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    • 6. 发明授权
    • Synthesis of asparagine-linked glycopeptides on a polymeric solid support
    • 在聚合物固体支持物上合成天冬酰胺连接的糖肽
    • US5679769A
    • 1997-10-21
    • US477776
    • 1995-06-07
    • Samuel J. DanishefskyJacques RobergeXenia Beebe
    • Samuel J. DanishefskyJacques RobergeXenia Beebe
    • A61K38/00A61K39/00C07H3/06C07H15/10C07H15/18C07H17/02C07K1/04C07K9/00C07K16/30C07K16/44A61K31/02
    • A61K39/0011C07H15/10C07H15/18C07H17/02C07H3/06C07K1/04C07K16/3015C07K16/44C07K9/005A61K38/00
    • The present invention provides a process for synthesizing a glycopeptide having the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each independently H, OH, OR.sup.1, NH.sub.2, NHCOR.sup.i, F, CH.sub.2 OH, CH.sub.2 OR.sup.i, or a substituted or unsubstituted linear or branched chain alkyl, arylalkyl or aryl group, where R.sup.i is H, CHO, CO.sub.2 R.sup.ii, a linear or branched chain alkyl, arylalkyl or aryl group, or an oligosaccharide moiety, etc., wherein R.sub.0 is H, a linear or branched chain alkyl, arylalkyl or aryl group; wherein R.sub.10 is a substituted or unsubstituted linear or branched chain acyl, arylacyl or aroyl group; wherein R.sub.11�x! represents X amino acid side-chains, and denotes position from the N-terminus, and R.sub.13�y! represents Y amino acid side-chains, and denotes position from the C-terminus, wherein a, b, c, h, i, j, r, s and t are each independently an integer between about 0 and about 3; wherein m and n are each independently an integer between about 0 and about 5; and wherein x, x'(N), y and y'(N) are each independently an integer between about 0 and,about 25; such glycopeptides being useful as a vaccine for inducing antibodies to human breast cancer cells in an adjuvant therapy therefor.
    • 本发明提供一种合成具有以下结构的糖肽的方法:其中R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8各自独立地为H,OH,OR 1,NH 2,NHCOR 1 ,F,CH2OH,CH2ORi或取代或未取代的直链或支链烷基,芳烷基或芳基,其中R 1为H,CHO,CO 2 R 11,直链或支链烷基,芳烷基或芳基或寡糖部分等 其中R 0是H,直链或支链烷基,芳烷基或芳基; 其中R 10是取代或未取代的直链或支链酰基,芳基酰基或芳酰基; 其中R11 [x]表示X氨基酸侧链,表示从N-末端的位置,R13 [y]表示Y氨基酸侧链,表示C末端的位置,其中a,b,c ,h,i,j,r,s和t各自独立地为约0和约3之间的整数; 其中m和n各自独立地为约0和约5之间的整数; 并且其中x,x'(N),y和y'(N)各自独立地为约0和约25之间的整数; 这样的糖肽可用作用于在其辅助治疗中诱导人乳腺癌细胞的抗体的疫苗。