IP Library Granted Patent US 9,795,594
Granted Patent B2
US 9,795,594 · App. 15/016,599 · Granted Oct 24, 2017

Human protein tyrosine phosphatase inhibitors and methods of use

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Quick Facts
Patent No.
US 9,795,594
App. No.
15/016,599
Granted
Oct 24, 2017
Kind
B2
Abstract

The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.

Claims (21)

1. A method of promoting repair of tissue damaged by an angiogenesis elevated disorder in a subject in need thereof, the method comprising administering to the subject a therapeutically-effective amount of a Tie-2 modulator having the formula:

wherein:

R is a thiazolyl group that is substituted or unsubstituted;

R 1 is alkyl, phenyl, or benzyl, any of which is substituted or unsubstituted, or hydrogen;

R 2 is alkyl or alkoxy; and

R 3 is hydrogen or alkyl,

or a pharmaceutically-acceptable salt thereof,

wherein the angiogenesis elevated disorder is selected from the group consisting of diabetic retinopathy, macular degeneration, vein occlusion, and retinal detachment;

and wherein the tissue damaged by the angiogenesis elevated disorder is ocular tissue.

2. The method of claim 1 , wherein the Tie-2 modulator is an HPTP-β inhibitor.

3. The method of claim 1 , wherein the Tie-2 modulator induces enhanced tissue growth.

4. The method of claim 1 , wherein the Tie-2 modulator binds to HPTP-β.

5. The method of claim 1 , wherein the subject is a human.

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

7. The method of claim 1 , wherein the angiogenesis elevated disorder is diabetic retinopathy.

8. The method of claim 1 , wherein the angiogenesis elevated disorder is macular degeneration.

9. The method of claim 1 , wherein the angiogenesis elevated disorder is vein occlusion.

10. The method of claim 1 , wherein the angiogenesis elevated disorder is retinal detachment.

11. The method of claim 1 , wherein the Tie-2 modulator is

12. The method of claim 1 , wherein the Tie-2 modulator is

13. The method of claim 1 , wherein the Tie-2 modulator is

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 9, 2021
From: AERPIO PHARMACEUTICALS, INC.
To: EYEPOINT PHARMACEUTICALS, INC.
Reel/Frame 057448/0033 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 17, 2020
From: AERPIO THERAPEUTICS LLC
To: AERPIO PHARMACEUTICALS, INC.
Reel/Frame 052432/0789 →
CHANGE OF NAME Recorded Jul 31, 2019
From: AERPIO THERAPEUTICS, INC.
To: AERPIO THERAPEUTICS LLC
Reel/Frame 049922/0273 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 27, 2017
From: GRAY, JEFFREY LYLE; AMARASINGHE, KANDE K.D.; CLARK, CYNTHIA MONESA; NICHOLS, RYAN MATTHEW; MAIER, MATTHEW B.
To: AERPIO THERAPEUTICS, INC.
Reel/Frame 043116/0165 →