Pseudopolymorphic forms of a HIV protease inhibitor
View Patent ↗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.
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.