Dimeric IAP Inhibitors
AssigneeTetraLogic Birinapant UK Ltd.
InventorsStephen M. Condon, Matthew G. Laporte, Yijun Deng, Susan R. Rippin
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AssigneeTetraLogic Birinapant UK Ltd.
InventorsStephen M. Condon, Matthew G. Laporte, Yijun Deng, Susan R. Rippin
Estimating the term…
Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language
A compound of formula (II):
The compound of claim 11, wherein R3a and R3b are independently selected from H, hydroxy, alkyloxy, aryloxy, alkylamino, dialkylamino, amido, sulfonamido, or amidino.
The compound of claim 14, wherein the optionally substituted alkyl of R5a and R5b independently is selected from alkoxylated and hydroxylated alkyls.
A pharmaceutical composition comprising:
A method for inducing apoptosis in a cell comprising contacting the cell with a compound selected from compounds of formula (I), (II), (III), (IV), (V), and (VI), in an amount sufficient to induce apoptosis in the cell.
Dependencies are inferred from the claim text.