Therapeutic compounds and uses thereof

• US 9,861,634 B2
• Filed: 04/26/2016
• Issued: 01/09/2018
• Est. Priority Date: 02/20/2013
• 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
• Primary Examiner(s): Ward, Paul V
• Application Number:
  US15/139,135
• Publication Number:
  US 20160237094A1
• Time in Patent Office: 623 Days
• CPC Class Codes: A61K 31/517 ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61P 17/02 for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07D 403/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 491/107 with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• CPC Class Codes: C07D 519/00 Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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

1. A compound of Formula (I):

2. The compound of claim 1, wherein R₁ is CH₃.

3. The compound of claim 1, wherein R₂ is)

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):

9. The compound of claim 8, wherein at least one instance of R₄ is CH₃.

10. The compound of claim 8, wherein at least one instance of R₄ is F.

11. The compound of claim 8, wherein at least one instance of R₄ is H.

12. The compound of claim 8, wherein R₅ is H.

13. The compound of claim 3, wherein R₂ is

14. The compound of claim 3, wherein R₂ is

15. The compound of claim 3, wherein R₂ 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.