发明名称 |
Method involving 1-benzotriazolyl carbonate esters of poly(ethylene glycol) |
摘要 |
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. |
申请公布号 |
US8816002(B2) |
申请公布日期 |
2014.08.26 |
申请号 |
US201314059020 |
申请日期 |
2013.10.21 |
申请人 |
Nektar Therapeutics |
发明人 |
Kozlowski Antoni |
分类号 |
C08F16/06;C08F116/06;C07D249/08;C07D401/00 |
主分类号 |
C08F16/06 |
代理机构 |
|
代理人 |
Wilson Mark A. |
主权项 |
1. A method for preparing a polymer-active agent conjugate, the method comprising:
reacting an amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate, wherein the amino acid derivative was prepared by a method comprising: providing a poly(ethylene glycol)1 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 N-succinimidyl, and wherein the biologically active agent is an oligonucleotide. |
地址 |
San Francisco CA US |