IP Library Granted Patent US 10,098,888
Granted Patent B2
US 10,098,888 · App. 15/359,538 · Granted Oct 16, 2018

Substituted benzene compounds

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Quick Facts
Patent No.
US 10,098,888
App. No.
15/359,538
Granted
Oct 16, 2018
Kind
B2
Abstract

The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Claims (20)

1. A method of treating a cancer being lymphoma, leukemia, or melanoma, comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

2. The method of claim 1 , wherein the cancer is diffuse large B-cell lymphoma (DLBCL), non-Hodgkin's lymphoma (NHL), follicular lymphoma, chronic myelogenous leukemia (CML), acute myeloid leukemia, acute lymphocytic leukemia, or mixed lineage leukemia.

3. A method of treating an INI1-deficient tumor, comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

4. The method of claim 3 , wherein the INI1-deficient tumor is malignant rhabdoid tumor.

5. A method of treating myelodysplastic syndrome (MDS), comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

6. A method of modulating an activity of EZH2 or a mutant thereof, comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

7. The method of claim 6 , being of inhibiting the histone methyltransferase activity of EZH2 or the mutant thereof.

8. The method of claim 6 , wherein the mutant of EZH2 is EZH2 Y641 mutant, EZH2 A677 mutant, or EZH2 A687 mutant.

9. The method of claim 8 , wherein the EZH2 Y641 mutant is EZH2 Y641F mutant, EZH2 Y641N mutant, EZH2 Y641H mutant, EZH2 Y641S mutant, or EZH2 Y641C mutant.

10. The method of claim 6 , wherein the subject has cancer.

11. The method of claim 10 , wherein the cancer is lymphoma, leukemia, or melanoma.

12. The method of claim 10 , wherein the cancer is diffuse large B-cell lymphoma (DLBCL), non-Hodgkin's lymphoma (NHL), follicular lymphoma, chronic myelogenous leukemia (CML), acute myeloid leukemia, acute lymphocytic leukemia, or mixed lineage leukemia.

13. The method of claim 10 , wherein the cancer is an INI1-deficient tumor.

14. The method of claim 13 , wherein the INI-deficient tumor is malignant rhabdoid tumor.

15. The method of claim 6 , wherein the subject has a precancerous condition.

16. The method of claim 15 , wherein the precancerous condition is myelodysplastic syndrome (MDS).

Assignments (6)
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 →
SECURITY INTEREST Recorded Nov 19, 2019
From: EPIZYME, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 051057/0848 →
CORRECTIVE ASSIGNMENT TO CORRECT THE SECOND ASSIGNOR NAME PREVIOUSLY RECORDED AT REEL: 040450 FRAME: 0668. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Dec 5, 2016
From: KUNTZ, KEVIN WAYNE; CAMPBELL, JOHN EMMERSON
To: EPIZYME, INC.
Reel/Frame 040854/0440 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2016
From: EISAI R&D MANAGEMENT CO., LTD.
To: EPIZYME, INC.
Reel/Frame 040478/0354 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2016
From: KUNTZ, KEVIN WAYNE; CAMPELL, JOHN EMMERSON
To: EPIZYME, INC.
Reel/Frame 040450/0668 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2016
From: SEKI, MASASHI
To: EISAI R&D MANAGEMENT CO., LTD.
Reel/Frame 040450/0691 →