IP Library › Granted Patent US 12,570,620
Granted Patent B2
US 12,570,620 · App. 18/033,269 · Granted Mar 10, 2026

Covalent inhibitors of creatine kinase (CK) and uses thereof for treating and preventing cancer

Inventors: Nathanael S. Gray (Boston, MA); Edward Chouchani (Boston, MA); Tinghu Zhang (Brookline, MA); Narek Darabedian (Boston, MA); Wenzhi Ji (Boston, MA); Jianwei Che (Sharon, MA)
Assignee: Dana-Farber Cancer Institute, Inc.
C07D265/36C07D217/24C07D401/12C07D413/04C07D413/06C07D413/12C07D498/04C07F9/65335
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Quick Facts
Patent No.
US 12,570,620
App. No.
18/033,269
Granted
Mar 10, 2026
Kind
B2
Abstract

The present disclosure relates to compounds that are capable of inhibiting creatine kinase. The present disclosure also relates to methods of treating cancer, such as hematological malignancies.

Claims (19)

1 . A compound of Formula IV or V:

or a pharmaceutically acceptable salt thereof, wherein

R 4 is alkyl, alkenyl, alkynyl, halo, hydroxyl, carboxyl, acyl, acetyl, ester, thioester, alkoxy, phosphoryl, amino, amide, cyano, nitro, azido, alkylthio, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, heteroaralkyl, sulfonamide, aryl, heteroaryl, heterocyclyl, or aralkyl;

R 5A and R 5B are each independently selected from hydrogen, alkyl, alkenyl, alkynyl, hydroxyl, carboxyl, acyl, acetyl, ester, thioester, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, heteroaralkyl, aryl, heteroaryl, heterocyclyl, and aralkyl;

n=0-4; such that when n=0, then:

a) one of R 5A and R 5B in Formula IV are selected from alkyl, alkenyl, alkynyl, hydroxyl, carboxyl, acyl, acetyl, ester, thioester, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, heteroaralkyl, aryl, heteroaryl, heterocyclyl, and aralkyl; and

b) R 5A and R 5B in Formula V are independently selected from alkyl, alkenyl, alkynyl, hydroxyl, carboxyl, acyl, acetyl, ester, thioester, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, heteroaralkyl, aryl, heteroaryl, heterocyclyl, and aralkyl.

2 . A compound of claim 1 , where n=0-1.

3 . A compound of claim 2 , where R 4 is selected from alkyl, halo, ester, and sulfonamide.

4 . A compound of claim 3 , where R 5A is hydrogen and R 5B is alkyl.

5 . A compound of claim 1 , where the compound is of Formula IV.

6 . A compound of claim 1 , where the compound is of Formula V.

7 . A compound of claim 6 , where n=0-1.

8 . A compound of claim 7 , where R 4 is selected from alkyl, halo, ester, and sulfonamide.

9 . A compound of claim 8 , where R 5A is hydrogen and R 5B is hydrogen or alkyl.

10 . A compound of claim 1 , where the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

11 . A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutical excipient.

12 . A method of treating cancer in a subject in need therefore, comprising administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to the subject.

Continuity (2)
Provisional Application 63104963 · Oct 23, 2020
Related Publication 20230399304A1 · Dec 14, 2023
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