INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING VLA-4

摘要

The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.;

主权项

1. A compound of formula I: or a pharmaceutically acceptable salt or ester thereof; wherein n is 1-24 and wherein: R1 is selected from the group consisting of:
(1) a compound of the formula: wherein m is 0-3 and G is selected from the group consisting of: (2) a compound of the formula: wherein m is 0-3, R4 and R5 are independently hydrogen or halogen, W is O or CH2, and G is selected from the group consisting of:  and(3) a compound of the formula: R2 is selected from the group consisting of:
(1) a compound of the formula: (2) a compound of the formula: (3) a compound of the formula:  and(4) a compound of the formula: wherein R3 is a conjugated moiety and X represents either sulfur or a compound of the formula: