发明名称 Pharmaceutical Compositions and Administrations Thereof
摘要 The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.;
申请公布号 US2015164881(A1) 申请公布日期 2015.06.18
申请号 US201514629097 申请日期 2015.02.23
申请人 Vertex Pharmaceuticals Incorporated 发明人 Van Goor Fredrick F.;Alargova Rossitza Gueorguieva;Alcacio Tim Edward;Binch Hayley Marie;Botfield Martyn Curtis;Fanning Lev Tyler Dewey;Grootenhuis Peter Diederik Jan;Hurley Dennis James;Kadiyala Irina Nikolaevna;Kaushik Ritu Rohit;Keshavarz-Shokri Ali;Krawiec Mariusz;Lee Elaine Chungmin;Luisi Brian;Medek Ales;Numa Mehdi;Sheth Urvi Jagdishbhai;Silina Alina;Verwijs Marinus Jacobus;Yang Xiaoqing;Young Christopher Ryan;Zaman Noreen Tasneem;Zhang Beili;Zhang Yuegang;Zlokarnik Gregor
分类号 A61K31/4709;A61K31/404;C12Q1/34;A61K31/443 主分类号 A61K31/4709
代理机构 代理人
主权项 1. A pharmaceutical composition comprising: A Compound of Formula I or pharmaceutically acceptable salts thereof, wherein: ring A is selected from: 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 one or both of the following: B. A Compound of Formula II or pharmaceutically acceptable salts thereof, wherein: T is —CH2—, —CH2CH2—, —CF2—, —C(CH3)2—, or —C(O)—; R1′ is H, C1-6 aliphatic, halo, CF3, CHF2, O(C1-6 aliphatic); and RD1 or RD2 is ZDR9 wherein:ZD is a bond, CONH, SO2NH, SO2N(C1-6 alkyl), CH2NHSO2, CH2N(CH3)SO2, CH2NHCO, COO, SO2, or CO; andR9 is H, C1-6 aliphatic, or aryl; and/or C. A Compound of Formula III or pharmaceutically acceptable salts thereof, wherein: R is H, OH, OCH3 or two R taken together form —OCH2O— or —OCF2O—; R4 is H or alkyl; R5 is H or F; R6 is H or CN; R7 is H, —CH2CH(OH)CH2OH, —CH2CH2N+(CH3)3, or —CH2CH2OH; R8 is H, OH, —CH2CH(OH)CH2OH, —CH2OH, or R7 and R8 taken together form a five membered ring.
地址 Boston MA US