3 cells expressing the F508del-CFTR mutation. Extensive medicinal chemistry and iterative structure-activity relationship (SAR) studies to evaluate potency, selectivity, and pharmacokinetic properties resulted in the identification of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, 48, ivacaftor), an investigational drug candidate approved by the FDA for the treatment of CF patients 6 years of age and older carrying the G551D mutation.

COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.