发明名称 PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL
摘要 The present invention provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I),;;and process for preparation thereof.;The present application also provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I) having an XRPD pattern as per FIG. 1, and IR spectrum as per FIG. 3 and is useful as an active pharmaceutical in a pharmaceutical composition comprising thereof and has anti-cancer activity.
申请公布号 US2014336246(A1) 申请公布日期 2014.11.13
申请号 US201214349332 申请日期 2012.12.26
申请人 SHILPA MEDICARE LIMITED 发明人 Shrawat Vimal Kumar;Purohit Prashant;Dr Rafiuddin;Singh Vinod Kumar;Chaturvedi Akshaykant
分类号 C07D305/14 主分类号 C07D305/14
代理机构 代理人
主权项 1. A non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[(tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I),having up to 2% w/w or less of volatiles measured up to 160° C.
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