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Last Updated: December 12, 2025

Claims for Patent: 8,518,987

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Summary for Patent: 8,518,987

Title:	Pseudopolymorphic forms of a HIV protease inhibitor
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.
Inventor(s):	Hans Wim Pieter Vermeersch, Daniel Joseph Christiaan Thone, Luc Donne Marie-Louise Janssens, Piet Tom Bert Paul Wigerinck
Assignee:	Janssen Sciences Ireland ULC
Application Number:	US12/536,807
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,518,987
Patent Claims:	1. A hydrate 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 water is about 1:0.5 to about 1:3. 2. A hydrate having the formula: 3. A composition comprising a hydrate 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 water is about 1:0.5 to about 1:3, and an inert carrier. 4. The composition of claim 3 wherein the inert carrier is a pharmaceutically acceptable carrier. 5. The composition of claim 4 wherein the pharmaceutically acceptable carrier is a solid inert carrier. 6. A composition comprising a hydrate having the formula: and an inert carrier. 7. The composition of claim 6 wherein the inert carrier is a pharmaceutically acceptable carrier. 8. The composition of claim 7 wherein the pharmaceutically acceptable carrier is a solid inert carrier. 9. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:1 to about 1:2. 10. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:0.5. 11. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:1. 12. The hydrate of claim 1, wherein the ratio of the compound to water is about 1:2. 13. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:3. 14. The composition of claim 3 wherein the ratio of the compound to water is about 1:1 to about 1:2. 15. The composition of claim 3 wherein the ratio of the compound to water is about 1:0.5. 16. The composition of claim 3 wherein the ratio of the compound to water is about 1:1. 17. The composition of claim 3 wherein the ratio of the compound to water is about 1:2. 18. The composition of claim 3 wherein the ratio of the compound to water is about 1:3. 19. The composition of claim 3 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. 1. A hydrate 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 water is about 1:0.5 to about 1:3. 2. A hydrate having the formula: ##STR00002## 3. A composition comprising a hydrate of the compound (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypr- opylcarbamate, in which the ratio of compound to water is about 1:0.5 to about 1:3, and an inert carrier. 4. The composition of claim 3 wherein the inert carrier is a pharmaceutically acceptable carrier. 5. The composition of claim 4 wherein the pharmaceutically acceptable carrier is a solid inert carrier. 6. A composition comprising a hydrate having the formula: ##STR00003## and an inert carrier. 7. The composition of claim 6 wherein the inert carrier is a pharmaceutically acceptable carrier. 8. The composition of claim 7 wherein the pharmaceutically acceptable carrier is a solid inert carrier. 9. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:1 to about 1:2. 10. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:0.5. 11. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:1. 12. The hydrate of claim 1, wherein the ratio of the compound to water is about 1:2. 13. The hydrate of claim 1 wherein the ratio of the compound to water is about 1:3. 14. The composition of claim 3 wherein the ratio of the compound to water is about 1:1 to about 1:2. 15. The composition of claim 3 wherein the ratio of the compound to water is about 1:0.5. 16. The composition of claim 3 wherein the ratio of the compound to water is about 1:1. 17. The composition of claim 3 wherein the ratio of the compound to water is about 1:2. 18. The composition of claim 3 wherein the ratio of the compound to water is about 1:3. 19. The composition of claim 3 further comprising amorphous (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypr- opylcarbamate.

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