IP Library Granted Patent US 10,398,703
Granted Patent B2
US 10,398,703 · App. 15/868,894 · Granted Sep 3, 2019

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.
A61K31/5377A61K9/0048A61K9/10A61K9/146A61K31/4709A61K31/505A61K31/506C07D239/88C07D405/12C07D413/14C07D491/107Y02A50/473
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Quick Facts
Patent No.
US 10,398,703
App. No.
15/868,894
Granted
Sep 3, 2019
Kind
B2
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 (51)

1. A pharmaceutical composition, comprising a compound of Formula (I) and a pharmaceutically acceptable carrier, wherein Formula (I) is:

or a pharmaceutically acceptable salt thereof,

wherein:

R 1 is H or C 1-6 alkyl;

R 2 is an optionally substituted oxetanyl, or optionally substituted spiro bicyclic heterocyclyl wherein one or two atoms in the heterocyclic ring are independently O or N;

X is a bond, —O—, or —C(═O)—;

each instance of R 3 is independently H, F, Cl, Br, I, CN, or OH;

Z is optionally substituted aliphatic, optionally substituted heterocyclylalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted quinolyl;

m is 0, 1, 2, 3, or 4; and

n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

2. The pharmaceutical composition of claim 1 , wherein m is 0.

3. The pharmaceutical composition of claim 1 , wherein m is 1 and R 3 is Cl.

4. The pharmaceutical composition of claim 1 , wherein m is 1 and R 3 is F.

5. The pharmaceutical composition of claim 1 , wherein R 1 is CH 3 .

6. The pharmaceutical composition of claim 1 , wherein Z is optionally substituted isooxazolyl.

7. The pharmaceutical composition of claim 1 , wherein Z is optionally substituted phenyl.

8. The pharmaceutical composition of claim 1 , wherein Z is:

wherein e, f, and h are independently 1, 2, or 3.

9. The pharmaceutical composition of claim 1 , wherein Z is C 1-6 alkyl.

10. The pharmaceutical composition of claim 1 , wherein Z is optionally substituted thiophenyl.

11. The pharmaceutical composition of claim 1 , wherein X is a bond.

12. The pharmaceutical composition of claim 1 , wherein X is —O—.

13. The pharmaceutical composition of claim 1 , wherein X is —C(═O)—.

14. The pharmaceutical composition of claim 1 , wherein n is 1.

15. The pharmaceutical composition of claim 1 , wherein n is 2.

16. The pharmaceutical composition of claim 1 , wherein R 2 is:

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

17. The pharmaceutical composition of claim 1 , wherein R 2 is:

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

18. The pharmaceutical composition of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

19. A method of treating an ocular disease, comprising administering a pharmaceutical composition according to claim 1 to a subject in need thereof.

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

21. A pharmaceutical composition, comprising a compound of Formula (VI) and a pharmaceutically acceptable carrier, wherein Formula (VI) is:

or a pharmaceutically acceptable salt thereof,

wherein:

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

R 2 is heterocyclyl;

X is a bond, —O—, or —C(═O)—;

each instance of R 3 is independently H, F, Cl, Br, I, CN, or OH;

Y is CH;

Z is C 1-6 alkyl, optionally substituted heterocyclylalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted quinolyl;

m is independently 0, 1, 2, 3, or 4; and

n is independently 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

22. A method of treating an ocular disease, comprising administering a pharmaceutical composition according to claim 21 to a subject in need thereof.

23. The method of claim 22 , wherein the ocular disease is a retinopathy, age-related macular degeneration, or glaucoma.

24. The pharmaceutical composition of claim 18 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

25. The pharmaceutical composition of claim 18 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

26. The pharmaceutical composition of claim 21 , wherein R 1 is H or C 1-6 alkyl.

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 Sep 13, 2018
From: ONG, WINSTON ZAPANTA; NOWAK, PAWEL W.; KIM, JINSOO
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 046865/0343 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2018
From: ASKEW, BEN C.
To: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
Reel/Frame 046865/0433 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2018
From: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 046865/0470 →
Continuity (5)
Continuation 15139107 · Apr 26, 2016
Division 14181095 · Feb 14, 2014
Provisional Application 61898778 · Nov 1, 2013
Provisional Application 61765487 · Feb 15, 2013
Related Publication 20180133225A1 · May 17, 2018