发明授权
US07589099B2 7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists
失效
在20位缀合有整联蛋白拮抗剂的7-叔丁氧基亚氨基甲基喜树碱
- 专利标题： 7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists
- 专利标题（中）： 在20位缀合有整联蛋白拮抗剂的7-叔丁氧基亚氨基甲基喜树碱
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申请号： US11596016申请日： 2005-04-28
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公开(公告)号： US07589099B2公开(公告)日： 2009-09-15
- 发明人: Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Ming Hong , Sabrina Dallavalle , Lucio Merlini , Maria Ornella Tinti , Franco Zunino
- 申请人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Ming Hong , Sabrina Dallavalle , Lucio Merlini , Maria Ornella Tinti , Franco Zunino
- 申请人地址： IT Rome
- 专利权人： Sigma-Tau Industrie Farmaceutiche Reunite S.p.A.
- 当前专利权人： Sigma-Tau Industrie Farmaceutiche Reunite S.p.A.
- 当前专利权人地址： IT Rome
- 代理机构： Lucas & Mercanti, LLP
- 优先权： ITRM2004A0242 20040513
- 国际申请： PCT/IT2005/000245 WO 20050428
- 国际公布： WO2005/110486 WO 20051124
- 主分类号： A61K31/4745
- IPC分类号： A61K31/4745 ; C07D491/22
摘要：
Compounds of Formula (I) are described: in which the R1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
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