首页> 外国专利> CYCLODEXTRIN DIMERS WITH SPACERS HAVING PEPTIDE STRUCTURES FOR ENCAPSULATION OF PHARMACEUTICALLY ACTIVE SUBSTANCES WITH POTENTIAL HIGH SIDE-EFFECTS

CYCLODEXTRIN DIMERS WITH SPACERS HAVING PEPTIDE STRUCTURES FOR ENCAPSULATION OF PHARMACEUTICALLY ACTIVE SUBSTANCES WITH POTENTIAL HIGH SIDE-EFFECTS

机译:具有肽结构的间隔环环糊精,用于包封具有潜在高副作用的药物活性物质

摘要

A rigidly spaced, cyclodextrin dimers having a preselected breaking point within the spacer sequence so as to controllably release the active pharmaceutically active substance only after it reaches the desired treatment site is described. These preselected breaking points are stable in blood but are cleavable within cells. In preferred embodiments, the cyclodextrin-pharmaceutically active substance complex is targeted to specific sites via incorporation of specific antibodies for the targeted sites, typically by complexing a biotin-avidin system to specific antibodies which thereby targets the complex to a specific site. Once at the site as the complex is taken up into the cell the preselected break point is cleaved and the encapsulated pharmaceutically active substance becomes available for action within the targeted cell. This approach permits the use of highly effective and efficient pharmaceutically active substances, whose safety restricts use to last chance efforts or which are unable to qualify for human use due to their potential side effects. In a preferred embodiment peptide structures are used as part of the spacers between bridged cyclodextrins The cyclodextrin oligomers are complexed with pharmaceuticals with potential high side effects to safely, efficiently achieve the therapeutic action dsired.
机译:描述了在间隔序列内具有预先选择的断裂点的刚性间隔的环糊精二聚体,以便仅在活性药物活性物质到达所需的治疗部位后才可控制地释放活性药物活性物质。这些预先选择的断裂点在血液中稳定,但在细胞内可裂解。在优选的实施方案中,通常通过将生物素-亲和素系统与特异性抗体复合,从而将复合物靶向特定位点,通过掺入针对靶向位点的特异性抗体将环糊精-药物活性物质复合物靶向至特定位点。一旦在复合物被吸收到细胞中的位置,就裂解了预先选择的断裂点,并且包囊的药物活性物质变得可用于在靶细胞内起作用。该方法允许使用高效和高效的药物活性物质,其安全性限制了最后的努力使用,或者由于其潜在的副作用而不能用于人类。在优选的实施方案中,肽结构用作桥连的环糊精之间的间隔物的一部分。环糊精低聚物与具有潜在高副作用的药物复合,以安全,有效地实现所需的治疗作用。

著录项

  • 公开/公告号EP1265930A4

    专利类型

  • 公开/公告日2005-12-21

    原文格式PDF

  • 申请/专利权人 CERAMOPTEC GMBH;

    申请/专利号EP20010904865

  • 发明设计人 MOSER JOERG G.;HOFFMANN RALPH;

    申请日2001-01-12

  • 分类号C12N9/48;C08B30/18;C08B37/16;A61K31/715;C07K5/00;

  • 国家 EP

  • 入库时间 2022-08-21 21:33:13

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