发明名称 Modulators of cystic fibrosis transmembrane conductance regulator
摘要 The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
申请公布号 US8969382(B2) 申请公布日期 2015.03.03
申请号 US201314074158 申请日期 2013.11.07
申请人 Vertex Pharmaceuticals Incorporated 发明人 Binch Hayley;Fanning Lev T. D.;Botfield Martyn;Grootenhuis Peter D. J.;Van Goor Fredrick;Numa Mehdi Michel Djamel
分类号 A61K31/04;C07D401/14;C07D487/08 主分类号 A61K31/04
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 method of treating or lessening the severity of a disease in a patient, wherein said disease is selected from cystic fibrosis, smoke induced COPD, pancreatitis, pancreatic insufficiency, hereditary emphysema, COPD, and dry-eye disease, said method comprising the step of administering to said patient an effective amount of a compound of Formula I or pharmaceutically acceptable salts thereof, wherein: ring A is selected from: wherein: R1 is —CH3, —CF3 or —CN;R2 is hydrogen, —CH3, —CF3, —OH, or —CH2OH;R3 is hydrogen, —CH3, —OCH3, or —CN;Ra is hydrogen or a silyl protecting group selected from the group consisting of trimethylsilyl (TMS), tert-butyldiphenylsilyl (TBDPS), tert-butyldimethylsilyl (TBDMS), triisopropylsilyl (TIPS), and [2-(trimethylsilyl)ethoxy]methyl (SEM);provided that both R2 and R3 are not simultaneously hydrogen; andone of X and Y is nitrogen and the other is carbon.
地址 Boston MA US