RIPA, Lena Elisabeth,NIKITIDIS, Grigorios,LUNDKVIST, Johan Rune Michael,KRISTOFFERSSON, Anna,HEMMERLING, Martin,BERGLUND, Susanne Elisabeth,CONNOLLY, Stephen,SHAMOVSKY, Igor,HOSSAIN, Nafizal
申请号:
PE2016001600
公开号:
PE20170205A1
申请日:
2015.03.17
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
Pyridine compound extracted from formula (I),R1 is h or C1-C4 tar; m is 1 or 2; a is phenyl or isopropyl; X is C (= O) -,-C(=O)-NR4--Among others, n is 2 or 3; R2 is h or C1-C8 tar; R3 is c5-c6-oh tar, wherein the tar is replaced; R4 is h or C1-C4 tar. The most popular compounds are: 3, 5-diamin-6-chloro-n - ((R) - 2 - (2-methylphenyl) - 3 - ((1 - (3 - ((2 s, 3R, 4R) - 2, 3, 4, 4, 5-tetrahydropentabenzo (TETRA) amine (c) propane (1) pichia-4-il) methyl (toluene) amine (1) pyr-2-carbox amine; 3, 5-diamin-6-chloro-n - ((R) - 3 - (4 - (4 ------ - (2, 3 --------- (2, 3)------- 5-tetrahypentil) amino (ethyl) carbamoil (bencil) bencil) - 2 - (2-methylbencil) propil) pirazina-2-carboxamida, etc. He also said that a combination can understand it These compounds are modulators of epinephrine (ENaC), which can be used to treat asthma and other diseases.Cystic fibrosis and othersSe refiere a compuestos derivados de pirazina de formula (I), en donde R1 es H o alquilo C1-C4; m es 1 o 2; A es fenilo o heterociclilo; X es -C(=O)-, -C(=O)-NR4-, entre otros; n es 2 o 3; R2 es H o alquilo C1-C8; R3 es alquilo C5-C6-OH, donde dicho alquilo esta sustituido; R4 es H o alquilo C1-C4. Son compuestos preferidos: 3,5-diamino-6-cloro-N-((R)-2-(2-metilbencil)-3-(((1-(3-(((2S,3R,4R)-2,3,4,5-tetrahidroxipentil)amino)propanoil)piperidin-4-il)metil)amino)propil)pirazina-2-carboxamida; 3,5-diamino-6-cloro-N-((R)-3-((4-((2-(hexil((2S,3R,4R)-2,3,4,5-tetrahidroxipentil)amino)etil)carbamoil)bencil)amino)-2-(2-metilbencil)propil)pirazina-2-carboxamida; entre otros. Tambien se refiere a una combinacion que la comprende. Dichos compuestos son moduladores del canal de sodio epitelial (ENaC) siendo utiles en el tratamiento de enfermedades tales como asma, fibrosis quistica, COPD, entre otras