Telomerase inhibitors and methods of their use
AssigneeGeron Corporation
InventorsTsutomu Akama, Ryan Holcomb, Richard L. Tolman
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Abstract
Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are methods for assaying or screening for inhibitors of telomerase activity.
Claims21
A compound comprising the formula:
- 69
- wherein X is O or S;
- L1 is a direct bond, —CHR1—, or ═CR1—, wherein R1 is H or alkyl;
- A is aryl or heteroaryl;
- L2 is a direct single bond or a linking group having from 1 to 3 atoms independently selected from unsubstituted or substituted carbon, N, O or S;
- W is selected from the group consisting of 0, NR5, and S, wherein R5 is selected from the group consisting of H, alkyl, aryl, and aralkyl;
- Y and Z are independently selected to be C or N;
- and
- R2, and R3 are independently selected from the group consisting of hydrogen, hydroxyl, halogen, alkyl, aryl, alkoxyl, cyano, nitro, alkylthio, arylthio, aralkyl, and heteroaryl;
- or a pharmaceutically acceptable salt thereof.
A compound comprising the formula:
- 71
- wherein L1 is a direct bond, —CHR1—, or ═CR1—, wherein R1 is H or alkyl;
- A is aryl or heteroaryl;
- L2 is a direct single bond or a linking group having from 1 to 3 atoms independently selected from unsubstituted or substituted carbon, N, O or S;
- W is selected from the group selected from O, N R5, and S, wherein R5 is selected from the group consisting of H, alkyl, aryl, and aralkyl;
- Y and Z are independently selected to be C or N;
- and
- R2 and R3 are independently selected from the group consisting of hydrogen, hydroxyl, halogen, alkyl aryl, alkoxyl, cyano, nitro, alkylthio, arylthio, aralkyl, and heteroaryl;
- or a pharmaceutically acceptable salt thereof.
A compound comprising the formula:
- 73
- wherein L1 is a direct bond, —CHR1—, or ═CR1—, wherein R1 is H or alkyl;
- A is aryl or heteroaryl;
- L2 is a direct single bond or a linking group having from 1 to 3 atoms independently selected from unsubstituted or substituted carbon, N, O or S;
- Y and Z are independently selected to be C or N;
- and
- R2, R3 and R4 are independently selected from the group consisting of hydrogen, hydroxyl, halogen, alkyl, aryl, alkoxyl, cyano, nitro, alkylthio, arylthio, aralkyl, and heteroaryl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.