CFTR regulators and methods of use thereof
AssigneeThe Regents of the University of California
InventorsAlan S. Verkman, Marc H. Levin, Onur Cil, Sujin Lee
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Abstract
Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders, and other diseases and disorders.
Claims17
A method of treating a dry eye disorder in a subject in need thereof, comprising administering to the subject an effective amount a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X is —O-;
- R2 is C2-C4 haloalkyl substituted with at least four fluorines, substituted heteroalkyl, or unsubstituted heteroalkyl;
- R3 is hydrogen;
- R4 is substituted or unsubstituted alkyl;
- R5 is hydrogen;
- and
- R′, R6, R7, R8 and R9 are each hydrogen.
A method of increasing lacrimation in a subject in need thereof, comprising administering to the subject an effective amount of a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X is —O-;
- R2 is C2-C4 haloalkyl substituted with at least four fluorines, substituted heteroalkyl, or unsubstituted heteroalkyl;
- R3 is hydrogen;
- R4 is substituted or unsubstituted alkyl;
- R5 is hydrogen;
- and
- R′, R6, R7, R8 and R9 are each hydrogen.
A method of activating a Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), comprising contacting the CFTR with an effective amount of a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X is —O-;
- R2 is C2-C4 haloalkyl substituted with at least four fluorines, substituted heteroalkyl, or unsubstituted heteroalkyl;
- R3 is hydrogen;
- R4 is substituted or unsubstituted alkyl;
- R5 is hydrogen;
- and
- R′, R6, R7, R8 and R9 are each hydrogen.
Dependencies are inferred from the claim text.