Hydroxylation activated drug release

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/48 (2006.01) A61K 31/265 (2006.01) A61K 31/27 (2006.01) A61K 31/352 (2006.01) A61K 31/513 (2006.01) A61K 31/538 (2006.01) A61K 31/565 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2319837

The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.

L'invention concerne des promédicaments dont l'oxydation aromatique, en particulier, l'hydroxylation aromatique, enzymatique, produit leur activation par libération d'une fraction de médicament. L'invention concerne, en particulier, des promédicaments antitumoraux ainsi que ceux activés, de manière spécifique, par l'activité d'hydroxylation de l'enzyme CYP1B1 de P-450. L'invention concerne également des techniques de détection d'activité d'oxydation aromatique.

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