New cystic fibrosis transmembrane conductance regulator inhibitor

A technology of atoms and compounds, applied in the field of medicine, can solve the problems of undiscovered treatment methods, death, and decreased fertility of female CF patients.

Inactive Publication Date: 2015-07-22
CHENGDU UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to respiratory problems, CF patients often suffer from typical gastrointestinal problems and pancreatic insufficiency, which can lead to death if left untreated
In addition, most men with CF are infertile and women with CF have reduced ferti...

Method used

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  • New cystic fibrosis transmembrane conductance regulator inhibitor
  • New cystic fibrosis transmembrane conductance regulator inhibitor
  • New cystic fibrosis transmembrane conductance regulator inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0025] Example: N-(5-(1-sec-butyl-6-oxo-1,6-dihydropyridin-3-yl)-4-(2,4-difluorophenyl)-1H-imidazole- 2-yl) preparation of cyclopropyl formamide

[0026]

[0027] The first step: 2-bromo-1-(2,4-difluorophenyl)ethanone

[0028]

[0029] Copper bromide (28.6 g, 128.0 mmol) was added to a mixed solution of 1-(2,4-difluorophenyl)ethanone (10.0 g, 64.0 mmol) in chloroform (100 mL) and ethanol (80 mL). The oil bath was heated to 80° C., and the reaction was kept for about 10 hours. Insoluble matter was removed by filtration, ethyl acetate (200 mL) was added, and the resulting mixed solution was washed successively with saturated brine (200 mL*2) and saturated sodium sulfite solution (200 mL*2). The organic phase was dried over anhydrous sodium sulfate, filtered, and the solvent was evaporated under reduced pressure to obtain 13.2 g of a yellow oily substance, namely 2-bromo-1-(2,4-difluorophenyl)ethanone, with a yield of 87.8%. MS: m / z=235.0, 237.0 (M+H + ).

[0030] The ...

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PUM

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Abstract

The invention relates to amidoimidazole coupled dihydropyridone compounds represented by formula I, and/or medicinal salts thereof, a preparation method of the compounds and/or the medicinal salt a use of the compounds and/or the medicinal salts thereof in the treatment and/or prevention of cystic fibrosis (CF) related hereditary diseases induced by cystic fibrosis transmembrane conductance regulator (CFTR) gene mutation, and a medicinal composition containing the compounds and/or the medicinal salts thereof. In the formula I, R<1> and R<2> are respectively independently selected from H, cyan groups, trifluoromethyl groups, halogens, (C1-C6) straight chain or branched chain alkyl groups, C3-12 alicyclic groups, phenyl groups, other (C5-C10) aryl groups, (C5-C10) heteroaryl groups or (C3-C7) heterocyclic groups.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to a dihydropyridone imidazole compound and a physiologically acceptable salt thereof described in the claims, their preparation and their use in the treatment and / or prevention of cystic fibrosis Among the diseases related to male infertility caused by hypertrophy, abnormally increased intestinal secretion, secretory diarrhea, polycystic kidney disease, chronic obstructive pulmonary disease, chronic bronchitis, mucopolysaccharidosis, and congenital bilateral absence of the vas deferens (CBAVA) use. technical background [0002] Cystic fibrosis transmembrane conductance regulator (English for cystic fibrosis transmembrane conductance regulator, abbreviated as CFTR) is a member of the ATP binding cassette (English for ATP binding cassette, abbreviated as ABC) transporter superfamily, and ABC transporter has such as Absorb nutrients, eliminate toxins, mediate cell-to-cel...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/4439A61P1/00A61P1/12A61P13/12A61P11/00A61P29/00A61P3/08A61P15/08A61P43/00
CPCC07D401/04
Inventor 周立宏
Owner CHENGDU UNIVERSITY OF TECHNOLOGY
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