Inhibitors of dipeptidylpeptidase iv for regulating glucose...

Details Inhibitors of dipeptidylpeptidase iv for regulating glucose... Inhibitors of dipeptidylpeptidase iv for regulating glucose...

C - Chemistry, Metallurgy

07

F

C07F 5/02 (2006.01) A61K 31/69 (2006.01) A61P 3/10 (2006.01)

Patent

CA 2558106

The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods of using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

Cette invention concerne des inhibiteurs d'enzymes de clivage post-proline, tels que des inhibiteurs de la dipeptidyl peptidase IV, des compositions pharmaceutiques renfermant ces inhibiteurs, ainsi que des méthodes d'utilisation de ces inhibiteurs. En particulier, les inhibiteurs de cette invention sont meilleurs que ceux de la technique antérieure grâce à la sélection de certaines catégories de chaînes latérales en position P1 et/ou P2 de l'inhibiteur qui contiennent une fraction d'acide carboxylique. Les composés de cette invention peuvent présenter un meilleur coefficient thérapeutique grâce, notamment, à leur toxicité réduite et/ou à leur meilleure spécificité pour la protéase ciblée.

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