Substituted 4-aryl-chromene as activator of caspases and...

C - Chemistry – Metallurgy – 07 – D

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C07D 311/58 (2006.01) A61K 31/352 (2006.01)

Patent

CA 2656706

The present invention is directed to a substituted 4H-chromene represented by the Formula (1R), substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth, and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.

Cette invention concerne un 4H-chromène substitué représenté par la formule 1R, qui est sensiblement exempt du (S)-stéréoisomère correspondant. L'invention concerne également la découverte selon laquelle un composé 1R sensiblement exempt du (S)-stéréoisomère correspondant est un activateur de capsases et un inducteur d'apoptose, ainsi qu'un agent anti-vascularisation. Dans ces conditions, le composé 1R sensiblement exempt du (S)-stéréoisomère correspondant peut s'utiliser pour induire la mort cellulaire dans divers états cliniques s'accompagnant d'une croissance sauvage et d'une dissémination de cellules anormales. Le composé 1R sensiblement exempt du (S)-1stéréoisomère correspondant peut être également utilisé pour le traitement de maladies dues à une vascularisation excessive, tels que des tumeurs solides ou une néovascularisation oculaire.

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