IP Library Granted Patent US 8,563,651
Granted Patent B2
US 8,563,651 · App. 13/664,021 · Granted Oct 22, 2013

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

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Quick Facts
Patent No.
US 8,563,651
App. No.
13/664,021
Granted
Oct 22, 2013
Kind
B2
Abstract

The invention provides a method comprising the steps of providing a poly(ethylene glycol) having one terminal hydroxyl group; 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 an amino acid to form an amino acid derivative; and reacting the amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate.

Claims (9)

1. A method comprising;

providing a poly(ethylene glycol)l having one terminal hydroxyl group;

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 an amino acid derivative, said amino acid derivative having the following structure:

wherein PEG is a poly(ethylene glycol) and Z is selected from the group consisting of H, N-succinimidyl, and 1-benzotriazolyl; and

reacting the amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate.

2. The method of claim 1 , wherein each PEG is capped with a capping group.

3. The method of claim 2 , wherein the capping group is methoxy.

4. The method of claim 1 , wherein the biologically active agent is a protein.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Apr 17, 2020
From: TC LENDING, LLC, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 053180/0009 →
RELEASE OF SECURITY INTEREST RECORDED AT REEL 30040, FRAME 0952 Recorded Oct 14, 2015
From: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 036855/0793 →
GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Oct 6, 2015
From: NEKTAR THERAPEUTICS
To: TC LENDING, LLC, AS COLLATERAL AGENT
Reel/Frame 036796/0562 →
SECURITY AGREEMENT Recorded Mar 19, 2013
From: NEKTAR THERAPEUTICS
To: WELLS FARGO, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 030040/0952 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 18, 2013
From: KOZLOWSKI, ANTONI
To: NEKTAR THERAPEUTICS
Reel/Frame 029659/0296 →