Leland Stanford Junior University

Cellgate, Inc.

Christopher L VanDeusen

Paul A Wender

Jonathan B Rothbard

Erik Kreider

Lee Robert Wright

Kanaka Pattabiraman

Erin T Pelkey

Theodore C Jessop

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)Z, (ZY)Z, (ZYY)Z and (ZYYY)Z. 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 &#x201c;n&#x201d; is an integer ranging from 2 to 10. The method for enhancing transport involves the administration of the aforementioned composition.

Transporters comprising spaced arginine moieties

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 &#x3c9;-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

Bi-directional synthesis of oligoguanidine transport agents

Growing community of inventors

Columbus, CA, United States of America

Christopher L VanDeusen