IP Library Granted Patent US 11,427,543
Granted Patent B2
US 11,427,543 · App. 16/318,846 · Granted Aug 30, 2022

Compounds for targeting cancer stem cells

Inventors: Igor Garkavtsev (Cambridge, MA); Rakesh K. Jain (Wellesley, MA)
Assignee: The General Hospital Corporation
C07D213/82A61P35/00C07C251/80C07D213/53
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Quick Facts
Patent No.
US 11,427,543
App. No.
16/318,846
Granted
Aug 30, 2022
Kind
B2
Abstract

This invention relates to antagonists of G3BP2, G3BP1, and ZEB1. Pharmaceutical compositions comprising G3BP2 inhibitors, methods of inhibiting G3BP2, G3BP1, and ZEB1, methods of treating cancer and inflammation, and methods of identifying an inhibitor of cancer stems cells are also provided.

Claims (16)

1. A method of treating a breast cancer, the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound having the formula:

or a pharmaceutically acceptable salt thereof.

2. A method of reducing metastasis of a breast cancer in a patient, the method comprising administering to the patient in need thereof a therapeutically effective amount of a compound having the formula:

or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the breast cancer is selected from: breast cancer associated with overexpression of G3BP2, breast cancer associated with overexpression of ZEB1, breast cancer associated with overexpression of G3BP2 and overexpression of ZEB1, breast cancer associated with overexpression of G3BP1, breast cancer associated with overexpression of G3BP1 and overexpression of G3BP2, and breast cancer associated with overexpression of G3BP1, overexpression of G3BP2, and overexpression of ZEB1.

4. A method of treating a breast cancer in a patient, the method comprising:

i) identifying the patient as having a breast cancer selected from: breast cancer associated with overexpression of G3BP2, breast cancer associated with overexpression of ZEB1, breast cancer associated with overexpression of G3BP2 and overexpression of ZEB1, breast cancer associated with overexpression of G3BP1, breast cancer associated with overexpression of G3BP1 and overexpression of G3BP2, and breast cancer associated with overexpression of G3BP1, overexpression of G3BP2, and overexpression of ZEB1; and

ii) administering to the patient a therapeutically effective amount of a compound having the formula:

or a pharmaceutically acceptable salt thereof.

5. A method of inhibiting G3BP1, G3BP2, or ZEB1, or any combination thereof, in a breast cancer cell, the method comprising contacting the breast cancer cell with an effective amount of a compound having the formula:

or a pharmaceutically acceptable salt thereof.

6. A method of inhibiting growth of a breast cancer stem cell, the method comprising contacting the breast cancer stem cell with an effective amount of a compound having the formula:

or a pharmaceutically acceptable salt thereof.

7. The method of claim 6 , wherein the breast cancer stem cell is associated with an overexpression selected from: overexpression of G3BP2, overexpression of ZEB1, overexpression of G3BP2 and ZEB1, overexpression of G3BP1, overexpression of G3BP1 and G3BP2, and overexpression of G3BP1, G3BP2, and ZEB1.

8. The method of claim 6 , wherein the breast cancer stem cell is resistant to treatment with a chemotherapeutic agent.

9. The method of claim 2 , wherein the breast cancer is selected from: breast cancer associated with overexpression of G3BP2, breast cancer associated with overexpression of ZEB1, breast cancer associated with overexpression of G3BP2 and overexpression of ZEB1, breast cancer associated with overexpression of G3BP1, breast cancer associated with overexpression of G3BP1 and overexpression of G3BP2, and breast cancer associated with overexpression of G3BP1, overexpression of G3BP2, and overexpression of ZEB1.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 9, 2022
From: GARKAVTSEV, IGOR; JAIN, RAKESH K.
To: THE GENERAL HOSPITAL CORPORATION
Reel/Frame 060328/0716 →
CONFIRMATORY LICENSE Recorded Mar 12, 2021
From: MASSACHUSETTS GENERAL HOSPITAL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 055578/0540 →
Continuity (3)
Provisional Application 62483587 · Apr 10, 2017
Provisional Application 62364215 · Jul 19, 2016
Related Publication 20210238140A1 · Aug 5, 2021