Method involving 1-benzotriazolyl carbonate esters of poly(ethylene glycol)

Patent metadata

Field	Value
Publication number	US-9346917-B2
Application number	US-201414467634-A
Country	US
Kind code	B2
Filing date	Aug 25, 2014
Priority date	Dec 22, 1999
Publication date	May 24, 2016
Grant date	May 24, 2016

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 water-soluble and non-peptidic polymer having the following structure

wherein:
POLY a and POLY b are each a water-soluble and non-peptidic polymer R is a central core molecule;
q is an integer from 2 to about 300; and
each X is a capping group.

2. The water-soluble and non-peptidic polymer of claim 1 , wherein each of POLY a and POLY b is the same.

3. The water-soluble and non-peptidic polymer of claim 2 , wherein each of POLY a and POLY b is a poly(ethylene glycol).

4. The water-soluble and non-peptidic polymer of claim 3 , wherein each of POLY a and POLY b has an average molecular weight from about 200 Da to about 100,000 Da.

5. The water-soluble and non-peptidic polymer of claim 1 , wherein each of POLY a and POLY b is different.

6. The water-soluble and non-peptidic polymer of claim 1 , wherein R is glycerol.

7. The water-soluble and non-peptidic polymer of claim 1 , wherein R is penaerythritol.

8. The water-soluble and non-peptidic polymer of claim 1 , wherein each X is independently selected from the group consisting of alkoxy, hydroxyl, protected hydroxyl, active ester, active carbonate, acetal, aldehyde, aldehyde hydrates, alkenyl, acrylate, methacrylate, acrylamide, active sulfone, protected amine, protected hydrazide, thiol, protected thiol, carboxylic acid, protected carboxylic acid, isocyanate, isothiocyanate, maleimide, vinylsulfone, dithiopyridine, vinylpyridine, iodoacetamide, epoxide, glyoxal, dione, mesylate, tosylate, and tresylate.

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

• A61K31/7088 Primary

  Compounds having three or more nucleosides or nucleotides · CPC title

• A61K47/6901

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