IP Library Granted Patent US 12,168,016
Granted Patent B2
US 12,168,016 · App. 18/606,946 · Granted Dec 17, 2024

Aryl-OR heteroaryl-substituted benzene compounds

Inventors: Kevin W. Kuntz (Woburn, MA); Richard Chesworth (Concord, MA); Kenneth W. Duncan (Westwood, MA); Heike Keilhack (Belmont, MA); Natalie Warholic (Cambridge, MA); Christine Klaus (Waban, MA); Sarah K. Knutson (Lincoln, MA); Timothy J. N. Wigle (Waltham, MA); Masashi Seki (Tsukuba, JP); Syuji Shirotori (Tsukuba, JP); Satoshi Kawano (Tsukuba, JP)
Assignee: Epizyme, Inc.
A61K31/5377A61K31/4412A61K31/443A61K31/4433A61K31/4436A61K31/4439A61K31/444A61K31/4545A61K31/4709A61K31/496A61K31/506A61K31/551A61K31/553C07D213/64C07D401/12C07D405/12C07D405/14C07D409/12C07D413/12C07D417/12C07D491/08C07D491/107C07D498/08
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Quick Facts
Patent No.
US 12,168,016
App. No.
18/606,946
Granted
Dec 17, 2024
Kind
B2
Abstract

The present invention relates to aryl- or heteroaryl-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 (13)

1. A method of inhibiting the histone methyltransferase activity of EZH2 in a human subject in need thereof, comprising oral administration to the human subject a compound of the following formula:

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is:

3. The method of claim 1 , wherein the compound is a pharmaceutically acceptable salt of:

4. The method of claim 3 , wherein the pharmaceutically acceptable salt is a hydrobromic acid salt.

5. The method of claim 4 , wherein the human subject has soft tissue sarcoma.

6. The method of claim 5 , wherein the compound is administered twice daily and in a total daily amount of from about 0.1 mg/day to about 3 g/day.

7. The method of claim 4 , wherein the human subject has follicular lymphoma.

8. The method of claim 7 , wherein the compound is administered twice daily and in a total daily amount of from about 0.1 mg/day to about 3 g/day.

9. The method of claim 1 , wherein the human subject has soft tissue sarcoma.

10. The method of claim 9 , wherein the compound is administered twice daily and in a total daily amount of from about 0.1 mg/day to about 3 g/day.

11. The method of claim 1 , wherein the human subject has follicular lymphoma.

12. The method of claim 11 , wherein the compound is administered twice daily and in a total daily amount of from about 0.1 mg/day to about 3 g/day.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2024
From: KUNTZ, KEVIN W.; CHESWORTH, RICHARD; DUNCAN, KENNETH W.; KEILHACK, HEIKE; WARHOLIC, NATALIE; KLAUS, CHRISTINE; KNUTSON, SARAH K.; WIGLE, TIMOTHY J.N.
To: EPIZYME, INC.
Reel/Frame 068013/0922 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2024
From: SEKI, MASASHI; SHIROTORI, SYUJI; KAWANO, SATOSHI
To: EISAI CO., LTD.
Reel/Frame 068013/0930 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2024
From: EISAI CO., LTD.
To: EISAI R&D MANAGEMENT CO., LTD.
Reel/Frame 068013/0937 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2024
From: EISAI R&D MANAGEMENT CO., LTD.
To: EPIZYME, INC.
Reel/Frame 068013/0940 →