Tetralogic Pharmaceuticals Corporation

Tetralogic Birinapant UK Ltd.

Medivir Ab

Wyeth

Viropharma Incorporated

Stephen M. Condon

Susan R. Rippin

Yijun Deng

Matthew G. Laporte

Matthew G Laporte

Stephen M Condon

Susan R Rippin

Matthew D Alexander

Christopher J Burns

Ariamala Gopalsamy

John W Ellingboe

Tarek Suhayl Mansour

Kaapjoo Park

Susan R Rippen

Marc S Collett

A SMAC mimetic and pharmaceutical compositions thereof and methods of use.

SMAC mimetic

SMAC Mimetic

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.

Dimeric IAP inhibitors

IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kof less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.

IAP binding compounds

SMAC mimetic for treating myelodysplastic syndromes

IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kof less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.

The present invention describes compounds of the formula 

IAP inhibitors

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Honey Brook, PA, United States of America

Matthew G Laporte