Derivatives of gambogic acid and analogs as activators of...

C - Chemistry – Metallurgy – 07 – D

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C07D 493/20 (2006.01) A61K 31/352 (2006.01) A61K 31/4523 (2006.01) A61K 31/495 (2006.01) A61K 31/5375 (2006.01)

Patent

CA 2491698

The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Cette invention a trait à des dérivés d'acide de gomme-gutte et aux analogues. Parmi les dérivés présentés à titre d'exemple, figurent, entre autres, des dérivés substitués en position C10 et C28 de l'acide de gomme-gutte. Elle traite également de la découverte selon laquelle certains composés préférés sont des activateurs des caspases et provoquent l'apoptose. Il est, de ce fait, possible d'utiliser ces activateurs et inducteurs pour provoquer une mort cellulaire dans différentes conditions cliniques non maîtrisées, au cours desquelles se produisent une croissance et un étalement incontrôlés de cellules anormales.

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