THERAPEUTIC COMPOUNDS AND USES THEREOF

• US 20140235634A1
• Filed: 02/14/2014
• Published: 08/21/2014
• Est. Priority Date: 02/15/2013
• Status: Active Grant

• Current Assignee: Kala Bio, Inc.
• Original Assignee: Kala Pharmaceuticals, Inc.
• Inventors: ONG, Winston Zapanta, NOWAK, Pawel Wojciech, ASKEW, Ben C., KIM, Jinsoo
• Granted Patent: US 9,353,122 B2
• Time in Patent Office: Days
• US Class Current: 514/234.5
• CPC Class Codes: A61K 31/4709 Non-condensed quinolines and containing further heterocyclic rings
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 31/506 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 31/5377 not condensed and containing further heterocyclic rings, e.g. timolol
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 239/88 Oxygen atoms
• CPC Class Codes: C07D 405/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 413/14 containing three or more hetero rings
• CPC Class Codes: C07D 491/107 with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.

Claims

1. A compound of Formula (I):

2. The compound of claim 1, wherein the compound is of Formula (II):

3. The compound of claim 1, wherein the compound is of Formula (II-a):

4. The compound of claim 1, wherein the compound is of Formula (II-b):

5. The compound of claim 1, wherein the compound is of Formula (II-c):

6. The compound of claim 1, wherein the compound is of Formula (II-c1):

7. The compound of claim 1, wherein the compound is of Formula (II-c2):

8. The compound of claim 1, wherein the compound is of Formula (II-c3):

9. The compound of claim 1, wherein the compound is of Formula (II-c4):

10. The compound of claim 1, wherein the compound is of Formula (III):

11. The compound of claim 1, wherein the compound is of Formula (III-a):

12. The compound of claim 1, wherein the compound is of Formula (III-b):

13. The compound of claim 1, wherein the compound is of Formula (III-c):

14. The compound of claim 1, wherein the compound is of Formula (III-c1):

15. The compound of claim 1, wherein the compound is of Formula (III-c2):

16. The compound of claim 1, wherein the compound is of Formula (III-c3):

17. The compound of claim 1, wherein the compound is of Formula (III-c4):

18. The compound of claim 1, wherein the compound is of Formula (IV):

19. The compound of claim 1, wherein the compound is of Formula (IV-a):

20. The compound of claim 1, wherein the compound is of Formula (IV-a1):

21. The compound of claim 1, wherein the compound is of Formula (IV-a1-i):

22. The compound of claim 1, wherein the compound is of Formula (IV-a1-ii):

23. The compound of claim 1, wherein the compound is of Formula (IV-a1-iii):

24. The compound of claim 1, wherein the compound is of Formula (IV-a1-iv):

25. The compound of claim 1, wherein the compound is of Formula (IV-b):

26. The compound of claim 1, wherein the compound is of Formula (IV-b1):

27. The compound of claim 1, wherein the compound is of Formula (IV-b1-i):

28. The compound of claim 1, wherein the compound is of Formula (IV-b1-ii):

29. The compound of claim 1, wherein the compound is of Formula (IV-b1-iii):

30. The compound of claim 1, wherein the compound is of Formula (IV-b1-iv):

31. The compound of claim 1, wherein the compound is of Formula (V):

32. The compound of claim 1, wherein the compound is of Formula (V-a):

33. The compound of claim 1, wherein the compound is of Formula (V-a1):

34. The compound of claim 1, wherein the compound is of Formula (V-a1-i):

35. The compound of claim 1, wherein the compound is of Formula (V-a1-ii):

36. The compound of claim 1, wherein the compound is of Formula (V-a1-ii):

37. The compound of claim 1, wherein the compound is of Formula (V-a1-iv):

38. The compound of claim 1, wherein the compound is of Formula (V-b):

39. The compound of claim 1, wherein the compound is of Formula (V-b1):

40. The compound of claim 1, wherein the compound is of Formula (V-b1-i):

41. The compound of claim 1, wherein the compound is of Formula (V-b1-ii):

42. The compound of claim 1, wherein the compound is of Formula (V-b1-iii):

43. The compound of claim 1, wherein the compound is of Formula (V-b1-iv):

44. The compound of claim 1, wherein R₂ is of the formula:

45. The compound of claim 44, wherein R₂ is of the formula:

46. The compound of claim 1, wherein R₂ is of the formula:

47. The compound of claim 46, wherein R₂ is of the formula:

48. The compound of claim 1 of one of the following formulae:

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

50. The pharmaceutical composition of claim 49, wherein the pharmaceutical composition is suitable for delivery to the eye.

51-64. -64. (canceled)

65. A compound of Formula (VI):