IP Library › Granted Patent US 11,220,509
Granted Patent B2
US 11,220,509 · App. 17/219,379 · Granted Jan 11, 2022

Substituted imidazo[1,2-c]pyrimidines as PRC2 inhibitors

Inventors: Matthew Arnold Marx (San Diego, CA); Matthew Randolph Lee (Del Mar, CA); Thomas P. Bobinski (San Diego, CA); Aaron Craig Burns (San Diego, CA); Nidhi Arora (San Diego, CA); James Gail Christensen (San Diego, CA); John Michael Ketcham (San Diego, CA)
Assignee: MIRATI THERAPEUTICS, INC.
C07D487/04
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Quick Facts
Patent No.
US 11,220,509
App. No.
17/219,379
Granted
Jan 11, 2022
Kind
B2
Abstract

The present disclosure relates to compounds of Formula (I), or pharmaceutically, acceptable salts thereof, that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present disclosure relates to compounds, or pharmaceutically acceptable salts thereof pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds of Formula (I), or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising compounds of Formula (I), or pharmaceutically acceptable salts thereof.

Claims (41)

1. A method for treating cancer in a patient, comprising administering to the patient in need thereof a therapeutically effective amount of a compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof, wherein the cancer is a polycomb repressive complex 2-associated cancer selected from the group consisting of bladder cancer, breast cancer, head and neck cancer, liver cancer, pancreatic cancer, prostate cancer, skin cancer, lymphoma, sarcoma, lung cancer, and ovarian cancer.

2. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is bladder cancer.

3. The method according to claim 1 , wherein the poly comb repressive complex 2-associated cancer is breast cancer.

4. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is head and neck cancer.

5. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is liver cancer.

6. The method according to claim 1 , wherein the poly comb repressive complex 2-associated cancer is pancreatic cancer.

7. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is prostate cancer.

8. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is skin cancer.

9. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is lymphoma.

10. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is sarcoma.

11. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is lung cancer.

12. The method according to claim 1 , wherein the polycomb repressive complex 2-associated cancer is ovarian cancer.

13. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

14. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

15. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

16. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

17. The method according to claim 1 , wherein the compound is

of a pharmaceutically acceptable salt thereof.

18. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

19. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

20. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

21. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

22. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

23. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

24. The method according to claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

25. A method for inhibiting poly comb repressive complex 2 activity in a patient, comprising administering to the patient in need thereof a therapeutically effective amount of a compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

26. The method according to claim 25 , wherein the patient has a polycomb repressive complex 2-associated cancer.

27. The method according to claim 26 , wherein the polycomb repressive complex 2-associated cancer is selected from the group consisting of bladder cancer, breast cancer, head and neck cancer, liver cancer, pancreatic cancer, prostate cancer, skin cancer, lymphoma, sarcoma, lung cancer, and ovarian cancer.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2021
From: MARX, MATTHEW ARNOLD; LEE, MATTHEW RANDOLPH; BOBINSKI, THOMAS P.; BURNS, AARON CRAIG; ARORA, NIDHI; CHRISTENSEN, JAMES GAIL; KETCHAM, JOHN MICHAEL
To: MIRATI THERAPEUTICS, INC.
Reel/Frame 055788/0957 →
Continuity (6)
Continuation 17116270 · Dec 9, 2020
Continuation 16966708
Provisional Application 62747736 · Oct 19, 2018
Provisional Application 62672701 · May 17, 2018
Provisional Application 62624176 · Jan 31, 2018
Related Publication 20210230168A1 · Jul 29, 2021
Cited By (1)
US 12,371,435