917804-48-9Relevant articles and documents
ALIPHATIC PRODRUG LINKER
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Page/Page column 24, (2008/06/13)
A polymeric prodrug is described which comprises at least one polymer attached via at least one permanent bond to a bicine linker. The bicine linker is attached via a temporary linkage to an amine containing biologically active moiety. The amine containing biologically active moiety - such as a drug - can be released by cleaving the temporary linkage. In one example, the prodrug of or corresponding polymeric prodrug linker reagent has the following structure: (formula Ia)in which T is D or A (D being a residue of an amine containing biologically active moiety and A being a leaving group). X is a spacer moiety such as R13-Y1. Y1 is O, S, NR6, succinimide, maleimide, unsaturated carbon-carbon bonds or any heteratom containing a free electron pair or is absent. Rl 3 is selected from substituted or non-substituted linear, branched or cyclical alkyl or heteroalkyl, aryls, substituted aryls, substituted or non-substituted heteroaryls. R2 and R3 are selected independently from hydrogen, acyl groups, or protecting groups for hydroxyl groups. R4 to R12 are selected independently from hydrogen, X-Rl, substituted or non-substituted linear, branched or cyclical alkyl or heteroalkyl, aryls, substituted aryls, substituted or non-substituted heteroaryls, cyano, nitro, halogen, carboxy, carboxamide. R1 is a polymer. In other examples the polymer Rl is placed at other positions.
