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公开(公告)号:US20140315954A1
公开(公告)日:2014-10-23
申请号:US14213504
申请日:2014-03-14
IPC分类号: C07C317/50 , C07C317/28 , C07D213/56 , C07C317/32 , C07D211/60 , C07D213/71
CPC分类号: C07C311/51 , A61K31/445 , A61K38/05 , A61K38/06 , A61K39/3955 , A61K47/48261 , A61K47/48415 , A61K47/6415 , C07C317/28 , C07C317/32 , C07C317/50 , C07C323/12 , C07C323/67 , C07C327/06 , C07C381/08 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/452 , C07D211/34 , C07D211/60 , C07D213/56 , C07D213/71 , C07D333/34 , C07K5/0205 , C07K5/06078 , Y02A50/385 , Y02A50/414 , Y02A50/423
摘要: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
摘要翻译: 公开了具有细胞毒性和/或抗有丝分裂活性的化合物。 该化合物具有以下结构(I):包括其立体异构体,药学上可接受的盐和前药,其中R 1,R 2,R 3,R 4和R 5如本文所定义。 还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。 还公开了具有以下结构的组合物:(T) - (L) - (D),其中(T)是靶向部分,(L)是任选的连接体,(D)是具有结构(I)的化合物。