发明申请
US20100210597A1 C21-Deoxy Ansamycin Derivatives as Antitumor Agents
审中-公开
C21-Deoxy Ansamycin衍生物作为抗肿瘤剂
- 专利标题: C21-Deoxy Ansamycin Derivatives as Antitumor Agents
- 专利标题(中): C21-Deoxy Ansamycin衍生物作为抗肿瘤剂
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申请号: US12526605申请日: 2008-03-03
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公开(公告)号: US20100210597A1公开(公告)日: 2010-08-19
- 发明人: Steven Moss , Christine Martin , Ming Zhang
- 申请人: Steven Moss , Christine Martin , Ming Zhang
- 优先权: GB0703973.8 20070301; GB0704088.4 20070302
- 国际申请: PCT/GB08/50150 WO 20080303
- 主分类号: A61K31/675
- IPC分类号: A61K31/675 ; C07D225/06 ; A61K31/33 ; A61P35/00 ; A61P31/00 ; A61P25/00 ; A61P37/06 ; A61P9/00
摘要:
According to the invention there are provided derivatives of a C21-deoxy ansamycin or salt thereof which contain a 1-hydroxyphenyl moiety bearing at position 3 an aminocarboxy substituent, in which position 5 and the aminocarboxy substituent at position 3 are connected by an aliphatic chain of varying length characterised in that the 1-hydroxy position of the phenyl ring is derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group (which may optionally be substituted by alkyl groups) has a chain length of 2 or 3 carbon atoms, a phosphoric acid, or a phosphoric acid ester (such as an alkyl ester) group, or a salt thereof, and which derivatising group increases the water solubility and/or the bioavailability of the parent molecule. Such compounds are useful in therapy eg in the treatment of cancer and B-cell malignancies.
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