发明名称 |
POTENT CONJUGATES AND HYDROPHILIC LINKERS |
摘要 |
Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided. |
申请公布号 |
KR20120080611(A) |
申请公布日期 |
2012.07.17 |
申请号 |
KR20127010084 |
申请日期 |
2009.10.06 |
申请人 |
IMMUNOGEN, INC. |
发明人 |
SINGH RAJEEVA;WILHELM SHARON D.;CHARI RAVI V.J. |
分类号 |
C07D498/18;A61K31/535;A61P35/00 |
主分类号 |
C07D498/18 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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