862574-87-6Relevant articles and documents
Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
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Page/Page column 101; 102, (2021/04/21)
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.
1 - (2, 2 - Difluorobenzene and [D] [1, 3] dioxo heterocyclic pentene -5 - yl) ring propyl nitrile of preparation method
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Page/Page column 5-6, (2019/02/08)
The invention discloses a preparation method for 1-(2,2-difluoro-benzo[D][1,3]dioxol-5-yl)-cyclopropanecarbonitrile. The method comprises the following steps: 5-(chloromethyl)benzo[d][1,3]dioxole is prepared from 2,2-difluoro-1,3-benzodioxole through Blanc chloromethylation, and then is subjected to cyanation by utilization of cuprous cyanide, finally cyclization is carried out by utilization of 1-Bromo-2-chloroethane and a product is obtained. In the above method, cyanation is carried out by utilization of low-toxic cuprous cyanide, a weak organic base triethylamine deacid reagent is employed to carry out cyclization preparation and a target product is obtained, usage of dangerous lithium aluminum hydride and sodium cyanide is avoided, strong alkaline and high temperature conditions are avoided, and therefore hydrolysis of cyan in the product is avoided. The preparation method is low-toxic to the environment and the product yield and quality are raised. The process flow is simple and safe, the reaction process is easy to control, the cost is low, the yield is high, and the preparation method is suitable for industrialization.
MODULATOR OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATOR
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Paragraph 00248; 00250; 00251, (2018/06/30)
Compounds of Formula (I) pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.