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    • 1. 发明申请
    • NOVEL PEPTIDE DERIVATIVES
    • 新肽衍生物
    • WO1987005608A1
    • 1987-09-24
    • PCT/SE1987000141
    • 1987-03-19
    • KABIVITRUM AB
    • KABIVITRUM ABARIELLY, SaloGUSTAVSSON, Stig, Ake, Ingemar
    • C07K05/08
    • C07K5/06026C07K5/0817
    • Tripeptide derivatives, characterized by general formula: R1 - X - D-Arg - A - Arg - NH - R2 wherein R1 is hydrogen, alpha - or beta -naphtyl residue, lower alkyl residue which may be substituted with a carboxyl group, unsubstituted or substituted phenyl- or phenylalkyl residue. X is (I), (II), (III) or a single bond with the proviso that when R1 is hydrogen then and only then X is a single bond; A = Gly or Sar; R2 = an aromatic or heterocyclic residue which gives a compound R2-NH2 by enzymatic hydrolysis, which can be determined quantitatively; or disalts and trisalts of inorganic or organic acids thereof, process for their preparation and method for determination of serine proteases, especially Factor Xa; or components which can interact with serine proteases or zymogen forms thereof.
    • 以通式表示的三肽衍生物:R1-X-D-Arg-A-Arg-NH-R2其中R1是氢,α-或β-萘基残基,可被羧基取代的低级烷基残基,未取代或未取代的 取代的苯基或苯基烷基残基。 X是(I),(II),(III)或单键,条件是当R1是氢时,只有X是单键; A = Gly或Sar; R2 =通过酶水解得到化合物R2-NH2的芳族或杂环残基,其可以定量测定; 或其无机或有机酸的三卤化物,其制备方法和丝氨酸蛋白酶,特别是因子Xa的测定方法; 或可与丝氨酸蛋白酶或其酶原形式相互作用的组分。