Polymer-active agent conjugate

Patent metadata

Field	Value
Publication number	US-9839695-B2
Application number	US-201615136632-A
Country	US
Kind code	B2
Filing date	Apr 22, 2016
Priority date	Dec 22, 1999
Publication date	Dec 12, 2017
Grant date	Dec 12, 2017

Abstract

The invention provides for preparing a polymer-active agent conjugate, the method comprising the steps of reacting an amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate.

First claim

What is claimed is:

1. A polymer-active agent conjugate, the polymer-active agent conjugate prepared by a method comprising:
reacting a polymeric amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate,
wherein the polymeric amino acid derivative was prepared by a method comprising:
providing a linear poly(ethylene glycol) having one terminal hydroxyl group and having a molecular weight of about 20,000 daltons;
reacting the terminal hydroxyl group of the poly(ethylene glycol) with di(1-benzotriazolyl) carbonate to form a 1-benzotriazolylcarbonate ester of the poly(ethylene glycol);
reacting the 1-benzotriazolylcarbonate ester of the poly(ethylene glycol) with lysine to form in one or more steps a polymeric amino acid derivative, said polymeric amino acid derivative having the following structure:

wherein:
PEG is a linear poly(ethylene glycol) having a molecular weight of about 20,000 daltons,
Z is N-succinimidyl, and
the biologically active agent is an oligonucleotide.

2. The polymer-active agent conjugate of claim 1 , wherein each PEG is capped with a capping group.

3. The polymer-active agent conjugate of claim 2 , wherein the capping group is methoxy.

Assignees

• Nektar Therapeutics

Inventors

• Kozlowski Antoni

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K47/60

  the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol · CPC title

• A61K47/6901

  Conjugates being cells, cell fragments, viruses, ghosts, red blood cells or viral vectors · CPC title

• C08G65/48

  Polymers modified by chemical after-treatment · CPC title