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Last Updated: December 19, 2025

Claims for Patent: 8,865,902


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Summary for Patent: 8,865,902
Title:Deuterated CFTR potentiators
Abstract:This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
Inventor(s):Adam J. Morgan
Assignee:Vertex Pharmaceuticals Europe Ltd, Sun Pharmaceutical Industries Inc
Application Number:US14/082,843
Patent Claims: 1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein each of X1, X2, X3, X4, X5, X6, and X7 is independently hydrogen or deuterium; each of Y1, Y2, Y3, Y4, Y5, and Y6 is independently CH3 or CD3; provided that if each of Y1, Y2, Y3, Y4, Y5, and Y6 is CH3, then at least one of X1, X2, X3, X4, X5, X6, and X7 is deuterium.

2. The compound of claim 1, wherein X1, X2, X3, and X4 are each hydrogen.

3. The compound of claim 2, wherein X6 and X7 are each hydrogen.

4. The compound of claim 2, wherein Y1, Y2, and Y3 are the same.

5. The compound of claim 2, wherein Y4, Y5, and Y6 are the same.

6. The compound of claim 1, wherein X5 is deuterium.

7. The compound of claim 3, wherein at least one of C(Y1)(Y2)(Y3)) and C(Y4)(Y5)(Y6) is C(CD3)3.

8. The compound of claim 7, wherein Y1, Y2, and Y3 are CD3.

9. The compound of claim 8, wherein Y4, Y5, and Y6 are CD3.

10. The compound of claim 1, wherein the compound of Formula I is any one of the compounds of the table below, Cmpd # X1 X2 X3 X4 X5 X6 X7 Y1 Y2 Y3 Y4 Y5 Y6 100 D D D D D D D CD3 CD3 CD3 CD3 CD3 CD3 101 H H H H D H H CD3 CD3 CD3 CD3 CD3 CD3 102 H H H H D H H CD3 CD3 CD3 CH3 CH3 CH3 103 H H H H D H H CH3 CH3 CH3 CD3 CD3 CD3 104 H H H H D H H CH3 CH3 CH3 CH3 CH3 CH3 105 H H H H H H H CD3 CD3 CD3 CD3 CD3 CD3 106 H H H H H H H CD3 CD3 CD3 CH3 CH3 CH3 107 H H H H H H H CH3 CH3 CH3 CD3 CD3 CD3 or a pharmaceutically acceptable salt thereof, wherein any atom not designated as deuterium is present at its natural isotopic abundance.

11. The compound of claim 1, wherein the compound of Formula I is any one of the compounds of the table below, Cmpd # X1 X2 X3 X4 X5 X6 X7 Y1 Y2 Y3 Y4 Y5 Y6 110 H H H H H D D CD3 CD3 CD3 CD3 CD3 CD3 111 H H H H D D D CD3 CD3 CD3 CD3 CD3 CD3 112 H H H H D D D CD3 CD3 CD3 CH3 CH3 CH3 113 H H H H D D D CH3 CH3 CH3 CD3 CD3 CD3 114 H H H H D D D CH3 CH3 CH3 CH3 CH3 CH3 115 H H H H H D D CD3 CD3 CD3 CH3 CH3 CH3 116 H H H H H D D CH3 CH3 CH3 CD3 CD3 CD3 117 D D D D D D D CD3 CD3 CD3 CH3 CH3 CH3 118 D D D D D D D CH3 CH3 CH3 CD3 CD3 CD3 119 D D D D D H H CD3 CD3 CD3 CH3 CH3 CH3 120 D D D D D H H CH3 CH3 CH3 CD3 CD3 CD3 121 H H H H H H D CD3 CD3 CD3 CD3 CD3 CD3 122 H H H H H H D CD3 CD3 CD3 CH3 CH3 CH3 123 H H H H H H D CH3 CH3 CH3 CD3 CD3 CD3 or a pharmaceutically acceptable salt thereof, wherein any atom not designated as deuterium is present at its natural isotopic abundance.

12. The compound of claim 1, wherein the compound of Formula I is any one of the compounds of the table below, Cmpd # X1 X2 X3 X4 X5 X6 X7 Y1 Y2 Y3 Y4 Y5 Y6 124 H H H H H D H CD3 CD3 CD3 CD3 CD3 CD3 125 H H H H H D H CD3 CD3 CD3 CH3 CH3 CH3 126 H H H H H D H CH3 CH3 CH3 CD3 CD3 CD3 or a pharmaceutically acceptable salt thereof, wherein any atom not designated as deuterium is present at its natural isotopic abundance.

13. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

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