Factor ix binding peptides, derived from factor viii and...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/755 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/37 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2221567

The present invention relates to biologically active peptides which specifically inhibit the Factor IX-dependent pathway of blood coagulation. These peptides are based on a specific motif which represents a sequence of Factor VIII (amino acid 1811-1818) involved in binding to activated Factor IX as well as to the intact Factor IX zymogen. Binding of said peptides to Factor IX or activated derivatives thereof effectively inhibits complex assembly with Factor VIII. These peptides thereby specifically interfere in the Factor IX- dependent pathway of thrombin formation, while leaving other haemostatic pathways unaffected. By virtue of this unique specificity, the peptides of this invention are particularly useful in novel pharmaceutical compositions for the treatment of thrombotic disorders.

La présente invention concerne des peptides biologiquement actifs qui inhibent spécifiquement le processus de coagulation sanguine dépendant du facteur IX. Ces peptides sont basés sur un motif spécifique qui représente une séquence du facteur VIII (acide aminé 1811-1818) impliqué dans la liaison au facteur IX activé, ainsi qu'au zymogène intact du facteur IX. La liaison de ces peptides au facteur IX ou à des dérivés activés de celui-ci inhibe efficacement la formation du complexe avec le facteur VIII. Ces peptides interfèrent ainsi de manières spécifique avec le processus de formation de la thrombine dépendant du facteur IX, tout en n'exerçant aucune influence sur les autres processus hémostatiques. Grâce à cette spécificité très particulière, les peptides de cette invention permettent de réaliser de nouvelles compositions pharmaceutiques très utiles contre les troubles thrombotiques.

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