发明授权
US09211340B2 Means and methods of enhancing delivery to biological systems 有权
增强对生物系统传播的手段和方法

  • 专利标题: Means and methods of enhancing delivery to biological systems
  • 专利标题(中): 增强对生物系统传播的手段和方法
  • 申请号: US12443236
    申请日: 2007-09-26
  • 公开(公告)号: US09211340B2
    公开(公告)日: 2015-12-15
  • 发明人: Paolo Botti
  • 申请人: Paolo Botti
  • 代理机构: Pillsbury Winthrop Shaw Pittman LLP
  • 优先权: EP06020286 20060927; EP07013218 20070705
  • 国际申请: PCT/EP2007/008396 WO 20070926
  • 国际公布: WO2008/037463 WO 20080403
  • 主分类号: A61K47/48
  • IPC分类号: A61K47/48
Means and methods of enhancing delivery to biological systems
摘要:
This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (ii) at a side-chain carboxylate of one or more Asp or GIu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulfhydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and/or (v) at the N-terminus with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group, wherein said N-terminus is previously amidated with an alpha- or beta-hydroxy acid, and wherein the ester is formed between the hydroxy group of said alpha- or beta-hydroxy acid and the carboxylic group of said guanidinium alkanoic acid or said PEG substituted with a guanidinium group and a carboxyl group; and/or (b) which contains one or more disulfides, the disulfide being formed between the sulfhydryl group of a Cys reside, if present, and a guanidinium alkanethiol or a PEG substituted with a guanidinium group and a sulfhydryl group.
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