Small molecule inhibitors of pendrin ion exchange and pharmaceutical compositions
AssigneeThe Regents of the University of California
InventorsAlan S. VERKMAN, Peter M. HAGGIE, Onur CIL
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Abstract
Provided herein are small molecule inhibitors of pendrin. More specifically, the small molecules disclosed herein may be used to inhibit pendrin-mediated anion exchange. These small molecules may be used for treatment of diseases and disorders that are treatable by inhibiting pendrin, such as cystic fibrosis, rhinitis, chronic rhinosinusitis, exposure to an industrial toxin, certain viral infections, certain bacterial infections, and chronic obstructive pulmonary disease. The small molecules may further be used to potentiate a diuretic effect of a diuretic compound. The small molecules may additionally be used to treat hypertension or thyroid conditions.
Claims31
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of Formula (I):
- wherein,
- n is 0, 1, 2, or 3;
- R1 at each occurrence is the same or different and independently optionally substituted alkyl, optionally substituted alkoxy, halo, trifluoroalkyl, or optionally substituted thioalkyl;
- and
- R2 is optionally substituted aryl or optionally substituted aralkyl.
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A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a pyrazolothiophenesulfonamide compound represented by Formula (II):
- wherein,
- R5a and R5b are the same or different and independently hydrogen, or optionally substituted alkyl;
- R6 and R7 are the same or different and independently hydrogen, optionally substituted alkyl, or —S(O)2NHR, provided one of R6 and R7 is —S(O)2NHR;
- and
- R is optionally substituted aryl or optionally substituted cycloalkyl.
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Dependencies are inferred from the claim text.