Azaindole derivatives as cftr modulators

A compound, heteroaryl technology, applied in the field of regulators, can solve problems such as increasing disease severity

Active Publication Date: 2010-05-26
VERTEX PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This dramatically increa...

Method used

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  • Azaindole derivatives as cftr modulators
  • Azaindole derivatives as cftr modulators
  • Azaindole derivatives as cftr modulators

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Embodiment Construction

[0172] Table 2 below contains a listing of carboxylic acid synthesis materials that are commercially available or prepared by one of the methods described below.

[0173] compound

[0174]The mixture was stirred at 70°C overnight, then the reaction mixture was diluted with water (30 mL) and extracted with ethyl acetate. The combined organic layers were dried over sodium sulfate and evaporated to dryness to yield crude 1-(2,2-difluoro-benzo[1,3]dioxol-5-yl)-cyclopropanenitrile, which was used directly in subsequent steps. Step f: 1-(2,2-difluoro-benzo[1,3]dioxol-5-yl)-cyclopropanecarboxylic acid [0007] converts 1-(2,2-difluoro- Benzo[1,3]dioxol-5-yl)-cyclopropanenitrile (crude product from previous step) was refluxed in 10% aqueous sodium hydroxide (50 mL) for 2.5 hours. The cooled reaction mixture was washed with diethyl ether (100 mL), and the aqueous phase was acidified to pH 2 with 2M hydrochloric acid. Filtration of the precipitated solid yielded 1-(2,2-difluo...

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Abstract

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

Description

[0001] technical field of invention [0002] The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including cystic fibrosis transmembrane conductance regulator ("CFTR"), compositions thereof, and related methods. The invention also relates to methods of using such modulators to treat ABC transporter mediated diseases. Background of the invention [0003] ABC transporters are a family of membrane transporters that regulate the transport of a variety of pharmacological components, potentially toxic drugs and xenobiotics, and anions. ABC transporters are homologous membrane proteins that bind and utilize cellular adenosine triphosphate (ATP) for their specific activity. Some of these transporters are found to be multidrug resistance proteins (like MDR1-P glycoprotein or multidrug resistance protein MRP1), which defend malignant cancer cells against chemotherapeutic agents. Forty-eight ABC transporters have been identifie...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61P3/00A61P25/00
CPCC07D471/04A61P11/00A61P13/02A61P13/12A61P19/00A61P21/00A61P21/04A61P25/00A61P25/14A61P25/16A61P25/28A61P27/02A61P3/00A61P35/00A61P3/06A61P3/08A61P37/06A61P43/00A61P5/00A61P5/10A61P5/14A61P5/16A61P5/18A61P7/00A61P7/04A61P7/10A61P3/10A61K31/437
Inventor S·哈迪达鲁阿周竞兰M·米勒B·贝尔
Owner VERTEX PHARMA INC
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