Therapeutics for the treatment of glaucoma

Patent metadata

Field	Value
Publication number	US-12209140-B2
Application number	US-202217991558-A
Country	US
Kind code	B2
Filing date	Nov 21, 2022
Priority date	Jan 31, 2014
Publication date	Jan 28, 2025
Grant date	Jan 28, 2025

Abstract

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K ATP channel to reduce an intraocular pressure.

First claim

What is claimed is:

1. A method to treat increased intraocular pressure, glaucoma, ocular hypertension, retinopathy, or age-related macular degeneration in a host in need thereof comprising administering an effective amount of a pharmaceutical formulation comprising a compound of the formula:

or a pharmaceutically acceptable salt thereof;
and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical formulation can be administered topically in the eye, and wherein the formulation has a pH of 5.5-8 and an osmolality of 150-450 mOsm.

2. The method of claim 1 , wherein the host is a human.

3. The method of claim 2 to treat increased intraocular pressure.

4. The method of claim 2 to treat ocular hypertension.

5. The method of claim 2 to treat glaucoma.

6. The method of claim 5 , wherein the glaucoma is selected from primary open angle glaucoma, primary angle closure glaucoma, normal tension glaucoma, pediatric glaucoma, pseudoexfoliative glaucoma, pigmentary glaucoma, traumatic glaucoma, neovascular glaucoma, and iridocorneal endothelial glaucoma.

7. The method of claim 6 , wherein the glaucoma is primary open angle glaucoma.

8. The method of claim 6 , wherein the glaucoma is pediatric glaucoma.

9. The method of claim 6 , wherein the glaucoma is neovascular glaucoma.

10. The method of claim 6 , wherein the glaucoma is normal tension glaucoma.

11. The method of claim 6 , wherein the glaucoma is primary angle closure glaucoma.

12. The method of claim 6 , wherein the glaucoma is pseudoexfoliative glaucoma.

13. The method of claim 6 , wherein the glaucoma is pigmentary glaucoma.

14. The method of claim 6 , wherein the glaucoma is traumatic glaucoma.

15. The method of claim 6 , wherein the glaucoma is iridocorneal endothelial glaucoma.

16. The method of claim 2 to treat retinopathy.

17. The method of claim 16 , wherein the retinopathy is diabetic retinopathy.

18. The method of claim 2 to treat age related macular degeneration.

19. The method of claim 2 , wherein the compound is of the formula:

20. The method of claim 2 , wherein the compound is of the formula:

Assignees

• Mayo Found Medical Education & Res
• Univ Minnesota

Inventors

• Fautsch Michael P
• Dosa peter
• Walters Michael A
• Georg Gunda I

Classifications

• C07F9/65586

  at least one of the hetero rings does not contain nitrogen as ring hetero atom · CPC title

• C07F9/6547

  condensed with carbocyclic rings or {carbocyclic} ring systems · CPC title

• C07D405/14

  containing three or more hetero rings · CPC title

• C07D311/70

  with two hydrocarbon radicals attached in position 2 and elements other than carbon and hydrogen in position 6 · CPC title

• C07D311/20

  hydrogenated in the hetero ring · CPC title