IP Library Granted Patent US 12,171,751
Granted Patent B2
US 12,171,751 · App. 18/304,511 · Granted Dec 24, 2024

Methods of treating intraocular pressure with activators of Tie-2

Inventor: Kevin Peters (Cincinnati, OH)
Assignee: EyePoint Pharmaceuticals, Inc.
A61K31/426A61K31/427A61K31/428A61K31/433A61K31/496A61K31/497A61K31/513A61P27/02A61P27/06
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Quick Facts
Patent No.
US 12,171,751
App. No.
18/304,511
Granted
Dec 24, 2024
Kind
B2
Abstract

Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for eye conditions associated with angiogenesis, for example, intraocular pressure, ocular hypertension, and glaucoma.

Claims (25)

1. A method for treating glaucoma in a subject in need thereof, the method comprising administering to the subject a therapeutically-effective amount of a Tie-2 activator, wherein:

the administration reduces intraocular pressure by about 0.1 mmHg to about 9 mmHg compared to absence of administration;

the subject expresses Ang-1 and Ang-2;

the subject is human; and

the Tie-2 activator is a compound of the formula:

or a pharmaceutically-acceptable salt, tautomer, or zwitterion thereof.

2. The method of claim 1 , wherein the Tie-2 activator binds a phosphatase.

3. The method of claim 1 , wherein the Tie-2 activator inhibits a phosphatase.

4. The method of claim 1 , wherein the Tie-2 activator binds HPTP-B.

5. The method of claim 1 , wherein the Tie-2 activator inhibits HPTP-B.

6. The method of claim 1 , wherein the Tie-2 activator is a phosphate mimetic.

7. The method of claim 1 , wherein the therapeutically-effective amount is from about 1 mg to about 100 mg.

8. The method of claim 7 , wherein the therapeutically-effective amount is from about 0.5 mg to about 30 mg.

9. The method of claim 8 , wherein the therapeutically-effective amount is about 15 mg.

10. The method of claim 8 , wherein the therapeutically-effective amount is about 22.5 mg.

11. The method of claim 1 , wherein the therapeutically-effective amount is about 30 mg.

12. The method of claim 1 , wherein the administration is to an eye of the subject.

13. The method of claim 1 , wherein the administration is intravitreal.

14. The method of claim 1 , wherein the administration is subcutaneous.

15. The method of claim 1 , wherein the administration is topical.

16. The method of claim 1 , wherein the administration is topical to an eye of the subject.

17. The method of claim 1 , wherein the Tie-2 activator, or a pharmaceutically-acceptable salt thereof, is formulated as a drop.

18. The method of claim 1 , wherein the Tie-2 activator, or a pharmaceutically-acceptable salt thereof, is formulated as a drop, wherein the drop is administered to an eye of the subject.

19. The method of claim 1 , wherein the intraocular pressure is reduced by at least about 2 mmHg.

20. The method of claim 1 , wherein the intraocular pressure is ocular hypertension.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2024
From: PETERS, KEVIN GENE
To: AERPIO THERAPEUTICS, INC.
Reel/Frame 068360/0078 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2024
From: AERPIO THERAPEUTICS LLC
To: AERPIO PHARMACEUTICALS, INC.
Reel/Frame 068360/0177 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2024
From: AERPIO PHARMACEUTICALS, INC.
To: EYEPOINT PHARMACEUTICALS, INC.
Reel/Frame 068741/0595 →
CHANGE OF NAME Recorded Aug 21, 2024
From: AERPIO THERAPEUTICS, INC.
To: AERPIO THERAPEUTICS LLC
Reel/Frame 068743/0231 →
Continuity (4)
Continuation 17150430 · Jan 15, 2021
Continuation 15273068 · Sep 22, 2016
Provisional Application 62222481 · Sep 23, 2015
Related Publication 20230398100A1 · Dec 14, 2023