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Pyrazine derivatives as modulators of epithelial sodium channel (ENAC)

机译:吡嗪衍生物作为上皮钠通道(ENAC)的调节剂

摘要

Pyrazine derivatives relates to compounds of formula (i), wherein R1 is H or c1-c4 alkyl, M is 1 or 2; is phenyl or heterociclilo; X is - C (= o) -, - C (= o) - NR4.Among others, N is 2 or 3; R2 is H, or C1 C8 alkyl alkyl; R3 is C5 C6 Oh where is substituted alkyl; R4 is H or c1-c4 alkyl.Preferred compounds are: 3.5 - diamino - 6 - Chloro - (R) - N - (2 - (2-methylbenzyl) - 3 - (((1 - (3 - ((2S, 3R, 4R) - - tetrahidroxipentil 2,3,4,5) amino) propanoil) piperidin-4-yl yl) methyl) Amine) propyl) pyrazine-2-carboxamide; 35 - diamino - 6 - Chloro - (N - (R) - 3 - ((4 - ((2 - (Hexyl ((2S, 3R, 4R) - - tetrahidroxipentil 2,3,4,5) amino) ethyl) Carbamoyl) benzyl) amino) - 2 - (2-methylbenzyl) propyl) pyrazine - 2 - carboxamide; among others.It also relates to a combination that includes.These compounds are modulators of epithelial sodium channel (ENAC) being useful in the treatment of diseases such as cystic fibrosis, Asthma, COPD, among others
机译:吡嗪衍生物涉及式(i)的化合物,其中R 1为H或c1-c4烷基,M为1或2;是苯基或杂环基; X是-C(= o)-,-C(= o)-NR4,其中N是2或3; R2是H或C1〜C8烷基的烷基; R3是C5,C6哦,其中是取代的烷基; R 4为H或c1-c4烷基。优选的化合物为:3.5-二氨基-6-氯-(R)-N-(2--(2-甲基苄基)-3-(((1-(3-((2S, 3R,4R)--四氢哌啶2,3,4,5)氨基)丙油)哌啶-4-基yl)甲基)胺)丙基)吡嗪-2-羧酰胺; 35-二氨基-6-氯-(N-(R)-3-((4-((2-(己基((2S,3R,4R)--四氢噻吩地2,3,4,5)氨基)乙基)氨基甲酰基)苄基)氨基)-2-(2-甲基苄基丙基)吡嗪-2-羧酰胺;这些化合物是上皮钠通道(ENAC)的调节剂,可用于治疗诸如囊性纤维化,哮喘,COPD等疾病

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