US2017362186A1PendingUtilityA1

Salts of a dihydroquinazoline derivative

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Assignee: AICURIS GMBH & CO KGPriority: Feb 29, 2012Filed: Jul 3, 2017Published: Dec 21, 2017
Est. expiryFeb 29, 2032(~5.6 yrs left)· nominal 20-yr term from priority
C07D 239/84C07C 309/29A61P 31/22A61P 31/20A61P 31/00C07C 309/30
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Claims

Abstract

The invention relates to besylate and tosylate salts of { 8 -fluoro- 2 -[ 4 -( 3 -methoxyphenyl)piperazin- 1 -yl]- 3 -[ 2 -methoxy- 5 -(trifluoromethyl)phenyl]- 3,4 -dihydroquinazolin- 4 -yl} acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses.

Claims

exact text as granted — not AI-modified
1 - 15 . (canceled) 
     
     
         16 . A zwitterionic form of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid produced by
 1 .) reacting {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid in a solvent with benzenesulfonic acid or toluenesulfonic acid to obtain a crystalline salt,   2.) isolating the salt obtained in step 1.),   3.) treating the isolated salt obtained in step 2.) with a buffer solution at a pH in the range of 5 to 7 to release a zwitterionic form of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid, and   4.) isolating the zwitterionic form of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid obtained in step 3.).

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