IP Library Granted Patent US 10,111,964
Granted Patent B2
US 10,111,964 · App. 15/842,712 · Granted Oct 30, 2018

Compounds and compositions for the treatment of ocular disorders

Inventors: Jeffrey L. Cleland (San Carlos, CA); Ming Yang (Lutherville-Timonium, MD); John G. Bauman (El Sobrante, CA); Nu Hoang (Annapolis, MD); Emmett Cunningham (Hillsborough, CA)
Assignee: Graybug Vision, Inc.
A61K47/54A61K47/481A61K47/542A61K47/543A61K47/55A61K47/59A61K47/593A61K47/60C07C69/73C07D403/06C07D495/04C07D513/04H05K999/99C07C2601/08
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Quick Facts
Patent No.
US 10,111,964
App. No.
15/842,712
Granted
Oct 30, 2018
Kind
B2
Abstract

The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

Claims (43)

1. A compound of Formula XV:

or a pharmaceutically acceptable salt thereof;

wherein:

R 32 is R 35 ;

R 35 is selected from

x and y are integers independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, and 30.

2. The compound of claim 1 , wherein x and y are independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, and 12.

3. The compound of claim 2 , wherein y is selected from 1, 2, 3, 4, 5, or 6.

4. The compound of claim 2 , wherein x is 1 and y is selected from 1, 2, 3, 4, 5, or 6.

5. The compound of claim 2 , wherein x is 2 and y is selected from 1, 2, 3, 4, 5, or 6.

6. The compound of claim 2 , wherein x is 1 and y is 1.

7. The compound of claim 2 , wherein x is 1 and y is 2.

8. The compound of claim 2 , wherein x is 1 and y is 3.

9. The compound of claim 2 , wherein x is 1 and y is 4.

10. The compound of claim 1 , wherein R 35 is

11. The compound of claim 10 , wherein x and y are independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, and 12.

12. The compound of claim 11 , wherein y is selected from 1, 2, 3, 4, 5, or 6.

13. The compound of claim 11 , wherein x is 1 and y is selected from 1, 2, 3, 4, 5, or 6.

14. The compound of claim 11 , wherein x is 2 and y is selected from 1, 2, 3, 4, 5, or 6.

15. The compound of claim 13 , wherein x is 1 and y is 1.

16. The compound of claim 13 , wherein x is 1 and y is 2.

17. The compound of claim 13 , wherein x is 1 and y is 3.

18. The compound of claim 13 , wherein x is 1 and y is 4.

19. The compound of claim 1 , wherein R 35 is

20. The compound of claim 19 , wherein x and y are independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, and 12.

21. The compound of claim 20 , wherein y is selected from 1, 2, 3, 4, 5, or 6.

22. The compound of claim 19 , wherein x is 1 and y is selected from 1, 2, 3, 4, 5, or 6.

23. The compound of claim 19 , wherein x is 2 and y is selected from 1, 2, 3, 4, 5, or 6.

24. The compound of claim 19 , wherein x is 1 and y is 1.

25. The compound of claim 19 , wherein x is 1 and y is 2.

26. The compound of claim 19 , wherein x is 1 and y is 3.

27. The compound of claim 19 , wherein x is 1 and y is 4.

28. The compound of claim 1 of the formula

or a pharmaceutically acceptable salt thereof.

29. A pharmaceutical composition comprising a compound of claim 1 in a pharmaceutically acceptable carrier.

30. A method for the treatment of an ocular disorder treatable with both a beta-blocker and a tyrosine kinase inhibitor comprising administering a therapeutically effective amount of a compound or pharmaceutically acceptable salt thereof of claim 1 to a host in need thereof wherein the disorder is selected from glaucoma, age-related macular degeneration (AMD), a disorder related to an increase in intraocular pressure (IOP), a disorder related to neuroprotection, diabetic retinopathy, or optic nerve damage caused by high intraocular pressure (IOP).

31. The method of claim 30 , wherein the disorder is glaucoma.

32. The method of claim 30 , wherein the disorder is related to an increase in intraocular pressure (IOP).

33. The method of claim 30 , wherein the disorder is optic nerve damage caused by high intraocular pressure (IOP).

34. The method of claim 30 , wherein the disorder is related to neuroprotection.

35. The method of claim 30 , wherein the host is a human.

36. The method of claim 30 , wherein the compound is administered via intravitreal, intrastromal, intracameral, sub-tenon, sub-retinal, retro-bulbar, peribulbar, suprachoroidal, choroidal, subchoroidal, conjunctival, subconjunctival, episcleral, posterior juxtascleral, circumcorneal, or tear duct injection.

37. The method of claim 36 , wherein the compound is administered via intravitreal injection.

Assignments (3)
CHANGE OF NAME Recorded Aug 19, 2025
From: GRAYBUG VISION, INC.
To: CALCIMEDICA, INC.
Reel/Frame 072498/0491 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 2, 2018
From: CLELAND, JEFFREY L.; YANG, MING; BAUMAN, JOHN G.; HOANG, NU; CUNNINGHAM, EMMETT
To: GRAYBUG VISION, INC.
Reel/Frame 044518/0429 →
CHANGE OF NAME Recorded Jan 2, 2018
From: GRAYBUG, INC.
To: GRAYBUG VISION, INC.
Reel/Frame 044981/0741 →
Continuity (4)
Continuation 15782744 · Oct 12, 2017
Division 15273686 · Sep 22, 2016
Provisional Application 62222095 · Sep 22, 2015
Related Publication 20180104350A1 · Apr 19, 2018