GB2427360A — Aliphatic prodrug linker

USPTO Abstract

A polymeric prodrug 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, such as a drug, which can be released by cleaving the temporary linkage. The prodrug or corresponding polymeric prodrug linker reagent may have the following structure: <EMI ID=1.1 HE=47 WI=76 LX=335 LY=762 TI=CF> <PC>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, R13 is substituted or non-substituted linear, branched or cyclical alkyl or heteroalkyl, aryls, substituted aryls, substituted or non-substituted heteroaryls, R2 and R3 are hydrogen, acyl groups, or protecting groups for hydroxyl groups, R4 to R12 are hydrogen, X-R1, substituted or non-substituted linear, branched or cyclical alkyl or heteroalkyl, aryls, substituted aryls, substituted or non-substituted heteroaryls, cyano, nitro, halogen, carboxy, carboxaxnide and R1 is a polymer. In other examples the polymer R1 is placed at other positions.