Hirudin peptide derivatives

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/06 (2006.01) A61K 38/00 (2006.01) A61K 38/04 (2006.01) A61K 38/16 (2006.01) A61K 38/58 (2006.01) A61K 51/08 (2006.01) A61L 33/00 (2006.01) A61L 33/12 (2006.01) C07K 7/08 (2006.01) C07K 14/815 (2006.01)

Patent

CA 2064195

2064195 9101328 PCTABS00003 This invention relates to novel, biologically active peptide derivatives which inhibit the fibrinolytic, but not the amidolytic activity of thrombin. The peptide derivatives, which display partial homology to the carboxy terminal portion of hirudin, are characterized by a modified tyrosine or cysteine residue at a predetermined site in the molecule. This invention also relates to compositions and methods employing such peptide derivatives for therapeutic, prophylactic or diagnostic purposes. This invention also relates to platelet and endothelial cell inhibitory compositions and methods characterized by the above-described peptide derivatives or similar peptide derivatives which do not contain a modified cysteine or tyrosine residue at a corresponding locus in the molecule. These methods and compositions are advantageously useful for decreasing or preventing platelet aggregation and platelet activation in a patient or in extracorporeal blood, especially in patients who have a history of heparin-induced thrombocytopenia.

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