IP Library › Granted Patent US 12,202,839
Granted Patent B2
US 12,202,839 · App. 17/309,260 · Granted Jan 21, 2025

In-flow photooxygenation of aminothienopyridinones generates PTP4A3 phosphatase inhibitors

Inventors: John S. Lazo (Charlottesville, VA); Elizabeth Sharlow (Butler, PA); Peter Wipf (Pittsburgh, PA); Nikhil Tasker (Trumbull, CT); Ettore Rastelli (Pittsburgh, PA)
Assignees: University of Virginia Patent Foundation; University of Pittsburgh—Of the Commonwealth System of Higher Education
C07D495/04
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Quick Facts
Patent No.
US 12,202,839
App. No.
17/309,260
Granted
Jan 21, 2025
Kind
B2
Abstract

The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH.

Claims (16)

1. A compound according to Formula (I), or a pharmaceutically acceptable salt thereof:

wherein

X is O or NH; and

(linker) is a linker moiety.

2. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein —X-(linker)- is selected from the group consisting of:

3. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is of the formula (EJR-876-34):

4. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is of the formula (EJR-876-35):

5. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is of the formula (EJR-887-24):

6. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is of the formula (EJR-887-35):

7. A method for treating a subject suffering from cancer, the method comprising administering to the subject a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof to treat the cancer.

8. The method according to claim 7 , wherein the cancer is selected from the group consisting of colorectal cancer, breast cancer, ovarian cancer, cervical cancer, lung cancer, liver cancer, stomach cancer, stromal cancer, leukemia, and lymphoma.

9. The method according to claim 8 , wherein the cancer is breast cancer or ovarian cancer.

10. The method according to claim 9 , wherein the cancer is triple negative breast cancer or advanced ovarian cancer.

11. A method for inhibiting a protein-tyrosine phosphatase in a cell, comprising contacting the cell with a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

12. The method according to claim 11 , wherein the protein tyrosine phosphatase is protein tyrosine phosphatase 4A3 (PTP4A3).

13. A pharmaceutical composition comprising a compound, or a pharmaceutically acceptable salt thereof, according to claim 1 in admixture with a pharmaceutically acceptable carrier.

Assignments (3)
CONFIRMATORY LICENSE Recorded Nov 10, 2022
From: UNIVERSITY OF VIRGINIA
To: UNITED STATES GOVERNMENT
Reel/Frame 061912/0660 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2021
From: LAZO, JOHN S.; SHARLOW, ELIZABETH
To: UNIVERSITY OF VIRGINIA
Reel/Frame 056309/0751 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2021
From: WIPF, PETER; TASKER, NIKHIL; RASTELLI, ETTORE
To: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Reel/Frame 056309/0814 →
Continuity (4)
Provisional Application 62870252 · Jul 3, 2019
Provisional Application 62758861 · Nov 12, 2018
Provisional Application 62758759 · Nov 12, 2018
Related Publication 20210395266A1 · Dec 23, 2021
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