US2016185766A1PendingUtilityA1

Novel Salts of Raltegravir

Assignee: LUPIN LTDPriority: Apr 6, 2011Filed: Sep 16, 2015Published: Jun 30, 2016
Est. expiryApr 6, 2031(~4.7 yrs left)· nominal 20-yr term from priority
C07D 413/12A61K 31/513C07C 211/04A61P 31/12
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Claims

Abstract

Provided herein are novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation.

Claims

exact text as granted — not AI-modified
1 . An Erbumine salt of raltegravir. 
     
     
         2 . A crystalline erbumine salt of raltegravir, represented by formula II, 
       
         
           
           
               
               
           
         
       
       which is characterized by XRPD (X-ray powder diffractogram) comprising of peaks expressed as 2θ at 4.2, 8.4, 9.1, 11.7, 12.6, 13.8, 15.2, 16.9, 18.0, 18.4, 18.8, 19.0, 20.8, 21.2, 22.0, 22.4 and 22.7±0.2 degrees. 
     
     
         3 . A process for preparation of crystalline erbumine salt of raltegravir of  claim 2 , which comprises treating raltegravir with tert-butyl amine in an alcohol. 
     
     
         4 . The process according to  claim 3 , wherein the alcohol is selected from methanol, ethanol, n-propanol and isopropanol. 
     
     
         5 . The process according to  claim 4 , wherein the alcohol is methanol. 
     
     
         6 . The process according to  claim 3 , wherein the molar ratio of tertiary butyl amine with respect to raltegravir is in the range of 1 to 3.

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