IP Library Granted Patent US 12,049,464
Granted Patent B2
US 12,049,464 · App. 17/901,775 · Granted Jul 30, 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 12,049,464
App. No.
17/901,775
Granted
Jul 30, 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 (24)

1. A method of treating a disorder mediated by BRD9 comprising administering an effective amount of a compound of Formula:

or a pharmaceutically acceptable salt thereof to a human in need thereof;

wherein:

Q 1 is selected from the group consisting of NH, N(alkyl), N(haloalkyl), CH 2 , a, and S;

X 3 is N, CH, or CR 3 ;

X 10 is Cc(R 7 ) 2 , C(O), or O;

X 11 is a 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 ;

R 3 is independently at each occurrence selected from the group consisting of hydrogen, hydroxyl, alkoxy, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, cycloalkyl, fluorine, chlorine, bromine, and iodine;

each R 4 is independently selected from the group consisting of hydrogen, aryl, heteroaryl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, C 1 -C 4 alkyl, fluorine, chlorine, bromine, and iodine;

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

R 8 is hydrogen, C 1 -C 4 alkyl, alkenyl, alkynyl, haloalkyl, or cycloalkyl.

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

or a pharmaceutically acceptable salt thereof.

3. The method of claim 2 , wherein Q 1 is NH.

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

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

6. The method of claim 5 , wherein X 11 is selected from:

7. The method of claim 6 , wherein the BRD9 mediated disorder is synovial sarcoma.

8. The method of claim 6 , wherein the BRD9 mediated disorder is a SMARCB1-perturbed cancer.

9. The method of claim 1 , wherein the compound is of structure

or a pharmaceutically acceptable salt thereof.

10. The method of claim 9 , wherein the BRD9 mediated disorder is synovial sarcoma.

11. The method of claim 9 , wherein the BRD9 mediated disorder is a SMARCB1-perturbed cancer.

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 (5)
Continuation 17541035 · Dec 2, 2021
Continuation PCTUS2021021240 · Mar 5, 2021
Provisional Application 63061659 · Aug 5, 2020
Provisional Application 62985774 · Mar 5, 2020
Related Publication 20230060334A1 · Mar 2, 2023
Cited By (1)
US 12,441,740