Patent ID: 6730293
Filing Date: 2004-05-04
Classification: A61K,C07K

Abstract:
A conjugate that comprises a) a compound selected from the group consisting of a glucocorticoid, cyclosporin, FK506 and an ascomycin, and b) a delivery-enhancing transporter that comprises 5 to 25 arginine residues, wherein the conjugate is selected from the group consisting of structures 3, 4, 5 and 6, as follows: wherein:R1â€”X comprises the glucocorticoid, cyclosporin, FK506, or ascomycin; X is a functional group on the glucocorticoid, cyclosporin, FK506, or ascomycin to which the remainder of the conjugate is attached; Ar is an aryl group having the attached radicals arranged in an ortho or para configuration, which aryl group can be substituted or unsubstituted; Y is N; R2 is hydrogen, alkyl, aryl, acyl, or allyl; R3 comprises the delivery-enhancing transporter, R4 is substituted or unsubstituted S or N; R5 is NHR6; R6 is hydrogen, alkyl, aryl, acyl or allyl; k is selected from 1 and 2; and n an m are each 1.