Invention Grant
US08455510B2 Rapamycin carbonic ester analogues, pharmaceutical compositions, preparations and uses thereof
失效
雷帕霉素碳酸酯类似物，药物组合物，制剂及其用途
- Patent Title: Rapamycin carbonic ester analogues, pharmaceutical compositions, preparations and uses thereof
- Patent Title (中): 雷帕霉素碳酸酯类似物，药物组合物，制剂及其用途
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Application No.: US13119700Application Date: 2009-09-17
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Publication No.: US08455510B2Publication Date: 2013-06-04
- Inventor: Fajun Nan , Jian Ding , Jianping Zuo , Linqian Yu , Linghua Meng , Yangming Zhang , Na Yang , Min Gu
- Applicant: Fajun Nan , Jian Ding , Jianping Zuo , Linqian Yu , Linghua Meng , Yangming Zhang , Na Yang , Min Gu
- Applicant Address: CN Shanghai
- Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Current Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Current Assignee Address: CN Shanghai
- Agency: Baker & Hostetler LLP
- Priority: CN200810200073 20080918
- International Application: PCT/CN2009/001042 WO 20090917
- International Announcement: WO2010/031251 WO 20100325
- Main IPC: C07D498/18
- IPC: C07D498/18 ; A61K31/436 ; A61P35/00
Abstract:
Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
Public/Granted literature
- US20110166172A1 Rapamycin Carbonic Ester Analogues, Pharmaceutical Compositions, Preparations and Uses Thereof Public/Granted day:2011-07-07
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