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Abstract

A compound of Formula I, providing tetrapartate prodrugs is provided ##STR1## wherein: L.sub.1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D].sub.y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof, Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are each independently O, S, or NR.sub.12 ; R.sub.11 is a mono- or divalent polymer residue; R.sub.1, R.sub.4, R.sub.9, R.sub.10 and R.sub.12 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls and substituted C.sub.1-6 heteroalkyls; R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-8 heteroalkyls, C.sub.1-8 heteroalkoxy, substituted C.sub.1-6 alkyls, C.sub.3-8 cycloalkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro- and cyano-, carboxy-, C.sub.1-6 carboxyalkyls and C.sub.1-6 alkylcarbonyls; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m), (r), (s), (t), and (u) are independently zero or one; (p) is zero or a positive integer; and (y) is 1 or 2; together with methods of preparing and using these new tetrapartate prodrugs.

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First Claim