IP Library Granted Patent US 11,672,800
Granted Patent B2
US 11,672,800 · App. 16/606,833 · Granted Jun 13, 2023

Combination therapies with EHMT2 inhibitors

Inventors: John Emmerson Campbell (Cambridge, MA); Kenneth William Duncan (Westwood, MA); Maria Alejandra Raimondi (Jamaica Plain, MA); Christine Klaus (Waban, MA); Elayne Penebre (Auburndale, MA)
Assignee: Epizyme, Inc.
A61K31/506A61K31/203A61K31/4375A61K31/44A61K31/496A61K31/517A61K31/519A61K31/706A61P35/00
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Quick Facts
Patent No.
US 11,672,800
App. No.
16/606,833
Granted
Jun 13, 2023
Kind
B2
Abstract

The present disclosure relates to a method of preventing or treating a cancer via administering an EHMT2 inhibitor or a combination comprising an EHMT2 inhibitor compound and one or more additional therapeutic agent disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds or combinations for research or other non-therapeutic purposes.

Claims (24)

1. A method for treating an acute myeloid leukemia (AML), acute lymphocytic leukemia (ALL), or melanoma comprising administering to a subject in need thereof a compound selected from:

or a pharmaceutically acceptable salt thereof,

and one or more additional therapeutic agent selected from a PI3K inhibitor, a MTOR inhibitor, an AKT inhibitor, a BRAF inhibitor, a MEK1 inhibitor, a MEK2 inhibitor, an ERK inhibitor, an EGFR inhibitor, a DNMT inhibitor, a cKIT inhibitor, and a CDK4/6 inhibitor, or any combination thereof.

2. The method of claim 1 , wherein the compound and the one or more additional therapeutic agent are administered simultaneously, sequentially, or in alteration.

3. The method of claim 1 , wherein the one or more additional therapeutic agent is BKM120, GDC-0068, sorafenib, BVD-523, erlotinib, trametinib, selumetinib, pictilisib, MK-2206, everolimus, decitabine, palbociclib, or imatinib, a pharmaceutically acceptable salt thereof, or any combination thereof.

4. A method of inhibiting or decreasing growth, viability, survival, or proliferation of an acute myeloid leukemia (AML), acute lymphocytic leukemia (ALL), or melanoma cell comprising (1) contacting the cell with (a) a compound selected from:

or a pharmaceutically acceptable salt thereof,

and (b) one or more additional therapeutic agent selected from a PI3K inhibitor, a MTOR inhibitor, an AKT inhibitor, a BRAF inhibitor, a MEK1 inhibitor, a MEK2 inhibitor, an ERK inhibitor, an EGFR inhibitor, a DNMT inhibitor, a cKIT inhibitor, and a CDK4/6 inhibitor, or any combination thereof.

5. The method of claim 1 , wherein the compound is a selective inhibitor of EHMT2.

6. The method of claim 1 , wherein the one or more additional therapeutic agent is a PI3K inhibitor.

7. The method of claim 1 , wherein the one or more additional therapeutic agent is a MTOR inhibitor.

8. The method of claim 1 , wherein the one or more additional therapeutic agent is an AKT inhibitor.

9. The method of claim 1 , wherein the one or more additional therapeutic agent is a BRAF inhibitor.

10. The method of claim 1 , wherein the one or more additional therapeutic agent is a MEK1 inhibitor or a MEK2 inhibitor.

11. The method of claim 1 , wherein the one or more additional therapeutic agent is an ERK inhibitor.

12. The method of claim 1 , wherein the one or more additional therapeutic agent is an EGFR inhibitor.

13. The method of claim 1 , wherein the one or more additional therapeutic agent is a DNMT inhibitor.

14. The method of claim 1 , wherein the one or more additional therapeutic agent is a cKIT inhibitor.

15. The method of claim 1 , wherein the one or more additional therapeutic agent is a CDK4/6 inhibitor.

16. The method of claim 1 , wherein the one or more additional therapeutic agent is decitabine.

17. The method of claim 1 , wherein the one or more additional therapeutic agent is azacitidine.

18. The method of claim 1 , wherein the one or more additional therapeutic agent is venetoclax.

19. The method of claim 1 , wherein the one or more additional therapeutic agent is ATRA.

20. The method of claim 1 , wherein the one or more additional therapeutic agent is everolimus.

Assignments (3)
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENTS AT REEL/FRAME: 051057/0848 Recorded Aug 13, 2022
From: BIOPHARMA CREDIT PLC
To: EPIZYME, INC.
Reel/Frame 061165/0501 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 14, 2020
From: CAMPBELL, JOHN EMMERSON; DUNCAN, KENNETH WILLIAM; RAIMONDI, MARIA ALEJANDRA; KLAUS, CHRISTINE; PENEBRE, ELAYNE
To: EPIZYME, INC.
Reel/Frame 051507/0924 →
SECURITY INTEREST Recorded Nov 19, 2019
From: EPIZYME, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 051057/0848 →
Cited By (3)
US 1,120,314 US 12,649,031 US 12,691,227