Therapeutic compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-9353122-B2
Application number	US-201414181095-A
Country	US
Kind code	B2
Filing date	Feb 14, 2014
Priority date	Feb 15, 2013
Publication date	May 31, 2016
Grant date	May 31, 2016

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.

First claim

What is claimed is:

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof,
wherein:
R 1 is hydrogen or C 1-6 alkyl;
R 2 is heterocyclyl;
X is a bond, —O—, or —C(═O)—;
each instance of R 3 is independently selected from the group consisting of hydrogen, F, Cl, Br, I, CN, and OH;
Y is N;
Z is optionally substituted aliphatic, 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.

2. The 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 hydrogen, optionally substituted C 1-6 alkyl, F, Cl, Br, I, or CN; and
j is 0, 1, or 2.

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

or a pharmaceutically acceptable salt thereof
wherein:
each instance of R 4 is independently hydrogen, optionally substituted C 1-6 alkyl, F, Cl, Br, I, or CN; and
j is 0, 1, or 2.

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-c):

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof,
wherein:
each instance of R 5 is independently hydrogen, optionally substituted C 1-6 alkyl, F, Cl, Br, I, or CN; and
k is 0, 1, 2, 3, 4, or 5.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof,
wherein Z 1 is branched or unbranched, acyclic or cyclic C 1-6 alkyl.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

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

Assignees

• Kala Pharmaceuticals Inc

Inventors

• Ong Winston Zapanta
• Nowak Pawel Wojciech
• Askew Ben C
• Kim Jinsoo

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P27/06

  Antiglaucoma agents or miotics · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61K9/146

  with organic macromolecular compounds · CPC title