C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 321/00 (2006.01) A61K 31/335 (2006.01) A61K 31/357 (2006.01)
Patent
CA 2382465
The present invention provides agents and compositions for modulating the apoptotic state of a cell. The agents comprise derivatives of antimycins which bind to an anti-apoptotic Bcl-2 family member protein. Further, the agents preferentially induce apoptosis in cells that over-express anti-apoptotic Bcl-2 family member proteins and typically exhibit reduced binding affinity for cytochrome B. Pharmaceutical uses of the agents and compositions include treating apoptosis-associated disease, such as neoplasia and drug resistance, are also disclosed.
La présente invention concerne des agents et des compositions destinés à moduler l'état d'apoptose d'une cellule. Ces agents comprennent des dérivés d'antimycines qui se lient à une protéine de la famille anti-apoptose Bcl-2. En outre, les agents induisent préférentiellement l'apoptose dans des cellules qui surexpriment des protéines de la famille anti-apoptose Bcl-2 et qui montrent ordinairement une affinité de liaison réduite pour le cytochrome B. L'invention concerne aussi des utilisations pharmaceutiques des agents et des compositions comprenant le traitement de maladie associée à l'apoptose, telle que la néoplasie et la pharmacorésistance.
Hockenbery David M.
Simon Julian A.
Tzung Shie-Pon
Fred Hutchinson Cancer Research Center
Oyen Wiggs Green & Mutala Llp
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