US2021179631A1PendingUtilityA1

Pseudopolymorphic Forms of a HIV Protease Inhibitor

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Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COPriority: May 16, 2002Filed: Oct 30, 2020Published: Jun 17, 2021
Est. expiryMay 16, 2022(expired)· nominal 20-yr term from priority
Inventors:Hans Wim Pieter VermeerschDaniel Joseph Christiaan ThoneLuc Donne Marie-Louise JanssensPiet Tom Bert Paul Wigerinck
C07D 493/04A61P 31/12A61P 31/18A61P 43/00
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Claims

Abstract

New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.

Claims

exact text as granted — not AI-modified
1 . A pseudopolymorph of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3 -[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate, wherein the pseudopolymorph is a C 1 -C 4  alcohol solvate. 
     
     
         2 . The pseudopolymorph according to  claim 1 , wherein the C 1 -C 4  alcohol is a straight chained saturated alcohol. 
     
     
         3 . The pseudopolymorph according to  claim 1 , in which the ratio of the compound to the alcohol ranges between (5:1) and (1:5). 
     
     
         4 . The pseudopolymorph according to  claim 1 , in which the ratio of the compound to the alcohol ranges between (1:0.2) and (1:3). 
     
     
         5 . The pseudopolymorph according to  claim 1 , in which the ratio of the compound to the alcohol ranges between (1:1) and (1:2). 
     
     
         6 . The pseudopolymorph according to  claim 1 , in which the ratio of the compound to the alcohol is about 1:1. 
     
     
         7 . The pseudopolymorph according to  claim 1 , additionally comprising water molecules. 
     
     
         8 . A pharmaceutical formulation comprising a therapeutically effective amount of a pseudopolymorph of  claim 1  and a pharamceutically acceptable carrier or diluent. 
     
     
         9 . A method of treating a retroviral infection in a human comprising administering to the human a pseudopolymorph according to  claim 1 .

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