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Pyridyl derivatives as modulators of CFTR
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
HADIDA-RUAH, SARA,MILLER, MARK,ZHOU, JINGLAN,BEAR, BRIAN,GROOTENHUIS, PETER
申请号:
ES12188920
公开号:
ES2552990T3
申请日:
2009.03.25
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: RN is H, alkyl, aryl, heteroaryl, aralkyl, cycloalkyl or heterocycloalkyl; A is a 3-membered monocyclic ring; B is optionally condensed to a 5-7 membered ring selected from the group consisting of cycloaliphatic, aryl, heterocyclic and heteroaryl; R1 is halo, alkyl, OH, alkoxy, thioalkyl, trifluoromethoxy; or two R1 in adjacent atoms that, taken together, form: ** Formula ** in which J is selected from the group consisting of CH2, CF2 or C (CH3) 2; W is, independently, an optionally substituted (C1-C6) alkylidene bond or chain, in which up to two methylene units of W are independently replaced by -O-, -S-, -SO2- or -NR'-; R 'is, independently, H, alkyl, aryl, heteroaryl, aralkyl, cycloalkyl or heterocycloalkyl; Rw is, independently, H, CN, NO2, N (R) 2, CF3, OCF3, OH, OR, C (O) N (R) 2, C (O) R, CO2R, -O (alkylidene ( C1-C6)) - OR, O (C1-C6 alkylidene) - N (R) 2, -O (C1-C6 alkylidene) - heterocycle or an aliphatic, cycloaliphatic, aryl, aryloxy, heterocyclic or heteroaryl, wherein, when substituted, Rw is substituted with up to two R2; R2 is halo, CN, NO2, CF3, OCF3, OR, OC (O) R, OC (O) N (R) 2, SR, S (O) R, SO2R, SO2N (R) 2, SO3R, C ( O) R, CO2R, C (O) N (R) 2, N (R) 2, NRC (O) R, NRCO2R, NRC (O) N (R) 2, NRSO2R, B (OH) 2 or NRSO2N ( R) 2; R is independently H, alkyl, cycloalkyl, heterocyclic, aryl or heteroaryl; n is 1 or 2; w is an integer from 0 to 4 inclusive; and x is an integer from 0 to 5 inclusive; provided that when W is a bond and Rw is cycloaliphatic, heterocycloaliphatic, aryl or heteroaryl, -W-Rw will be attached to position 3 or 4 of the pyridyl ring.Un compuesto de fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en el que: RN es H, alquilo, arilo, heteroarilo, aralquilo, cicloalquilo o heterocicloalquilo; A es un anillo monocíclico de 3 miembros; B está opcionalmente condensado a un anillo de 5-7 miembros seleccionado del grupo que c
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