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US 2023/0399304 A1Published application
Covalent inhibitors of creatine kinase (ck) and uses thereof for treating and preventing cancer
AssigneeDana-Farber Cancer Institute, Inc.
InventorsNathanael S. Gray, Edward Chouchani, Tinghu Zhang, Narek Darabedian, Wenzhi JI, Jianwei Che
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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.
Claims90
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein
- A is a five or six membered aryl or heteroaryl ring;
- E is an electrophile;
- X1 is a bond, O, NR3A, CR3AR3B, or S;
- R1A is alkyl, alkyloxy, cycloalkyloxy, aryloxy, heteroaryloxy, amino, cycloalkyl, heterocyclyl, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, amide, ester, urea, or carbamate;
- or R1A and R1B combine to form a cycloalkyl or heterocyclyl;
- R1B, R2A, R2B, R3A, and R3B are each independently selected from H, alkyl, aralkyl, acyl, amide, carboxyl, ester, and carbamate;
- R4 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;
- and
- n is 0-5.
7 more elements
Dependencies are inferred from the claim text.