| 发明名称 | Conjugates of CC-1065 analogs and bifunctional linkers | ||
| 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. | ||
| 申请公布号 | US9629924(B2) | 申请公布日期 | 2017.04.25 |
| 申请号 | US201113642847 | 申请日期 | 2011.04.21 |
| 申请人 | Syntarga BV | 发明人 | Beusker Patrick Henry;Coumans Rudy Gerardus Elisabeth;Elgersma Ronald Christiaan;Menge Wiro Michael Petrus Bernardus;Joosten Johannes Albertus Frederikus;Spijker Henri Johannes;De Groot Franciscus Marinus Hendrikus |
| 分类号 | A61K47/48;C07D495/04;A61K31/437;C07D471/04;A61K38/38;A61K39/44 | 主分类号 | A61K47/48 |
| 代理机构 | Sterne, Kessler, Goldstein & Fox P.L.L.C. | 代理人 | Sterne, Kessler, Goldstein & Fox P.L.L.C. |
| 主权项 | 1. A compound having the formulawherein R is (CH2CH2O)2H, (CH2)3C(O)NH2, (CH2)4C(NH2)COOH, (CH2)3COOH, (CH2)3NHC(O)NH2, or (CH2CH2O)3H; q ranges from 1 to 4; and Ab is selected from trastuzumab or an epitope-binding functional fragment of trastuzumab. | ||
| 地址 | Nijmegen NL | ||