Trimethyl lock based tetrapartate prodrugs
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United States of America Patent
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Sep 23, 2003
Grant Date -
Jan 17, 2002
app pub date -
May 9, 2001
filing date -
Dec 30, 1997
priority date (Note) -
Expired
status (Latency Note)
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Abstract
The invention is directed primarily to compounds of Formula I: ##STR1## wherein: R.sub.1 is a polymeric residue; L.sub.1 is a bifunctional linking group; Y.sub.1 and Y.sub.2 are independently O, S or NR.sub.7 ; R.sub.2-7 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, substituted C.sub.1-6 heteroalkyls, C.sub.1-6 alkoxy, phenoxy and C.sub.1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.
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