Inhibitors of tnf-alpha secretion

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/04 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) A61K 31/66 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07C 237/22 (2006.01) C07C 259/06 (2006.01) C07C 323/41 (2006.01) C07F 9/09 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) C07K 5/068 (2006.01) C07K 5/072 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2170158

Compounds and methods are disclosed that are useful in inhibiting the TNF-.alpha. converting enzyme (TACE) responsible for cleavage of TNF-.alpha. precursor to provide biological active TNF-.alpha.. The compounds employed in the invention are peptidyl derivatives having active groups capable of inhibiting TACE such as hydroxamates, thiols phosphoryls and carboxyls.

L'invention concerne des composés et des procédés efficaces pour inhiber l'enzyme de conversion de TNF- alpha (facteur de nécrose tumorale) (TACE) responsable du clivage du précurseur du TNF- alpha , de façon à obtenir un TNF- alpha biologiquement actif. Les composés utilisés dans l'invention sont des dérivés de peptidyle possédant des groupes actifs capables d'inhiber TACE, tels que des hydroxamates, des thiols, des phosphoryles et des carboxyles.

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