- 专利标题: Conjugates of CC-1065 analogs and bifunctional linkers
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申请号: US15461560申请日: 2017-03-17
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公开(公告)号: US11052155B2公开(公告)日: 2021-07-06
- 发明人: Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michael Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus De Groot
- 申请人: SYNTARGA BV
- 申请人地址: NL Nijmegen
- 专利权人: SYNTARGA BV
- 当前专利权人: SYNTARGA BV
- 当前专利权人地址: NL Nijmegen
- 代理机构: Sterne, Kessler, Goldstein & Fox P.L.L.C.
- 主分类号: A61K39/44
- IPC分类号: A61K39/44 ; A61K47/64 ; A61K31/437 ; C07D471/04 ; A61K47/65 ; A61K47/60 ; A61K47/54 ; A61K38/38 ; A61K47/68
摘要:
This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
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