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1152311-62-0Relevant academic research and scientific papers
Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
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Page/Page column 112; 113, (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.
NOVEL CRYSTALLINE FORM OF 1-(2,2-DIFLUORO-2H-1,3BENZO DIOXOL-5-YL)-N-{1-[(2R)-2,3-DIHYDROXYPROPYL]-6-FLUORO-2-(1-HYDROXY-2-METHYLPROPAN-2-YL)-1H-INDOL-5-YL}CYCLOPROPANE-1-CARBOXAMIDE AND ITS PROCESS FOR THE PREPARATION THEREOF
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, (2021/07/17)
The present application relates to a novel crystalline form of 1-(2,2-difluoro-2H- 1,3- benzodioxol-5-yl)- N- {1-[(2R)-2,3-dihydroxypropyl]- 6- fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl}cyclopropane-1-carboxamide compound of formula-1 and its process for the preparation thereof. Formula-1 The present application also relates to the novel process for the preparation of 1-(2,2-difluoro-2H-1,3-benzodioxol- 5-yl)- N- {1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2- (1-hydroxy-2-methylpropan-2-yl)- 1H-indol-5-yl} cyclopropane-1-carboxamide compound of formula-1.
NOVEL PROCESSES FOR PREPARATION OF TEZACAFTOR
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, (2021/08/14)
The present invention generally relates to processes for preparation of Tezacaftor and pharmaceutical composition comprising the same. The present invention also encompasses novel intermediates of tezacaftor, processes for its preparation and use of said intermediates in the preparation of tezacaftor.
SOLID FORMS OF TEZACAFTOR, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Page/Page column 34, (2021/05/21)
The present invention relates to solid forms of Tezacaftor, including its co-crystals, solvates, hydrates and/or polymorphs, processes for their preparation, pharmaceutical compositions containing the same and use of such solid forms of Tezacaftor in the preparation of another form of Tezacaftor such as amorphous form of Tezacaftor. The present invention also provides stable amorphous form of Tezacaftor, its preparation and pharmaceutical composition containing the same.
Processes for the Preparation of Tezacaftor and Intermediates Thereof
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Paragraph 0178-0180, (2020/08/12)
The present invention provides processes for the preparation of Tezacaftor, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (3), and its conversion to Tezacaftor (1).
METHODS OF TREATMENT FOR CYSTIC FIBROSIS
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, (2020/06/05)
This application describes methods of treating cystic fibrosis or a CFTR mediated disease comprising administering Compound I or a pharmaceutically acceptable salt thereof. (I) The application also describes pharmaceutical compositions comprising Compound I or a pharmaceutically acceptable salt thereof and optionally comprising one or more additional CFTR modulating agents.
METHODS OF TREATMENT FOR CYSTIC FIBROSIS
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, (2020/12/11)
This application describes methods of treating cystic fibrosis comprising administering Compound I:, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising any of the foregoing.
Preparation method of 5-substituted cyclopropyl formylamino indole derivative
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Paragraph 0107; 0108, (2020/10/21)
The invention provides a preparation method of a 5-substituted cyclopropyl formylamino indole derivative, and particularly relates to a preparation method of Tezaacaftor. 2-nitro-4-fluoro-5-halogenated phenylacetonitrile is used as an initial raw material, and the Tezaacaftor is obtained through an ammonia substitution reaction, an amidation reaction, a dehydration condensation reaction, a reduction cyclization reaction-elimination reaction, a ring-opening substitution reaction and a catalytic hydrogenolysis reaction. The method has the advantages of cheap and easily available raw materials, short reaction steps, simple and safe preparation method, easy realization and low cost; the design of the route provided by the invention fully combines the inherent characteristics of functional group reaction, ensures proper reaction activity and high selectivity of each step of unit, and provides essential guarantee for high yield and high purity of the product; the method is high in route atomeconomy, high in product yield and purity, low in waste acid and waste water yield, environmentally friendly and suitable for industrial production.
Tezacaftor intermediate II preparation method
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Paragraph 0042, (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.
METHODS OF TREATMENT FOR CYSTIC FIBROSIS
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, (2019/02/06)
Compound I of the formula (I) and/or pharmaceutically acceptable salt(s) of Compound I comprised in a pharmaceutical composition and methods of using the same to treat cystic fibrosis.
![(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](/upload/2026/7/fe310920-fd2d-45ba-9238-1005fb677f67.png)
