A hydroxamic acid thrombospondin peptide analog that...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/81 (2006.01) A61K 38/10 (2006.01) A61K 38/55 (2006.01) A61K 47/16 (2006.01) A61P 19/02 (2006.01) A61P 19/04 (2006.01) C07C 259/04 (2006.01) C07C 259/06 (2006.01) C07K 7/08 (2006.01) C07K 14/78 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2453346

The present invention concerns the generation of hydroxamic acid thrombospondin-peptide analogs that inhibit aggrecanase activity. These analogs are useful in the treatment of diseases characterized by cartilage degradation, such as osteoarthritis, rheumatoid arthritis spondylarthropathies, and septic arthritis. The invention describes a novel small molecule, enzyme inhibitor that binds both the enzyme and its naturally occurring substrate.

La présente invention concerne la génération de thrombospondine peptide analogue de l'acide hydroxamique inhibant l'activité aggrécanase. Ces analogues conviennent pour le traitement d'affections marquées par la dégradation des cartilages telles que l'arthrose, les spondylarthropathies de l'arthrite rhumatoïde, et l'arthrite purulente. L'invention concerne également un inhibiteur d'enzyme à petite molécule qui se lie tant à l'enzyme qu'à son substrat naturel.

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