Acid labile prodrugs

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 315/00 (2006.01) A61K 31/22 (2006.01) A61K 31/35 (2006.01) C07H 15/234 (2006.01) C07H 15/252 (2006.01)

Patent

CA 2325542

The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and a blocking group, characterized by the presence of a covalent bond which is cleaved at pH values below 7Ø The prodrug may be used in a technique for treating a condition or disease in a mammal related to elevated hydrogen ion concentrations, whereby on administering it to a mammal having such a condition or disease, the pharmacologically active compound is activated selectively within tissues having such elevated hydrogen ion concentrations.

L'invention concerne un bioprécurseur pharmaceutiquement acceptable qui est un conjugat covalent d'un composé pharmacologiquement actif et un groupe de blocage, caractérisé par la présence d'une liaison covalente et clivé à des valeurs de pH inférieures à 7,0. Le bioprécurseur peut être utilisé dans le traitement d'une pathologie ou d'une maladie chez un mammifère liée à des concentrations élevées en ions hydrogène. Lors de l'administration du bioprécurseur précité à un mammifère souffrant d'une pathologie ou maladie, le composé pharmacologiquement actif est activé de manière sélective dans les tissus présentant des concentrations élevées en ions hydrogène.

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