US2016318888A1PendingUtilityA1

Crystalline form of cabazitaxel and process for preparing the same

Assignee: AVENTIS PHARMA SAPriority: Dec 13, 2011Filed: Apr 7, 2016Published: Nov 3, 2016
Est. expiryDec 13, 2031(~5.4 yrs left)· nominal 20-yr term from priority
A61P 35/00A61P 15/00C07D 305/14A61P 13/08
37
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Claims

Abstract

The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β, 10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.

Claims

exact text as granted — not AI-modified
1 . A crystalline ethyl acetate solvate form of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β, 10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate. 
     
     
         2 . The [[C]]crystalline form of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β, 10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate according to  claim 1 , characterized by X-Ray Powder Diffraction diagram exhibiting characteristic lines located at 8.7, 10.1, 13.8, 14.1 and 14.8±0.2 degrees 2-theta. 
     
     
         3 . The crystalline form of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β, 10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate according to  claim 1 , characterized by X-Ray Powder Diffraction diagram exhibiting characteristic lines located at 7.5, 7.9, 8.7, 10.1, 10.2, 12.6, 12.9, 13.8, 14.1 and 14.8±0.2 degrees 2-theta. 
     
     
         4 . (canceled) 
     
     
         5 . A pharmaceutical composition comprising a crystalline form according to  claim 1 , and also at least one pharmaceutically acceptable excipient. 
     
     
         6 . (canceled) 
     
     
         7 . A method for treating or preventing cancer in a patient, comprising administering the crystalline form according to  claim 1  to said patient. 
     
     
         8 . The method according to  claim 7 , wherein the cancer is prostate cancer. 
     
     
         9 . (canceled)

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