US2015336980A1PendingUtilityA1

Pseudopolymorphic Forms Of A HIV Protease Inhibitor

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Assignee: JANSSEN SCIENCES IRELAND UCPriority: May 16, 2002Filed: Aug 4, 2015Published: Nov 26, 2015
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
A61P 31/12A61P 43/00A61P 31/18C07D 493/04
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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 - 15 . (canceled) 
     
     
         16 . An alcohol solvate of the compound (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate. 
     
     
         17 . The alcohol solvate of  claim 16 , wherein the alcohol is a C1-C4 alcohol. 
     
     
         18 . The alcohol solvate of  claim 16 , wherein the alcohol is a C1 alcohol, a C3 alcohol, or a C4 alcohol. 
     
     
         19 . The alcohol solvate of  claim 16 , wherein the alcohol is a C1 alcohol. 
     
     
         20 . The alcohol solvate of  claim 16 , wherein the alcohol is a C3 alcohol. 
     
     
         21 . The alcohol solvate of  claim 16 , wherein the alcohol is a C4 alcohol. 
     
     
         22 . A composition comprising an alcohol solvate of the compound (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and a carrier. 
     
     
         23 . The composition of  claim 22 , wherein the alcohol is a C1 alcohol, a C3 alcohol, or a C4 alcohol. 
     
     
         24 . The composition of  claim 22 , wherein the alcohol is a C1 alcohol. 
     
     
         25 . The composition of  claim 22 , wherein the alcohol is a C3 alcohol. 
     
     
         26 . The composition of  claim 22 , wherein the alcohol is a C4 alcohol. 
     
     
         27 . A method of treating a mammal having an HIV infection comprising administering to the mammal, a therapeutically effective amount of an alcohol solvate of the compound (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate. 
     
     
         28 . The method of  claim 27 , wherein the alcohol solvate is administered in an amount sufficient to reduce the viral load of the HIV, increase CD4+ cell count, or inhibit HIV protease activity. 
     
     
         29 . The method of  claim 27 , wherein the alcohol is a C1-C4 alcohol. 
     
     
         30 . The method of  claim 27 , wherein the alcohol is a C1 alcohol. 
     
     
         31 . The method of  claim 27 , wherein the alcohol is a C2 alcohol. 
     
     
         32 . The method of  claim 27 , wherein the alcohol is a C3 alcohol. 
     
     
         33 . The method of  claim 27 , wherein the alcohol is a C4 alcohol.

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