IP Library › Granted Patent US 9,783,545
Granted Patent B2
US 9,783,545 · App. 15/141,949 · Granted Oct 10, 2017

Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome

Inventors: Roland Werner Bürli (Bishop's Strotford, GB); William Rameshchandra Krishna Esmieu (Cambridge, GB); Christopher James Lock (Burwell, GB); Karine Fabienne Malagu (Saffron Walden, GB); Andrew Pate Owens (Huntingdon, GB); William E Harte (Moorpark, CA)
Assignee: USHER III INITIATIVE, INC.
C07D487/04A61K31/5025C07D519/00
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Quick Facts
Patent No.
US 9,783,545
App. No.
15/141,949
Granted
Oct 10, 2017
Kind
B2
Abstract

Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.

Claims (39)

1. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

2. A composition comprising an effective amount of a compound or pharmaceutically acceptable salt of the compound of claim 1 and a pharmaceutically acceptable carrier or vehicle.

3. A method for treating a retinal degenerative disease, comprising administering to a subject in need thereof an effective amount of a compound or pharmaceutically acceptable salt of the compound of claim 1 .

4. The method of claim 3 , wherein the retinal degenerative disease is retinitis pigmentosa, Leber's congenital Amaurosis, a syndromic retinal degeneration, age-related macular degeneration or Usher Syndrome.

5. A method for treating retinitis pigmentosa, Leber's congenial Amaurosis, syndromic retinal degeneration, age-related macular degeneration or Usher Syndrome, comprising administering to a subject in need thereof an effective amount of a compound or pharmaceutically acceptable salt of the compound of Formula I, Formula II, Formula III, Formula XIII, Formula XIV or Formula XV;

wherein Formula I has the structure:

wherein R 1 is:

R 2 is:

and a is 0, 1, or 2;

wherein Formula II has the structure:

wherein R 3 is:

b is 0 or 1; and

c is 1 or 2;

wherein Formula III has the structure:

wherein R 4 is

wherein Formula XIII has the structure:

wherein R 5 is:

R 6 is:

 and

a is 0, 1, or 2;

wherein Formula XIV has the structure:

wherein R 7 is:

b is 0 or 1; and

c is 1 or 2; and

wherein Formula XV has the structure:

wherein R 8 is:

6. The method of claim 5 , wherein the Usher syndrome is Usher I Syndrome, Usher II Syndrome, or Usher III Syndrome.

7. The method of claim 5 , wherein the Usher syndrome is Usher III syndrome.

8. A method for treating retinitis pigmentosa, Leber's congenital oAmaurosis, syndromic retinal degeneration, age-related macular degeneration or Usher Syndrome, comprising administering to a subject in need thereof an effective amount of a compound having the structure:

or a pharmaceutically acceptable salt thereof, or XIIIa:

9. The method of claim 8 , wherein the Usher syndrome is Usher I Syndrome, Usher II Syndrome, or Usher III Syndrome.

10. The method of claim 8 , wherein the Usher syndrome is Usher III syndrome.

11. The method of claim 4 , wherein the retinal degenerative disease is Usher Syndrome.

12. A method for treating hearing loss associated with Usher syndrome, comprising administering to a subject in need thereof an effective amount of a compound or pharmaceutically acceptable salt of the compound of claim 1 .

13. The method of claim 12 , wherein the Usher syndrome is Usher I Syndrome, Usher II Syndrome, or Usher III Syndrome.

14. The method of claim 12 , wherein the Usher syndrome is Usher III syndrome.

15. The method of claim 11 , wherein the Usher syndrome is Usher I Syndrome, Usher II Syndrome, or Usher III Syndrome.

16. The method of claim 11 , wherein the Usher syndrome is Usher III syndrome.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: BÜRLI, ROLAND WERNER; KRISHNA ESMIEU, WILLIAM RAMESHCHANDRA; LOCK, CHRISTOPHER JAMES; MALAGU, KARINE FABIENNE; OWENS, ANDREW PATE
To: BIOFOCUS DPI LTD.
Reel/Frame 043256/0733 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: HARTE, WILLIAM E.
To: USHER III INITIATIVE, INC.
Reel/Frame 043256/0738 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: BIOFOCUS DPI LTD.
To: USHER III INITIATIVE, INC.
Reel/Frame 043256/0742 →
Continuity (4)
Continuation 14731535 · Jun 5, 2015
Division 13791744 · Mar 8, 2013
Provisional Application 61718611 · Oct 25, 2012
Related Publication 20160272647A1 · Sep 22, 2016