IP Library Granted Patent US 12,157,735
Granted Patent B2
US 12,157,735 · App. 17/965,569 · Granted Dec 3, 2024

Compounds for targeted degradation of BRD9

Inventors: Christopher G. Nasveschuk (Stoneham, MA); Rhamy Zeid (Arlington, MA); Ning Yin (Lexington, MA); Katrina L. Jackson (Weston, MA); Gesine Kerstin Veits (Sommerville, MA); Moses Moustakim (Brighton, MA); Jeremy L. Yap (Sudbury, MA)
Assignee: C4 Therapeutics, Inc.
C07D471/04A61P35/00C07D401/14
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Quick Facts
Patent No.
US 12,157,735
App. No.
17/965,569
Granted
Dec 3, 2024
Kind
B2
Abstract

BRD9 protein degradation compounds or pharmaceutically acceptable salts thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.

Claims (39)

1. A compound of Formula:

or a pharmaceutically acceptable salt thereof;

wherein:

Q 1 is NH or O;

X 3 is N, CH, or CR 3 ;

X 10 is CH 2 or C(O);

X 11 is heterocycle optionally substituted with 1, 2, or 3 groups independently selected from R 3 ;

X 16 is selected from the group consisting of N, CH, and CR 4 ;

each R 3 is independently selected from the group consisting of hydrogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, fluorine, and chlorine;

each R 4 is independently selected from the group consisting of hydrogen, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, fluorine, and chlorine;

each R 7 is independently hydrogen, methyl, or ethyl; and

R 8 is C 1 -C 4 alkyl or C 2 -C 4 alkenyl.

2. The compound of claim 1 , wherein X 11 is selected from the group consisting of:

3. The compound of claim 1 , wherein Q 1 is NH.

4. The compound of claim 3 , wherein X 10 is CH 2 .

5. The compound of claim 4 , wherein each R 7 is CH 3 .

6. The compound of claim 5 , wherein each R 4 is OCH 3 .

7. The compound of claim 6 , wherein X 11 is selected from the group consisting of:

8. The compound of claim 1 , wherein the compound is of Formula:

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 8 , wherein Q 1 is NH.

10. The compound of claim 8 , wherein X 10 is CH 2 .

11. The compound of claim 10 , wherein each R 7 is CH 3 .

12. The compound of claim 11 , wherein X 11 is selected from the group consisting of:

13. The compound of claim 1 , wherein the compound is of Formula:

or a pharmaceutically acceptable salt thereof.

14. The compound of claim 13 , wherein each R 7 is CH 3 .

15. The compound of claim 1 , wherein the compound is of Formula:

or a pharmaceutically acceptable salt thereof.

16. The compound of claim 1 , wherein the compound is of Formula:

or a pharmaceutically acceptable salt thereof.

17. The compound of claim 16 , wherein X 11 is selected from the group consisting of:

18. The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

19. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutical salt thereof and a pharmaceutically acceptable excipient.

20. The pharmaceutical composition of claim 19 , wherein the pharmaceutical composition is formulated for oral administration.

21. The pharmaceutical composition of claim 20 , wherein the pharmaceutical composition is a tablet or capsule.

22. The pharmaceutical composition of claim 19 , wherein the pharmaceutical composition is formulated for parenteral administration.

23. The pharmaceutical composition of claim 19 , wherein the pharmaceutical composition is formulated for intravenous administration.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 4, 2024
From: NASVESCHUK, CHRISTOPHER G.; ZEID, RHAMY; YIN, NING; JACKSON, KATRINA L.; VEITS, GESINE KERSTIN; MOUSTAKIM, MOSES; YAP, JEREMY L.
To: C4 THERAPEUTICS, INC.
Reel/Frame 067618/0560 →
Continuity (6)
Continuation 17901775 · Sep 1, 2022
Continuation 17541035 · Dec 2, 2021
Continuation PCTUS2021021240 · Mar 5, 2021
Provisional Application 63061659 · Aug 5, 2020
Provisional Application 62985774 · Mar 5, 2020
Related Publication 20240051953A1 · Feb 15, 2024
Cited By (1)
US 12,441,740