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US 8,314,239 B2Granted
Modulators of cystic fibrosis transmembrane conductance regulator
AssigneeVertex Pharmaceutical Incorporated
InventorsHayley Binch, Lev T. D. Fanning, Mehdi Michel Djamel Numa
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Abstract
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.
Claims24
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;
- and
- one of X and Y is nitrogen and the other is carbon.
7 more elements
A compound selected from
Dependencies are inferred from the claim text.