IP Library Granted Patent US 9,126,958
Granted Patent B2
US 9,126,958 · App. 14/569,106 · Granted Sep 8, 2015

Human protein tyrosine phosphatase inhibitors and methods of use

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Quick Facts
Patent No.
US 9,126,958
App. No.
14/569,106
Granted
Sep 8, 2015
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 (32)

1. A compound of the formula:

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.

2. The compound of claim 1 , wherein:

each instance of alkyl is independently C 1 -C 6 linear alkyl, C 3 -C 6 branched alkyl, or C 3 -C 6 cyclic alkyl; and

alkoxy is C 1 -C 6 linear alkoxy or C 3 -C 6 branched alkoxy.

3. The compound of claim 1 , wherein R 1 is substituted or unsubstituted phenyl.

4. The compound of claim 1 , wherein R 1 is substituted or unsubstituted benzyl.

5. The compound of claim 1 , wherein R 2 is alkyl.

6. The compound of claim 1 , wherein R 2 is alkoxy.

7. The compound of claim 1 , wherein R 2 is methoxy.

8. The compound of claim 1 , wherein R 3 is hydrogen.

9. The compound of claim 1 , wherein R is:

wherein R 6 is alkyl, phenyl, or heteroaryl, any of which is substituted or unsubstituted, or hydrogen.

10. The compound of claim 9 , wherein R 6 is alkyl.

11. The compound of claim 9 , wherein R 6 is substituted or unsubstituted heteroaryl.

12. The compound of claim 9 , wherein R 6 is substituted or unsubstituted thiophen-2-yl.

13. A pharmaceutical composition comprising:

a) a compound of the formula:

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; and

b) a pharmaceutically-acceptable excipient.

14. The compound of claim 1 , wherein the compound is:

15. The compound of claim 1 , wherein the compound is:

16. The pharmaceutical composition of claim 13 , wherein the compound is:

17. The pharmaceutical composition of claim 13 , wherein the compound 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 Apr 30, 2015
From: GRAY, JEFFREY LYLE; CLARK, CYNTHIA MONESA; MAIER, MATTHEW B.; AMARASINGHE, KANDE K.D.; NICHOLS, RYAN MATTHEW
To: AERPIO THERAPEUTICS, INC.
Reel/Frame 035533/0055 →