Invention Grant
- Patent Title: Potent conjugates and hydrophilic linkers
- Patent Title (中): 强效共轭物和亲水接头
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Application No.: US12574466Application Date: 2009-10-06
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Publication No.: US09150649B2Publication Date: 2015-10-06
- Inventor: Rajeeva Singh , Yelena Kovtun , Sharon D. Wilhelm , Ravi V. J. Chari
- Applicant: Rajeeva Singh , Yelena Kovtun , Sharon D. Wilhelm , Ravi V. J. Chari
- Applicant Address: US MA Waltham
- Assignee: ImmunoGen, Inc.
- Current Assignee: ImmunoGen, Inc.
- Current Assignee Address: US MA Waltham
- Agency: McCarter & English, LLP
- Agent Yu Lu; Xin Zhang
- Main IPC: A61K47/48
- IPC: A61K47/48 ; C07K16/28 ; A61K39/00 ; A61P35/00 ; C07D498/18 ; C07K16/30

Abstract:
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.
Public/Granted literature
- US20100129314A1 POTENT CONJUGATES AND HYDROPHILIC LINKERS Public/Granted day:2010-05-27
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