Glycopeptides, process for their preparation and their use
    4.
    发明授权
    Glycopeptides, process for their preparation and their use 失效
    糖肽,其制备方法及其用途

    公开(公告)号:US4719289A

    公开(公告)日:1988-01-12

    申请号:US776380

    申请日:1985-09-16

    摘要: Compounds of the general formula I, II or IIIR.sup.1 --A.sup.1 --T--NH--R.sup.2 --COR.sup.3 IR.sup.1 --A.sup.1 --T--A.sup.2 --NH--R.sup.2 --COR.sup.3 IIR.sup.1 --A.sup.1 --T--A.sup.2 --A.sup.3 --T--A.sup.4 --NH--R.sup.2 --COR.sup.3 IIIare described, in whichR.sup.1 is a hydrogen atom, an alkoxycarbonyl or arylalkoxycarbonyl group conventionally used for protecting amino groups, or CH.sub.3 --(CH.sub.2).sub.m --CO, in which m=0-16,R.sup.2 is --(CH.sub.2).sub.n -- or --(CHOH).sub.n --, in which n=1-10,R.sup.3 is a hydroxyl group, an 0-alkyl or 0-arylalkyl protecting group, a group which activates carboxyl groups, a cephalin radical, an amino acid radical of oligopeptides, polypeptides or proteins which carries NH groups, or a carrier,A.sup.1, A.sup.2, A.sup.3 or A.sup.4 is a bonding dash or an amino acid radical present in glycophorin A, such as Ala, Val, Leu, Ile, Ser, Pro, Glu or Arg, in which, if appropriate, the reactive groups not forming part of the peptide bond are protected by protecting groups, and the radical T is ##STR1## in which R.sup.4 denotes a hydrogen atom or an acyl protecting group,R.sup.5 denotes a hydrogen atom, an acyl protecting group or the 2,3,4,6-tetra-0-acetyl-beta-D-galactopyranosyl or beta-D-galactopyranosyl radical,R.sup.6 denotes N.sub.3, NH.sub.2 or NHAc andR.sup.7 denotes H or CH.sub.3,together with a process for their preparation and their use, bound to a carrier, as artificial antigens, glycolipids or immunoadsorbents.

    摘要翻译: 通式I,II或III的化合物R1-A1-T-NH-R2-COR3I R1-A1-T-A2-NH-R2-COR3II R1-A1-T-A2-A3-T-A4-NH- 描述了其中R 1是氢原子,通常用于保护氨基的烷氧基羰基或芳基烷氧基羰基或其中m = 0-16的R 3 - (CH 2)m -CO,R 2是 - (CH 2) 正 - 或 - (CHOH)n - ,其中n = 1-10,R3是羟基,O-烷基或O-芳基烷基保护基,活化羧基的基团,头孢菌素基团,氨基酸基团 携带NH基团的载体,A1,A2,A3或A4的寡肽,多肽或蛋白质是血型糖蛋白A中存在的结合破伤或氨基酸,例如Ala,Val,Leu,Ile,Ser,Pro, Glu或Arg,其中如果合适的话,不形成肽键部分的反应性基团被保护基团保护,并且基团T是其中R 4表示氢原子或酰基保护基,R 5表示 氢原子,酰基保护基或2,3,4,6-四 a-O-乙酰基-β-D-吡喃半乳糖基或β-D-吡喃半乳糖基,R6表示N3,NH2或NHAc,R7表示H或CH3,以及其制备方法及其用途,结合载体,如 人造抗原,糖脂或免疫吸附剂。