Variants of hirudine or its salts, method for their production and anticoagulants having the said compounds as active ingredients

The invention relates to variants of hirudine having high anti-thrombin and anti-platelet activity, methods for their production and anticoagulants having the said variants as active ingredients. These variants of hirudine are shown by the formula (I) and contain tyrosine residues or have the hydrox...

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Hauptverfasser: AKIKO SUKESADA, RYO MURAMATSU, TADANORI MORIKAWA, KOICHI WADA, ERIKO NUKUI, SATORU MISAWA, MASAHARU NAKANO, KYOICHI KOBASHI
Format: Patent
Sprache:eng ; por
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Zusammenfassung:The invention relates to variants of hirudine having high anti-thrombin and anti-platelet activity, methods for their production and anticoagulants having the said variants as active ingredients. These variants of hirudine are shown by the formula (I) and contain tyrosine residues or have the hydroxyl group sulphated: Phen - Glu - A - Ile - Pro - B - Tyr(R) - Tyr(R) (I) In the formula A indicates Glu or Pro, B indicates Glu, Tyr(R), Glu-Asp or Glu-Tyr(R) and (R) indicates the hydroxyl group or its sulphated ester (-O-SO3H) of the tyrosine residue. The method for the production of variants of hirudine consists of sulphating the hydrxyl group of the tyrosine residues mentioned.