| 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 | US8785640(B2) | 申请公布日期 | 2014.07.22 |
| 申请号 | US201313944171 | 申请日期 | 2013.07.17 |
| 申请人 | Vertex Pharmaceuticals Incorporated | 发明人 | Binch Hayley;Fanning Lev T. D.;Hurley Dennis;Sheth Urvi;Silina Alina;Yang Xiaoqing;Botfield Martyn;Grootenhuis Peter D. J.;Van Goor Fredrick;Numa Mehdi Michel Djamel |
| 分类号 | C07D221/22;C07D215/56 | 主分类号 | C07D221/22 |
| 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 process for preparing a compound of Formula (Ic): or pharmaceutically acceptable salts thereof, wherein the process comprises: (a) reacting the acid of formula 1d with an amine of formula 2c to provide a compound of Formula (Ic) wnerein:ring A is selected from: wherein R1 is —CF3, —CN, or —C≡CCH2N(CH3)2; R2 is hydrogen, —CH3, —CF3, —OH, or —CH2OH; R3 is hydrogen, —CH3, —OCH3, or —CN; provided that both R2 and R3 are not simultaneously hydrogen, and 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). | ||
| 地址 | Boston MA US | ||