Patent ID: 6593292
Filing Date: 2003-07-15
Classification: A61K,A61P,B82Y,C07K

Abstract:
A method for enhancing delivery of a compound into and across one or more layers of an animal epithelial or endothelial tissue, the method comprising:contacting the endothelial or epithelial tissue with a conjugate that comprises the compound attached to a delivery-enhancing transporter by a linker, wherein the delivery-enhancing transporter comprises sufficient guanidino or amidino moieties to increase delivery of the conjugate into and across one or more intact epithelial or endothelial tissue layers compared to delivery of the compound in the absence of the delivery-enhancing transporter; and the conjugate has a structure selected from the group consisting of structures 3, 4, 5 and 6, as follows: â€ƒwherein: R1â€”X comprises the compound; X is a functional group on the compound to which the linker is attached; Y is N or CH; R2 is hydrogen, alkyl, aryl, acyl, or allyl; R3 comprises the delivery-enhancing transporter; R4 is unsubstituted O, substituted N or C or substituted or unsubstituted S; R5 is OH, SH or NHR6; R6 is hydrogen, alkyl, aryl, acyl or allyl; k and m are each independently selected from 1 and 2; n is 1 to 10; and Ar is an aryl group having the attached radicals arranged in an ortho or para configuration, which aryl group can be substituted or unsubstituted.