Soft protease inhibitors, and pro-soft forms thereof

Details Soft protease inhibitors, and pro-soft forms thereof Soft protease inhibitors, and pro-soft forms thereof

C - Chemistry, Metallurgy

07

F

C07F 5/02 (2006.01) A61K 31/69 (2006.01)

Patent

CA 2753884

The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features prosoft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia.

La présente invention concerne des composés et des procédés pour inhiber des protéases. Un aspect de l'invention concerne des inhibiteurs pro-assouplissants qui réagissent avec une protéase activatrice pour libérer un fragment inhibiteur actif à proximité d'une protéase cible. Dans certains cas, les composés inhibent des protéasomes et/ou des enzymes de clivage post-proline (PPCE), telles que la dipeptidyl-peptidase IV. Les composés de l'invention produisent un meilleur indice thérapeutique, grâce en partie à une toxicité réduite et/ou une spécificité améliorée pour la protéase ciblée. Un autre aspect de l'invention concerne l'utilisation des composés décrits pour traiter le diabète de type II, l'insulinorésistance, l'intolérance au glucose, l'hyperglycémie, l'hypoglycémie, l'hyperinsulinémie, l'obésité, l'hyperlipidémie, ou l'hyperlipoprotéinémie.

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