Hirudin variants or their salts, method for their production...

C - Chemistry – Metallurgy – 12 – P

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C12P 21/02 (2006.01) A61K 38/08 (2006.01) A61K 38/58 (2006.01) C07K 1/02 (2006.01) C07K 7/06 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2081305

ABSTRACT The present invention relates to hirudin variants having high anti-thrombin and anti-platelet activity, methods for producing them, and anti-coagulants having said variants as active ingredients. Hirudin variants shown in formula (I) having tyrosine residues or having their hydroxyl group sulfated. Methods for producing hirudin variants by sulfating hydroxyl group of said tyrosine residues, and anti-coagulants having hirudin variants shown in formula (I) as active ingredients. Phe-Glu-A-Ile-Pro-B-Tyr(R)-Tyr(R) (I) [In the formula, A represents Glu or Pro, B represents Glu, Tyr (R), Glu-Asp or Glu-Tyr(R), and (R) represents the hydroxy group or its sulfated ester (-O-SO3H) of tyrosine residue.] 62

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