952664-69-6

Usage

Uses

Used in Pharmaceutical Industry:
Benzenamine, 2-broMo-5-fluoro-4-nitro-, is used as a key building block for the synthesis of various pharmaceuticals. Its unique structure allows for the development of new drugs with specific therapeutic properties, contributing to the advancement of medicine.
Used in Agrochemical Industry:
In the agrochemical sector, Benzenamine, 2-broMo-5-fluoro-4-nitro-, serves as an essential intermediate in the production of agrochemicals. Its incorporation into these compounds can enhance their effectiveness in pest control and crop protection, thereby supporting agricultural productivity.
Used in Dye and Pigment Production:
Benzenamine, 2-broMo-5-fluoro-4-nitro-, is utilized as an intermediate in the manufacturing of dyes and pigments. Its presence in these products imparts specific color characteristics and improves their performance in various applications, such as textiles, plastics, and printing inks.

Upstream product

• 2369-13-3 3-fluoro-4-nitroaniline 
• 1003-99-2 2-bromo-5-fluoroaniline 
• 1643796-25-1 benzyl (2-bromo-5-fluorophenyl)carbamate 
• 446-09-3 2-bromo-5-fluoronitrobenzene 
• 1009-06-9 N-(2-bromo-5-fluoro-phenyl)acetamide 
• 128-08-5 N-Bromosuccinimide 

Downstream Products

• 952664-70-9 2-(3,3-dimethylbut-1-ynyl)-5-fluoro-4-nitroaniline 
• 1152311-72-2 ethyl 5-(2-amino-4-fluoro-5-nitrophenyl)-3,3-dimethylpent-4-ynoate 
• 1225589-66-1 benzyl 4-(2-amino-4-fluoro-5-nitrophenyl)-2,2-dimethylbut-3-ynoate 
• 1294504-64-5 (R)-1-((4-amino-2-bromo-5-fluorophenyl)amino)-3-(benzyloxy)propan-2-ol p-toluenesulfonic acid salt 
• 1342896-73-4 (R)-1-(benzyloxy)-3-(2-bromo-5-fluoro-4-nitrophenylamino)propan-2-ol 
• 1294504-63-4 (R)-1-(4-amino-2-bromo-5-fluorophenylamino)-3-(benzyloxy)propan-2-ol 
• 1294504-68-9 N-{1-[(2R)-3-(benzyloxy)-2-hydroxypropyl]-2-[1-(benzyloxy)-2-methylpropan-2-yl]-6-fluoro-1H-indol-5-yl}-1-(2,2-difluoro-2H-1,3-benzodioxol-5-yl)cyclopropane-1-carboxamide 
• 1294504-67-8 (2R)-1-{5-amino-2-[1-(benzyloxy)-2-methylpropan-2-yl]-6-fluoro-1H-indol-1-yl}-3-(benzyloxy)propan-2-ol 

Relevant academic research and scientific papers

Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases

The present invention features compositions comprising a plurality of therapeutic agents wherein the presence of one therapeutic agent enhances the properties of at least one other therapeutic agent. In one embodiment, the therapeutic agents are cystic fibrosis transmembrane conductance regulators (CFTR) such as a CFTR corrector or CFTR potentiator for the treatment of CFTR mediated diseases such as cystic fibrosis. Methods and kits thereof are also disclosed.

Synthesis method and intermediate for 2-bromo-5-fluoro-4-nitroaniline

The invention discloses a synthesis method and an intermediate for 2-bromo-5-fluoro-4-nitroaniline. The synthesis method for 2-bromo-5-fluoro-4-nitroaniline comprises the step of carrying out a nitration reaction on 2-bromo-5-fluoroaniline and a nitration reagent to generate the 2-bromo-5-fluoro-4-nitroaniline, or comprises the following steps: reacting the 2-bromo-5-fluoroaniline with an amino protection reagent to obtain amino-protected 2-bromo-5-fluoroaniline, then carrying out the nitration reaction on the amino-protected 2-bromo-5-fluoroaniline and the nitration reagent to generate a nitration product that is the intermediate, and finally, removing the amino protection group from the nitration product to obtain the 2-bromo-5-fluoro-4-nitroaniline. The synthesis method has the advantages of high reaction yield, high product purity and easily available raw materials.

CYCLOPROPANECARBOXAMIDE MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.

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.

PHARMACEUTICAL COMPOSITIONS OF (R)-1-(2,2-DIFLURORBENZO[D][1,3]DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPROPAN-2-YL)-1H-INDOL-5-YL) CYCLOPROPANECARBOXAMIDE AND ADMINISTRATION THEREOF

A pharmaceutical composition comprising Compound 1, (R)- 1 -(2,2- difluorobenzo[d] [ 1,3]dioxol-5-yl)-N-( 1 -(2,3-dihydroxypropyl)-6-fluoro-2-( 1 -hydroxy-2- methylpropan-2-yl)- l H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from : a filler, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.

Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide

The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.

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.

PHARMACEUTICL COMPOSITIONS FOR THE TREATMENT OF CFTR -MEDIATED DISORDERS

The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5- hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxaraide (Compound 1), solids forms, and pharmaceutical compositions thereof for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to the use of Compound ? in combination with 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxoI- 5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 2), and Compound 1 in combination with (S)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3- dihydroxypropyl)~6~fluoro-2-( 1 -hydroxy-2-methylpropan-2-yl)- 1H-indol-5- yl)cyclopropanecarboxamide (Compound 3), for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to solid forms and formulations of Compound 2 or Compound 3 in combination with Compound 1, and pharmaceutical compositions thereof, for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.

FORMULATIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPROPAN-2-YL)-1H-INDOL-5-YL)CYCLOPROPANECARBOXAMIDE

The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith.

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.