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ORALLY ADMINISTERED BIOLOGICALLY ACTIVE PEPTIDES AND PROTEINS

机译:口服修饰的生物活性肽和蛋白质

摘要

Composition of peptides or biologically active proteins and effective enterally, comprising a complex comprising a sandwich complex hydrophobe core of a peptide or a biologically active protein with an alkyl or alkenyl sulfate having 6 to 24 carbon atoms and 0 to 3 double bonds, forming an electrostatic complex with a corresponding flexible binder quaternary ammonium of the formula NR1R2R3R4 wherein R1 represents a C1 - C12 - C12 - alkyl; R2 and R3 independently represent hydrogen or a C1-C12-alkyl; and R4 represents hydrogen or a radical of the formula (I) wherein R5 is hydrogen and R6 is alkenyl or linear alkyne having 6 to 22 carbon atoms and from 0 to 3 double bonds; or R1 and R2 together represent a bivalent radical of the formula - CH2-, -CH2 -, -CH = CH -N = CH-, or -CH2OH2CH2- and R3 and R4 are as defined above; provided that R1, R2 or R3 may be optionally substituted with a hydroxyl group or an alkoxyl group of formula -OR4, where R4 is an alkyl group having 1 to 4 carbon atoms; that when R1 and R2 together represent a bivalent radical, the radical may be substituted by methyl, by hydroxyl, R1O -OR4; and that when R2 is hydrogen, R1 is not methyl.
机译:肽或生物活性蛋白的组合物,其对肠内有效,包含一种复合物,该复合物包含肽或生物活性蛋白的三明治复合物疏水核心与具有6至24个碳原子和0至3个双键的烷基或链烯基硫酸盐形成静电与相应的式NR1R2R3R4的柔性粘合剂季铵盐的配合物,其中R1代表C1-C12-C12-烷基; R 2和R 3独立地表示氢或C 1 -C 12烷基; R4代表氢或式(I)的基团,其中R5为氢,R6为具有6至22个碳原子和0至3个双键的烯基或直链炔。或R 1和R 2一起表示式-CH 2-,-CH 2-,-CH = CH -N = CH-或-CH 2 OH 2 CH 2-的二价基团,并且R 3和R 4如上所定义。条件是R1,R2或R3可以任选地被式-OR4的羟基或烷氧基取代,其中R4是具有1-4个碳原子的烷基;当R 1和R 2一起代表二价基团时,该基团可以被甲基,羟基,R 10 -OR 4取代;并且当R 2是氢时,R 1不是甲基。

著录项

  • 公开/公告号EP0129582A1

    专利类型

  • 公开/公告日1985-01-02

    原文格式PDF

  • 申请/专利权人 RESEARCH CORPORATION;

    申请/专利号EP19840900255

  • 发明设计人 TENG LIN-NAR L.;

    申请日1983-12-12

  • 分类号A61K38/00;A61K9/00;A61K9/08;A61K38/22;A61K38/28;A61K47/48;

  • 国家 EP

  • 入库时间 2022-08-22 08:02:47

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