IP Library Granted Patent US 9,353,123
Granted Patent B2
US 9,353,123 · App. 14/184,886 · Granted May 31, 2016

Therapeutic compounds and uses thereof

Inventors: Winston Zapanta Ong (Stoneham, MA); Pawel Wojciech Nowak (Woodcliff Lake, NJ); Ben C. Askew (Marshfield, MA); Jinsoo Kim (Brighton, MA)
Assignee: Kala Pharmaceuticals, Inc.
C07D491/107C07D403/12
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,353,123
App. No.
14/184,886
Granted
May 31, 2016
Kind
B2
Abstract

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

Claims (76)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is hydrogen or optionally substituted C 1-6 alkyl;

R 2 is optionally substituted heterocyclyl having 1 or 2 heteroatoms;

X is a bond, —O—, or —C(═O)—;

Y is N;

R 3 is optionally substituted heteroaryl; and

n is 0, 1, 2, 3, or 4.

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

or a pharmaceutically acceptable salt thereof, wherein:

each instance of R 4 is independently selected from the group consisting of hydrogen, optionally substituted C 1-6 alkyl, F, CI, Br, I, CN, OH, and alkoxy;

R 5 is hydrogen or a nitrogen protecting group; and

m is 0, 1, 2, 3, 4, or 5.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , wherein the compound is of Formula (II-b2):

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 1 , wherein the compound is of Formula (II-b3):

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 1 , wherein the compound is of Formula (II-b4):

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , wherein the compound is of Formula (II-d1):

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 1 , wherein the compound is of Formula (II-d2):

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 , wherein the compound is of Formula (II-d3):

or a pharmaceutically acceptable salt thereof.

14. The compound of claim 1 , wherein the compound is of Formula (II-d4):

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof, wherein:

each instance of R 4 is independently selected from the group consisting of hydrogen, optionally substituted C 1-6 alkyl, F, Cl, Br, I, CN, OH, and alkoxy;

R 5 is hydrogen or nitrogen protecting group; and

m is 0, 1, 2, 3, or 4.

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

or a pharmaceutically acceptable salt thereat.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

19. The compound of claim 1 , wherein the compound is of Formula (III-b2):

or a pharmaceutically acceptable salt thereof.

20. The compound of claim 1 , wherein the compound is of Formula (III-b3).

or a pharmaceutically acceptable salt thereof.

21. The compound of claim 1 , wherein the compound is of Formula (III-b4):

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

24. The compound of claim 1 , wherein the compound is of Formula (III-d1):

or a pharmaceutically acceptable salt thereof.

25. The compound of claim 1 , wherein the compound is of Formula (III-d2):

or a pharmaceutically acceptable salt thereof.

26. The compound of claim 1 , wherein the compound is of Formula (III-d3):

or a pharmaceutically acceptable salt thereof.

27. The compound of claim 1 , wherein the compound is of Formula (III-d4):

or a pharmaceutically acceptable salt thereof.

28. The compound of claim 2 , wherein R 5 is hydrogen.

29. The compound of claim 1 , wherein R 2 is

wherein each instance of p, q, s, and t is independently 0, 1, 2, 3, or 4.

30. The compound of claim 29 , wherein R 2 is

31. The compound of claim 29 , wherein R 2 is

32. The compound of claim 29 , wherein R 2 is

33. The compound of claim 1 having one of the following structures:

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

35. A compound represented by a formula:

or a pharmaceutically acceptable salt thereof.

Assignments (8)
CHANGE OF NAME Recorded Sep 21, 2023
From: KALA PHARMACEUTICALS, INC.
To: KALA BIO, INC.
Reel/Frame 065017/0488 →
FIRST AMENDMENT TO IP SECURITY AGREEMENT Recorded Dec 22, 2022
From: KALA PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC
Reel/Frame 062205/0883 →
SECURITY INTEREST Recorded May 6, 2021
From: KALA PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC
Reel/Frame 056168/0602 →
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENTS AT REEL AND FRAME: 047602 / 0480 & 047172 / 0481 Recorded May 5, 2021
From: ATHYRIUM OPPORTUNITIES III ACQUISITION LP
To: KALA PHARMACEUTICALS, INC
Reel/Frame 056151/0092 →
SECURITY INTEREST Recorded Oct 1, 2018
From: KALA PHARMACEUTICALS, INC.
To: ATHYRIUM OPPORTUNITIES III ACQUISITION LP
Reel/Frame 047172/0481 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2014
From: ONG, WINSTON ZAPANTA; NOWAK, PAWEL WOJCIECH; KIM, JINSOO
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 032861/0803 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2014
From: ASKEW, BEN
To: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
Reel/Frame 032861/0868 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2014
From: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 032861/0976 →
Continuity (3)
Provisional Application 61767087 · Feb 20, 2013
Provisional Application 61898741 · Nov 1, 2013
Related Publication 20140235657A1 · Aug 21, 2014