Cftr regulators and methods of use thereof

Abstract

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders or other diseases and disorders.

Description

CROSS-REFERENCES TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application No. 62 / 387,591, filed Dec. 24, 2015, the contents of which is incorporated herein in its entirety and for all purposes.STATEMENT AS TO RIGHTS TO INVENTIONS MADE UNDER FEDERALLY SPONSORED RESEARCH AND DEVELOPMENT[0002]This invention was made with the government support under Grant Nos. TR000004, EY023981, EY013574, EB000415, DK035124, DK072517 and DK101373, awarded by the National Institutes of Health. The government has certain rights in the invention.BACKGROUND OF THE INVENTION[0003]Constipation is a common clinical complaint in adults and children that negatively impacts quality of life. The prevalence of chronic constipation has been estimated to be 15% in the U.S. population, with health-care costs estimated at approximately 7 billion dollars annually, with in excess of 500 million dollars spent on laxatives. The mainstay of constipation therapy includes laxatives an...

AI Technical Summary

Benefits of technology

The patent text describes compounds with specific formulas that have various uses in various applications. These compounds can be used in the production of optical materials, electronics, sensors, and other products. The compounds have specific structures that make them suitable for various uses. The technical effects of the patent text include the creation of new compounds with specific structures that can be used in various applications, and the improvement of existing compounds for use in specific applications.

Problems solved by technology

Constipation is a common clinical complaint in adults and children that negatively impacts quality of life.

There are two FDA-approved chloride channel activators, lubiprostone and linaclotide, for treatment of constipation, but clinical trials showed variable and unimpressive efficacy of both drugs.

Dry eye is a heterogeneous tear film disorder that results in eye discomfort, visual disturbance, and ocular surface pathology, and remains an unmet need in ocular disease with limited effective therapeutic options available.

The only medication currently approved for dry eye is topical cyclosporine, an anti-inflammatory that does not eliminate all symptoms in most dry eye patients.

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