Metalloprotease inhibitors

Abstract

Matrix metalloprotease (MMP) inhibitors have therapeutic potential in a wide range of important human diseases such as cancer, arthritis and multiple sclerosis. Over the last decade, a large number of pharmaceutical companies have initiated active programmes in the area and there are at least six orally bioavailable MMP inhibitors currently in clinical trials. This patent claims a structurally novel series of MMP inhibitors based on a 2,5-diketopiperazine scaffold. Compounds within this application have a promising in vitro profile, with nM potency against MMP-1 and MMP-9. However, since no in vivo efficacy or pharmacokinetic data have, as yet, been presented, it is not possible to ascertain whether this series will offer any advantage over current inhibitors.

• arthritis
• cancer
• diketopiperazines
• matrix metalloprotease inhibitors