发明授权
- 专利标题: ELONGATED AND MULTIPLE SPACERS IN ACTIVATIBLE PRODRUGS
- 专利标题(中): 细长且多ABSTANDSHALTER含有活性药物前体
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申请号: EP02727513.0申请日: 2002-03-25
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公开(公告)号: EP1370298B1公开(公告)日: 2008-10-08
- 发明人: DE GROOT, Franciscus, Marinus, Hendrikus , BEUSKER, Patrick, Henry , SCHEEREN, Johannes, Wilhelm , DE VOS, Dick , VAN BERKOM, Leonardus, Wilhelmus, Adriaan , BUSSCHER, Guuske, Frederike , SEELEN, Antoinette, Eugenie , KOEKKOEK, Ralph , ALBRECHT, Carsten
- 申请人: Syntarga B.V.
- 申请人地址: Toernooiveld 1 6525 ED Nijmegen NL
- 专利权人: Syntarga B.V.
- 当前专利权人: Syntarga B.V.
- 当前专利权人地址: Toernooiveld 1 6525 ED Nijmegen NL
- 代理机构: van Westenbrugge, Andries
- 优先权: EP01201095 20010323
- 国际公布: WO2002083180 20021024
- 主分类号: A61K47/48
- IPC分类号: A61K47/48
摘要:
This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V-(W)k-(X)1-A-Z, wherein: V is a specifier; (W)k-(X)1-A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, 1 and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: - when A is (Y)m: k+1+m ≥ 1, and if k+1+m = 1; - when A is U: k+1 ≥ 1.
公开/授权文献
- EP1370298A1 ELONGATED AND MULTIPLE SPACERS IN ACTIVATIBLE PRODRUGS 公开/授权日:2003-12-17
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