Improved specificity in treatment of diseases

Details Improved specificity in treatment of diseases Improved specificity in treatment of diseases

C - Chemistry, Metallurgy

07

H

C07H 19/052 (2006.01) C07H 19/056 (2006.01)

Patent

CA 2416748

A drug is modified by covalently coupling a blocking group to the drug via a nitrogen atom in the blocking group. The blocking group in the modified drug prevents metabolic conversion and sequestration of the drug in non-target cells, and the blocking group is enzymatically removed in the target cell. Particularly contemplated advantages of presented compounds and methods include reduction of cytotoxicity by inhibition of metabolic conversion to potentially cytotoxic metabolites, reduction of dosages of drugs by reduction of sequestration into non-target cells, and increase of selectivity of a drug.

Selon l'invention, on modifie un médicament en couplant par covalence un groupe de blocage au médicament via un atome d'azote dans le groupe de blocage. Ce groupe de blocage présent dans le médicament modifié empêche la conversion et la séquestration métaboliques du médicament dans des cellules non-cibles et le groupe de blocage est enlevé de manière enzymatique dans la cellule cible. Parmi les avantages des composés et des méthodes de l'invention qui sont considérés avec une attention particulière, on trouve la réduction de la cytotoxicité par inhibition de la conversion métabolique en métabolites potentiellement cytotoxiques, la réduction des dosages de médicaments par réduction de la séquestration dans des cellules non-cibles et l'augmentation de la sélectivité d'un médicament.

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