Pseudopolymorphic Forms of a HIV Protease Inhibitor
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 pseudopolymorph of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3 -[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate, wherein the pseudopolymorph is a C 1 -C 4 alcohol solvate.
2 . The pseudopolymorph according to claim 1 , wherein the C 1 -C 4 alcohol is a straight chained saturated alcohol.
3 . The pseudopolymorph according to claim 1 , in which the ratio of the compound to the alcohol ranges between (5:1) and (1:5).
4 . The pseudopolymorph according to claim 1 , in which the ratio of the compound to the alcohol ranges between (1:0.2) and (1:3).
5 . The pseudopolymorph according to claim 1 , in which the ratio of the compound to the alcohol ranges between (1:1) and (1:2).
6 . The pseudopolymorph according to claim 1 , in which the ratio of the compound to the alcohol is about 1:1.
7 . The pseudopolymorph according to claim 1 , additionally comprising water molecules.
8 . A pharmaceutical formulation comprising a therapeutically effective amount of a pseudopolymorph of claim 1 and a pharamceutically acceptable carrier or diluent.
9 . A method of treating a retroviral infection in a human comprising administering to the human a pseudopolymorph according to claim 1 .