TETRACYCLINES AND THEIR USE AS CALPAIN INHIBITORS

WIPO Patent Application WO2005082860

A8

Tetracyclines are useful as calpain inhibitors, particularly inhibitors of calpain I and II, as demonstrated in enzymatic assays as well as at the cellular and animal levels. Tetracyclines may be used in the treatment of a wide range of conditions implicated by or associated with calpain activity or activation, including cellular protection from apoptosis and necrosis, particularly n eu ro protection, prevention of cell motility (e.g. anti-metastasis of cancer) and treatment of certain infectious diseases (e.g. malaria and AIDS). Some tetracyclines are particularly useful as calpain inhibitors since they are also antioxidants, oxidative stress often being associated with conditions where calpain is activated.

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ANGUSTI ANGELA (CA)
HOU SHENG T (CA)
JIANG XIUXIAN SUSAN (CA)
KOMATSU HIROTO (CA)
KONISHI YASUO (CA)
KUBO TAKAHIRO (CA)
LERTVORACHON JITTIWUD (CA)
ROMAN GHEORGHE (CA)

PCT/CA2005/000279

December 08, 2005

February 25, 2005

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CA NAT RESEARCH COUNCIL (CA)
ANGUSTI ANGELA (CA)
HOU SHENG T (CA)
JIANG XIUXIAN SUSAN (CA)
KOMATSU HIROTO (CA)
KONISHI YASUO (CA)
KUBO TAKAHIRO (CA)
LERTVORACHON JITTIWUD (CA)
ROMAN GHEORGHE (CA)

A61K31/65; A61P9/10; A61P25/00; A61P39/06; C07C235/40; C07C237/26; C07D221/18; C07D231/12; (IPC1-7): C07D231/12; A61K31/65; A61P9/10; A61P25/00; A61P39/06; C07C235/40; C07C237/26; C07D221/18

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