发明名称 Heteroaryl derivatives as CFTR modulators
摘要 The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
申请公布号 US8796312(B2) 申请公布日期 2014.08.05
申请号 US201213627222 申请日期 2012.09.26
申请人 Vertex Pharmaceuticals Incorporated 发明人 Hadida Ruah Sara;Miller Mark;Zhou Jinglan;Bear Brian
分类号 C07D213/75;A61K31/435 主分类号 C07D213/75
代理机构 代理人 Kelly Susan C.
主权项 1. A compound of formula I:or a pharmaceutically acceptable salt thereof, wherein: Ar1 is Ar1 is optionally substituted with w occurrences of —W—RW; wherein W is independently an optionally substituted (C1-C6) alkylidene chain wherein up to two methylene units of W are independently replaced by —CO—, —O—, —S—, —SO2—, or —NR′—;R′ is independently H, alkyl, aryl, heteroaryl, aralkyl, cycloalkyl, or heterocycloalkyl; andRW is independently H, halo, CN, NO2, NH2, CF3, OCF3, OH, alkoxy, or an optionally substituted aliphatic, cycloaliphatic, heterocyclic, or heteroaryl, wherein, when substituted, RW is substituted with up to two R2;R2 is halo, CN, NO2, CF3, OCF3, OH, —(C1-C6)alkylidene-OH, —(C1-C6)alkylidene-N(R)2, 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(OR)2, or NRSO2N(R)2;R is independently H, alkyl, cycloalkyl, heterocyclic, aryl, or heteroaryl; RN is H, alkyl, aryl, heteroaryl, aralkyl, cycloalkyl, or heterocycloalkyl; A is an optionally substituted 3-7 membered monocyclic ring; B is optionally fused to a 5-7 membered ring selected from the group consisting of cycloaliphatic, aryl, heterocyclic, and heteroaryl; J is selected from the group consisting of CH2, CF2, C(CH3)2, C(O),C(Phenyl)2, B(OH), and CH(OEt); and w is independently an integer from 0 to 5 inclusive.
地址 Boston MA US