1294504-66-7Relevant articles and documents
Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
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, (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.
Tezacaftor intermediate II preparation method
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Paragraph 0047; 0050-0058; 0068-0070, (2019/11/20)
The invention provides a Tezacaftor intermediate II preparation method, which comprises: carrying out a reaction on a compound represented by a formula I and used as a reaction raw material under theactions of a catalyst and an alkali in an organic solvent to obtain a Tezacaftor intermediate II, wherein the reaction equation is defined in the specification, and the catalyst of the reaction is a mixture of a copper salt and N-methylpyrrolidone. According to the present invention, by using the completely-new CuI/NMP catalytic system, the problem that the Pd reagent is used in the prior art is eliminated so as to greatly reduce the production cost, the influence of the residual metal palladium on the drug Tezacaftor can be avoided, and importantly the reaction yield of the key step for Tezacaftor intermediate II synthesis is significantly increased by using the completely-new CuI/NMP catalytic system so as to greatly increase the Tezacaftor intermediate II production efficiency and further reduce the production cost.
CYCLOPROPANECARBOXAMIDE MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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, (2016/08/03)
The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.