Abstract: The instant disclosure provides crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, salts and solvates thereof. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form(s), as well of methods of using the crystalline form(s) in the treatment of HIV and/or AIDS, and methods for obtaining such crystalline form(s).

Abstract: Mono-lysine salts of triazole compounds having a secondary or tertiary hydroxy group are provided. More particularly, the new water-soluble triazole antifungal mono-lysine salt compounds, or solvates thereof, are provided having the general formula I: wherein A in formula I represents the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group. R and R1 in formula I can each be a hydrogen atom or an alkyl group having one to six carbon atoms. The novel water-soluble azole compounds are useful for the treatment of fungal infections and can be administered orally, topically and parenterally.

Abstract: The instant disclosure provides crystalline forms of 1-benzoyl-4-[2-[4,7-dimethoxy-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, salts and solvates thereof. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form(s), as well of methods of using the crystalline form(s) in the treatment of HIV and/or AIDS, and methods for obtaining such crystalline form(s).

Abstract: Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.

Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.

Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group.

Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.

Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.

Abstract: An improved process for preparing the R- and S-isomers of 2-hydroxymethyl-2-octadecyloxymethyl-tetrahydrofuran, a critical step of which involves the preparation of the R- and S-isomers of 2-[3-(1-methoxy-1-methylethoxy)]propyl-oxiranemethanol employing metal-catalyzed Sharpless epoxidation. In addition, the invention relates to the use of the R- and S-isomers of 2-hydroxymethyl-2-octadecyloxymethyl-tetrahydrofuran in preparing stereoisomers of pharmacologically active compounds, and to the R- and S-isomers of 2-[3-(1-methoxy-1-methylethoxy)]-propyl-oxiranemethanol as novel compounds.