公开(公告)号：EP1461084A2

公开(公告)日：2004-09-29

申请号：EP02794232.5

申请日：2002-12-11

申请人： THE BOARD OF TRUSTEES OFTHE LELAND STANFORD JUNIOR UNIVERSITY ,  Cellgate Inc.

发明人： ROTHBARD, Jonathan, B. ,  WENDER, Paul, A. ,  PATTABIRAMAN, Kanaka ,  PELKEY, Erin, T. ,  JESSOP, Theodore, C.

IPC分类号： A61K47/48

CPC分类号： A61K47/54

摘要： Transport reagents and conjugates of therapeutic agents linked to transport reagents are described. In particular, the transport reagents have a plurality of guanidinium moieties that are either contiguous or spaced along a backbone, but are sufficiently removed from the backbone via tethers, to allow their interaction with a cell or tissue surface, leading to uptake of the therapeutic agent.

公开(公告)号：EP1419172A2

公开(公告)日：2004-05-19

申请号：EP02756928.4

申请日：2002-08-02

申请人： THE BOARD OF TRUSTEES OFTHE LELAND STANFORD JUNIOR UNIVERSITY

发明人： WENDER, Paul, A. ,  VANDEUSEN, Christopher L. ,  PATTABIRAMAN, Kanaka ,  PELKEY, Erin, T. ,  JESSOP, Theodore, C.

IPC分类号： C07K1/107

CPC分类号： C07C271/22 ,  C07K1/006

摘要： Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of φ-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

摘要翻译： 描述了适用于大规模合成低聚胍化合物如低聚精氨酸化合物的合成路线，其使用全胍基化步骤将一组φ-氨基基团转化为相应的胍基基团。 这些化合物可用作运输剂。 还描述了修饰的寡聚胍化合物。