公开(公告)号：US07067698B2

公开(公告)日：2006-06-27

申请号：US10211986

申请日：2002-08-02

申请人： Paul A. Wender ,  Christopher L. VanDeusen ,  Kanaka Pattabiraman ,  Erin T. Pelkey ,  Theodore C. Jessop

发明人： Paul A. Wender ,  Christopher L. VanDeusen ,  Kanaka Pattabiraman ,  Erin T. Pelkey ,  Theodore C. Jessop

IPC分类号： C07C277/00

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 ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

公开(公告)号：US20100081618A1

公开(公告)日：2010-04-01

申请号：US12553649

申请日：2009-09-03

申请人： Paul A. Wender ,  Jonathan B. Rothbard ,  Lee Wright ,  Erik L. Kreider ,  Christopher L. VanDeusen

发明人： Paul A. Wender ,  Jonathan B. Rothbard ,  Lee Wright ,  Erik L. Kreider ,  Christopher L. VanDeusen

IPC分类号： A61K38/16 ,  A61K38/10 ,  A61K38/08 ,  A61P43/00

CPC分类号： A61K47/64

摘要： The present invention provides compositions and methods for enhancing transport of biologically active compounds across biological membranes and across and into animal epithelial or endothelial tissues. The composition includes a biologically active agent and a transport moiety. The transport moiety includes a structure selected from the group consisting of (ZYZ)nZ, (ZY)nZ, (ZYY)nZ and (ZYYY)nZ. Subunit “Z” is L-arginine or D-arginine, and subunit “Y” is an amino acid that does not comprise an amidino or guanidino moiety. Subscript “n” is an integer ranging from 2 to 10. The method for enhancing transport involves the administration of the aforementioned composition.

摘要翻译： 本发明提供用于增强生物活性化合物跨越生物膜并跨越动物上皮细胞或内皮组织的转运的组合物和方法。 组合物包括生物活性剂和运输部分。 运输部分包括选自（ZYZ）nZ，（ZY）nZ，（ZYY）nZ和（ZYYY）nZ的结构。 亚基“Z”是L-精氨酸或D-精氨酸，亚基“Y”是不包含脒基或胍基部分的氨基酸。 下标“n”是从2到10的整数。用于增强转运的方法涉及上述组合物的给药。

公开(公告)号：US07585834B2

公开(公告)日：2009-09-08

申请号：US10078247

申请日：2002-02-14

申请人： Paul A. Wender ,  Jonathan B. Rothbard ,  Lee Wright ,  Erik L. Kreider ,  Christopher L. VanDeusen

发明人： Paul A. Wender ,  Jonathan B. Rothbard ,  Lee Wright ,  Erik L. Kreider ,  Christopher L. VanDeusen

IPC分类号： A61K38/00 ,  C12P13/10

CPC分类号： A61K47/64

摘要： The present invention provides compositions and methods for enhancing transport of biologically active compounds across biological membranes and across and into animal epithelial or endothelial tissues. The composition includes a biologically active agent and a transport moiety. The transport moiety includes a structure selected from the group consisting of (ZYZ)nZ, (ZY)nZ, (ZYY)nZ and (ZYYY)nZ. Subunit “Z” is L-arginine or D-arginine, and subunit “Y” is an amino acid that does not comprise an amidino or guanidino moiety. Subscript “n” is an integer ranging from 2 to 10. The method for enhancing transport involves the administration of the aforementioned composition.

摘要翻译： 本发明提供用于增强生物活性化合物跨越生物膜并跨越动物上皮细胞或内皮组织的转运的组合物和方法。 组合物包括生物活性剂和运输部分。 运输部分包括选自（ZYZ）nZ，（ZY）nZ，（ZYY）nZ和（ZYYY）nZ的结构。 亚基“Z”是L-精氨酸或D-精氨酸，亚基“Y”是不包含脒基或胍基部分的氨基酸。 下标“n”是从2到10的整数。用于增强转运的方法涉及上述组合物的给药。