发明名称 Modulators of ATP-binding cassette transporters
摘要 The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, 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 US9090619(B2) 申请公布日期 2015.07.28
申请号 US201414446870 申请日期 2014.07.30
申请人 Vertex Pharmaceuticals Incorporated 发明人 Hadida-Ruah Sara;Hazlewood Anna;Grootenhuis Peter;Van Goor Fredrick;Singh Ashvani;Zhou Jinglan;McCartney Jason
分类号 C07C209/00;C07C211/17;C07C215/28;C07D471/10;C07C215/76;C07D209/08;C07D209/14;C07D209/18;C07D209/42;C07D209/94;C07D213/20;C07D213/73;C07D215/227;C07D215/38;C07D215/56;C07D217/06;C07D223/16;C07D265/36;C07D279/16;C07D311/58;C07D401/12;C07D401/14;C07D405/12;C07D409/12;C07D413/12;C07D417/12;C07D215/233;A61K8/49;A61K31/47;A61K31/4709;A61K45/06;C07C215/78;C07C217/84;C07D209/12;C07D209/20;A61K31/136;A61K31/265;A61K31/352;A61K31/404;A61K31/4045;A61K31/4747;A61K31/55;C07C219/34;G01N33/566;G01N33/487;G01N33/50;G01N33/68 主分类号 C07C209/00
代理机构 Honigman Miller Schwartz and Cohn LLP 代理人 Honigman Miller Schwartz and Cohn LLP ;Forbes Christopher C.;O'Brien Jonathan P.
主权项 1. A compound having formula A-I: or a salt thereof; wherein: G1 is hydrogen, R′, C(O)R′, C(S)R′, S(O)R′, S(O)2R′, Si(CH3)2R′, P(O)(OR′)3, P(S)(OR′)3, or B(OR′)2;G2 is halo, CN, CF3, isopropyl, or phenyl wherein said isopropyl or phenyl is optionally substituted with up to 3 substituents independently selected from WRW;G3 is an isopropyl or a C3-C10 cycloaliphatic ring, wherein said G3 is optionally substituted with up to 3 substituents independently selected from WRW;provided that when G1 is methyl, G3 is tert-butyl, then G2 is not 2-amino-4-methoxy-5-tert-butyl-phenyl;W is a bond or is an optionally substituted C1-C6 alkylidene chain, wherein up to two methylene units of W are optionally and independently replaced by —CO—, —CS—, —COCO—, —CONR′—, —CONR′NR′—, —CO2—, —OCO—, —NR′CO2—, —O—, —NR′CONR′—, —OCONR′—, —NR′NR′, —NR′NR′CO—, —NR′CO—, —S—, —SO, —SO2—, —NR′—, —SO2NR′—, NR′SO2—, or —NR′SO2NR′—;RW is independently R′, halo, NO2, CN, CF3, or OCF3; andR′ is independently selected from hydrogen or an optionally substituted group selected from a C1-C8 aliphatic group, a 3-8-membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or two occurrences of R′ are taken together with the atom(s) to which they are bound to form an optionally substituted 3-12 membered saturated, partially unsaturated, or fully unsaturated monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur.
地址 Boston MA US