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Claims for Patent: 8,518,987

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Claims 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-hydroxypr- opylcarbamate and processes for producing them are disclosed.
Inventor(s): Vermeersch; Hans Wim Pieter (Ghent, BE), Thone; Daniel Joseph Christiaan (Beerse, BE), Janssens; Luc Donne Marie-Louise (Malle, BE), Wigerinck; Piet Tom Bert Paul (Terhagen, BE)
Assignee: Janssen R&D Ireland (Little Island, Co. Cork, IE)
Application Number:12/536,807
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: ##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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