HIRUDIN ANALOGUE OR SALT THEREOF, PRODUCTION THEREOF, AND ANTICOAGULANT CONTAINING THE SAME AS ACTIVE INGREDIENT
申请人:JAPAN ENERGY CORPORATION
公开号:EP0531537A1
公开(公告)日:1993-03-17
A hirudin analogue having high antithrombin activity and platelet aggregation resistance, represented by formula Phe-Glu-A-Ile-Pro-B-Tyr(R)-Tyr(R) and having a tyrosine residue with its hydroxyl group optionally sulfated. In the said formula, A represents Glu or Pro; B represents Glu, Tyr(R), Glu-Asp or Glu-Tyr(R); and (R) represents the hydroxyl group of a tyrosine residue or the sulfate thereof (-O-SO₃H). A process for producing a hirudin analogue by sulfating the hydroxyl group of the tyrosine residue. An anticoagulant containing the hirudin analogue (I) as the active ingredient.
一种具有高抗凝血酶活性和抗血小板聚集性的水蛭素类似物,由式 Phe-Glu-A-Ile-Pro-B-Tyr(R)-Tyr(R) 表示,其酪氨酸残基的羟基可选择硫酸化。在所述式中,A 代表 Glu 或 Pro;B 代表 Glu、Tyr(R)、Glu-Asp 或 Glu-Tyr(R);(R) 代表酪氨酸残基的羟基或其硫酸盐(-O-SO₃H)。一种通过硫酸化酪氨酸残基的羟基来生产水蛭素类似物的工艺。一种含有水蛭素类似物(I)作为活性成分的抗凝剂。