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Cftr regulators and methods of use thereof
Inactive Publication Date: 2019-01-31
RGT UNIV OF CALIFORNIA
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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.
Dry eye is a heterogeneous tear film disorder that results in eye discomfort, visual disturbance, and ocular surfacepathology, 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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embodiment p1
[0261]A pharmaceutical composition, comprising a pharmaceutically acceptable excipient, and a compound of Formula I:
or a pharmaceutically acceptable salt thereof, wherein: Ar is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; L1 and L2 are independently substituted or unsubstituted C1-C3 alkylene; n1 is an integer from 0 to 4; m1 and v1 are independently 1 or 2; R1 is hydrogen, halogen, —CX1.13, —CHX1.12, —CH2X1.1, —CN, —SOn1R1A, —SOv1NR1BR1C, —NHNR1BR1C, —ONR1BR1C, —NHC(O)NHNR1BR1C, —NHC(O)NR1BR1C, —N(O)m1, —NR1BR1C, —C(O)R1D, —C(O)OR1D, —C(O)NR1BR1C, —OR1A, —NR1BSO2R1A, —NR1BC(O)R1D, —NR1BC(O)OR1D, —NR1BOR1D, —OCX1.13, —OCHX1.12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R2 is hydrogen, halogen, —CX2.13, —CHX2.12, —CH2X2.1, —CN, —SOn1R2A, —SOv1NR2BR2C,...
embodiment p2
[0262]The pharmaceutical composition of embodiment P1, wherein: Ar is unsubstituted heteroaryl; L1 and L2 are independently —CH2—; and R1, R2, R3, R4 and R5 are independently hydrogen, —OCH3 or —OCH2CH3.
embodiment p3
[0263]The pharmaceutical composition of embodiment P2, wherein R1, R4 and R5 are independently hydrogen.
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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...
Claims
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Application Information
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