IP Library Granted Patent US 9,861,634
Granted Patent B2
US 9,861,634 · App. 15/139,135 · Granted Jan 9, 2018

Therapeutic compounds and uses thereof

Inventors: Winston Zapanta Ong (Waltham, MA); Pawel Wojciech Nowak (Waltham, MA); Ben C. Askew (Marshfield, MA); Jinsoo Kim (Waltham, MA)
Assignee: Kala Pharmaceuticals, Inc.
A61K31/517A61K9/0048C07D403/12C07D491/107C07D519/00
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Quick Facts
Patent No.
US 9,861,634
App. No.
15/139,135
Granted
Jan 9, 2018
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 (33)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof, wherein:

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

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

X is a bond, —O—, or —C(═O)—;

Y is CH;

R 3 is optionally substituted heteroaryl; and

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

2. The compound of claim 1 , wherein R 1 is CH 3 .

3. The compound of claim 1 , wherein R 2 is)

wherein p, q, s, and t are independently 0, 1, 2, 3, or 4.

4. The compound of claim 1 , wherein X is a bond.

5. The compound of claim 1 , wherein X is —C(═O)—.

6. The compound of claim 1 , wherein n is 2.

7. The compound of claim 1 , wherein n is 1.

8. The compound of claim 1 , further represented by Formula (II) or Formula (III):

or a pharmaceutically acceptable salt thereof, wherein:

each instance of R 4 is independently H, optionally substituted C 1-6 alkyl, F, Cl, Br, I, CN, OH, or alkoxy;

R 5 is H or a nitrogen protecting group; and

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

9. The compound of claim 8 , wherein at least one instance of R 4 is CH 3 .

10. The compound of claim 8 , wherein at least one instance of R 4 is F.

11. The compound of claim 8 , wherein at least one instance of R 4 is H.

12. The compound of claim 8 , wherein R 5 is H.

13. The compound of claim 3 , wherein R 2 is

14. The compound of claim 3 , wherein R 2 is

15. The compound of claim 3 , wherein R 2 is

16. The compound of claim 1 having a structure:

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

18. The pharmaceutical composition of claim 17 , wherein the pharmaceutical composition is suitable for delivery to the eye.

19. A method of treating an ocular disease comprising administering a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, to a subject in need thereof.

20. The method of claim 19 , wherein the ocular disease is a retinopathy or age-related macular degeneration.

21. The method of claim 19 , wherein the ocular disease is glaucoma.

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 10, 2016
From: ASKEW, BEN C.
To: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
Reel/Frame 038538/0905 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2016
From: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 038538/0977 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2016
From: ONG, WINSTON ZAPANTA; NOWAK, PAWEL WOJCIECH; KIM, JINSOO
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 038539/0133 →
Continuity (4)
Division 14184886 · Feb 20, 2014
Provisional Application 61767087 · Feb 20, 2013
Provisional Application 61898741 · Nov 1, 2013
Related Publication 20160237094A1 · Aug 18, 2016