Lactams as conformationally constrained peptidomimetic...

C - Chemistry – Metallurgy – 07 – D

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C07D 207/273 (2006.01) A61P 3/00 (2006.01) C07D 487/10 (2006.01)

Patent

CA 2555961

The present invention relates to inhibitors of post-proline cleaving enzyme, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention incorporate a lactam ring in the backbone of the inhibitors. 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 comprennent un noyau lactame dans le squelette des inhibiteurs. 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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