US2014171499A1PendingUtilityA1

Pseudopolymorphic Forms Of A HIV Protease Inhibitor

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Assignee: JANSSEN R & D IRELANDPriority: May 16, 2002Filed: Feb 19, 2014Published: Jun 19, 2014
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 31/18A61P 43/00C07D 493/04
61
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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 - 14 . (canceled) 
     
     
         15 . An ethanolate 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 in which the ratio of the compound to ethanol is about 5:1 to about 1:5. 
     
     
         16 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:0.5 to about 1:3. 
     
     
         17 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:1 to about 1:2. 
     
     
         18 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:0.5. 
     
     
         19 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:1. 
     
     
         20 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:2. 
     
     
         21 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:3. 
     
     
         22 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:4. 
     
     
         23 . The ethanolate of  claim 15 , wherein the ratio of the compound to ethanol is about 1:5. 
     
     
         24 . A composition comprising an ethanolate 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, in which the ratio of compound to ethanol is about 5:1 to about 1:5, and an inert carrier. 
     
     
         25 . The composition of  claim 24 , wherein the ratio of compound to ethanol is about 1:0.5 to about 1:3. 
     
     
         26 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:1 to about 1:2. 
     
     
         27 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:0.5. 
     
     
         28 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:1. 
     
     
         29 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:2. 
     
     
         30 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:3. 
     
     
         31 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:4. 
     
     
         32 . The composition of  claim 24 , wherein the ratio of the compound to ethanol is about 1:5. 
     
     
         33 . The composition of  claim 24 , wherein the inert carrier is a pharmaceutically acceptable carrier. 
     
     
         34 . The composition of  claim 33 , wherein the pharmaceutically acceptable carrier is a solid inert carrier. 
     
     
         35 . The composition of  claim 24 , further comprising amorphous (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate.

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