67932-65-4

Usage

Structure

Bicyclic heterocyclic compound

Derivative

Indole derivative

Usage

Building block in the synthesis of pharmaceuticals, agrochemicals, and other organic compounds

Therapeutic potential

Cancer and neurological disorders

Precursor

Used in the production of dyes, perfumes, and flavorings

Versatility

Wide range of potential uses in various industries

InChI:InChI=1/C10H13N/c1-2-8-3-4-10-9(7-8)5-6-11-10/h3-4,7,11H,2,5-6H2,1H3

Upstream product

• 16078-35-6 1-(1-acetylindolin-5-yl)ethanone 
• 16078-30-1 1-Acetyl-2,3-dihydro-1H-indole 
• 81114-41-2 1-benzenesulfonyl-2,3-dihydro-1H-indole 
• 118757-07-6 1-(1-benzenesulfonyl-2, 3-dihydro-1H-indol-5-yl)ethanone 
• 496-15-1 1-indoline 
• 118757-02-1 1-benzenesulfonyl-5-ethyl-2,3-dihydro-1H-indole 

Downstream Products

• 873055-25-5 5-ethyl-6-nitro-2,3-dihydro-1H-indole 
• 873055-27-7 5-ethyl-1H-indol-6-amine 

Relevant academic research and scientific papers

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.

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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.

Modulators of ATP-binding cassette transporters

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.