New conjugates of ancrod and polyalkylene glycols - for treatment of Myocardial infarction, stroke, thrombosis etc., have longer half-life than ancrod alone

    公开(公告)号:DE4041570A1

    公开(公告)日:1992-06-25

    申请号:DE4041570

    申请日:1990-12-22

    Applicant: BASF AG

    Abstract: Protein-polyalkyleneglycol derivs. of formula (A-(CH2)n-(O-(CH2)q)m-B-))pX (I) are new, where A is OH, NH2, NHCOR, OR or OCOR; R is 1-4C alkyl; n is 2, 3 or 4; m is 30-500; q is 2, 3 or 4; B is a direct bond or a linker; p is 1-10; X is a polypeptide with anerod activity which is bound via NH2 gp(s).. The polyalkylene glycol is pref. a polyethyleneglycol with a mol. wt. of 1500-15000 D.a. The protein component is anerod or anerod in which aminoacids 1-105 have been exchanged. (I) is prepd. by mixing both components in soln.. USE/ADVANTAGE - (I) Like anerod (an enzyme isolated from Agkistrodon rhodostomer) acts as a fibrinogen cleaving agent. It thus has anticoagulant properties, and can be used to treat e.g. glomeralonephritis, coronary infarction, non-ischaemic stroke, peripheral arterial circulation disorders (e.g. atherosclerosis, thromangikis and diabetic microangiopathy), angina pectoris, thromboses, and rethromboses, e.g. after surgery to implant arterial and venous prostheses. (I) Have longer half-life, better activity, immunogenicity and stability, and are more suitable for therapeutic use than anerod.

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