New cystic fibrosis transmembrane conductance regulator inhibitor

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...

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 fertility

[0005] Although in the past few decades, modern medical efforts have made progress in the treatment of CF, which has greatly extended the life span of CF patients, but so far no safe and effective treatment methods directly targeting CFTR have been found.

Images