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    • 101. 发明公开
    • Protein derivatives and a process for their preparation
    • 蛋白衍生物和Verfahren zu ihrer Herstellung。
    • EP0360433A1
    • 1990-03-28
    • EP89308680.1
    • 1989-08-25
    • Offord, Robin Ewart
    • Offord, Robin EwartRose, Keith
    • C07K3/08A61K39/44A61K47/00G01N33/543
    • G01N33/532A61K47/62A61K47/6889C07K1/1072
    • Protein derivatives of formula (1)
      A-CO-N(R¹)CH₂-Z-R²      (1)
      wherein A-CO is the residue of a protein or peptide A-CO₂H (especially where -CO₂H is the C-terminal carboxyl group of the protein or peptide); R¹ is a hydrogen atom or an alkyl, aryl or aralkyl group; Z¹, which may be present or absent is a spacer group; R² is a group -C(OH)(R³)CH₂NHR⁴ or -C(R³)O (where R³ and R⁴ which may be the same or different, is each a hydrogen atom or an alkyl, aryl or aralkyl group); with the proviso that when A-CO is a residue of insulin, R¹ is other than a hydrogen atom; and the salts thereof. The compounds may be prepared by a condensation reaction,, especially in the presence of an enzyme capable of catalysing the formation of a peptide bond. The compounds may be used to form protein conjugates in which a group of interest such as another protein or peptide or an effector or reporter group is coupled to the protein through a -N(R¹)CH₂-Z¹-C(OH)(R³)CH₂N= or -N(R¹)CH₂Z¹-CH= group.
    • 式(1)的蛋白衍生物A-CO-N(R 1)CH 2 -ZR 2(1)其中A-CO是蛋白质或肽A-CO 2 H的残基(特别是其中-CO 2 H是C - 蛋白质或肽的末端羧基); R 1是氢原子或烷基,芳基或芳烷基; 可能存在或不存在的Z 1是间隔基; R 2是基团-C(OH)(R 3)CH 2 NHR 4或-C(R 3)O(其中R 3和R 4可以相同或不同) 各自为氢原子或烷基,芳基或芳烷基); 条件是当A-CO是胰岛素的残基时,R 1不是氢原子; 及其盐。 化合物可以通过缩合反应制备,特别是在能够催化形成肽键的酶的存在下。 所述化合物可用于形成蛋白质缀合物,其中目标组如另一蛋白质或肽或效应物或报道基团通过-N(R 1)CH 2 -Z 1 -C (OH)(R 3)CH 2 N =或-N(R 1)CH 2 Z 1 -CH =基团。
    • 102. 发明公开
    • Protein derivatives and a process for their preparation
    • 蛋白质衍生物及其制备方法
    • EP0359428A1
    • 1990-03-21
    • EP89308681.9
    • 1989-08-25
    • Offord, Robin EwartRose, Keith
    • Offord, Robin EwartRose, Keith
    • C07K1/107A61K47/00G01N33/543
    • G01N33/5748A61K47/62C07K1/1072G01N33/532
    • Protein derivatives of formula (1) A-CO-N(R 1 )N(R 2 )-Z 1 -
      wherein A-CO is the residue of a protein or peptide A-CO 2 H (especially where -C0 2 H is the C-terminal carboxyl group of the protein or peptide); R 1 , R 2 , R 3 and R 4 , which may be the same or different, and which may be present or absent, is each a spacer group, X is an oxygen or sulphur atom; and the salts thereof. The compounds may be prepared by a condensation reaction, especially in the presence of an enzyme capable of catalysing the formation of a peptide bond. The compounds may be used to form protein conjugates in which a group of interest such as another protein or peptide or an effector or reporter group is coupled to the protein through a -N-(R 1 )N(R 2 )-Z 1 -C(=X)-Z 2 -N(R 3 )N= group.
    • 式(1)的蛋白质衍生物A-CO-N(R1)N(R2)-Z1-其中A-CO是蛋白质或肽A-CO2H的残基(尤其是其中-CO2H是C端羧基 蛋白质或肽); R 1,R 2,R 3和R 4可以相同或不同,并且可以存在或不存在,各自为间隔基团,X为氧或硫原子; 及其盐。 化合物可以通过缩合反应来制备,特别是在能够催化形成肽键的酶的存在下。 该化合物可用于形成蛋白质偶联物,其中一组目的基团如另一种蛋白质或肽或效应物或报道基团通过-N-(R 1)N(R 2)-Z 1 -C(= X)-Z 2 -N(R 3)N =基团。