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US 2026/0103446 A1Published application
Cftr regulators and methods of use thereof
AssigneeThe Regents of the University of California
InventorsAlan S. VERKMAN, Marc H. LEVIN, Onur CIL, Sujin LEE
Life of this patent
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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.
Claims19
(canceled)
A process for preparing a compound of Formula (1):
- wherein:
- X is H, F, Cl, NO2, or CO2H;
- and
- R is CH(CF3)2 or CH2CF2CHF2;
- the process comprising
- (i) reacting cyanuric chloride with 1,1,1,3,3,3-hexafluoroisopropanol or 2,2,3,3-tetrafluoro-1-propanol to provide an intermediate (A):
- (ii) reacting the intermediate (A)) with diethyl amine to provide an intermediate (B):
- and
- (iii) heating the intermediate (B) with an intermediate (C) to provide the compound of Formula (1):
6 more elements
A process for preparing a compound of Formula (2):
- wherein, Y is O or S;
- comprising
- (i) reacting cyanuric chloride with 1,1,1,3,3,3-hexafluoroisopropanol or 2,2,3,3-tetrafluoro-1-propanol to provide an intermediate (A):
- wherein, R is CH(CF3)2 or CH2CF2CHF2;
- (ii) reacting the intermediate (A) with diethyl amine to provide an intermediate (B):
- and
- (iii) heating the intermediate (B) with intermediate (D) to provide the compound of Formula (2):
4 more elements
A process for preparing a compound of Formula (3):
- the process comprising
- (i) reacting cyanuric chloride with 1,1,1,3,3,3-hexafluoroisopropanol or 2,2,3,3-tetrafluoro-1-propanol to provide an intermediate (A):
- wherein, R is CH(CF3)2 or CH2CF2CHF2;
- (ii) reacting the intermediate (A) with diethyl amine to provide an intermediate (B):
- and
- (iii) heating the intermediate (B) with 5-NH2-indazole or 6-NH2-indazole to provide the compound of Formula (3).
3 more elements
A process for preparing a compound of Formula (4):
- wherein, R is CH(CF3)2 or CH2CF2CHF2;
- the process comprising
- (i) reacting cyanuric chloride with CH3NH2 to provide an intermediate (E):
- (ii) reacting the intermediate (E) with 1,1,1,3,3,3-hexafluoroisopropanol or 2,2,3,3-tetrafluoro-1-propanol to provide an intermediate (F):
- and
- (iii) reacting the intermediate (F) with aniline to provide the compound of Formula (4).
3 more elements
Dependencies are inferred from the claim text.