Patent ID: 8623833

Claim:
A method of enhancing delivery of a compound across the blood-brain barrier of an animal, the method comprising contacting the blood-brain barrier with a conjugate consisting of the compound and a delivery-enhancing transporter, at a concentration effective for delivering a therapeutically effective amount across the blood-brain barrier, wherein the delivery-enhancing transporter consists of 5 to 50 amino acids that comprises 5 to 25 arginine residues or analogs thereof, thereby increasing delivery of the conjugate across the blood-brain barrier compared to delivery of the compound in the absence of the delivery-enhancing transporter, and wherein the conjugate has a structure selected from the group consisting of structures 3, 4, and 5, as follows: wherein: R 1 comprises the compound; X is a linkage formed between a functional group on the compound and a terminal functional group on the linking moiety; Y is a linkage formed from a functional group on the transport moiety and a functional group on the linking moiety; A is N or CH; R 2 is hydrogen, alkyl, aryl, acyl, or allyl; R 3 comprises the delivery-enhancing transporter; R 4 is S, O, NR 6 or CR 7 R 8 ; R 5 is H, OH, SH or NHR 6 ; R 6 is hydrogen, alkyl, aryl, acyl or allyl; R 7 and R 8 are independently selected from hydrogen or alkyl; k and m are each independently selected from 1 and 2; and n is 1 to 10.