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
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