US 6,284,871 B1 · Factor IX binding peptides, derived from factor VIII and their use as inhibitors of blood coagulation

Abstract

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.

Claims12

Dependent claims

A peptide consisting of 8-20 amino acids, wherein said peptide has within said 8-20 amino acids, a sequence of amino acids from Factor VIII, Glu-Thr-Lys-Thr-Tyr-Phe-Trp-Lys (SEQ ID NO:

1), or a sequence of amino acids from Factor VIII, Glu-Thr-Lys-Thr-Tyr-Phe-Trp-Lys (SEQ ID NO:
1) wherein one or more of the SEQ ID NO:
1 amino acids have been substituted with other amino acids, and which peptide of 8-20 amino acids binds to activated Factor IX and to its non-activated precursor.

Dependencies are inferred from the claim text.

Factor IX binding peptides, derived from factor VIII and their use as inhibitors of blood coagulation

Life of this patent

Factor IX binding peptides, derived from factor VIII and their use as inhibitors of blood coagulation

Life of this patent

Abstract

Claims12