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Last Updated: May 16, 2024

Claims for Patent: 10,414,751


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Summary for Patent: 10,414,751
Title:Antifungal compounds and processes for making
Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.
Inventor(s): Hoekstra; William J. (Durham, NC), Wirth; David Dale (Oak Ridge, NC), Ehiwe; Tracy (Cambridge, GB), Bonnaud; Thierry (Cambridge, GB)
Assignee: Mycovia Pharmaceuticals, Inc. (Durham, NC)
Application Number:16/270,717
Patent Claims: 1. An anhydrous polymorph of a compound of formula 1, ##STR00003## wherein the polymorph has the crystal structure as shown in FIG. 9.

2. A process to prepare an anhydrous polymorph of compound 1: ##STR00004## comprising suspending a compound of formula 1 in a solvent and isolating any solid material.

3. The process of claim 2, wherein the compound suspended in the solvent is in one of an amorphous, solvate, or hydrate form.

4. The process of claim 2, wherein the solvent is an organic solvent.

5. The process of claim 2, wherein the solvent is a C.sub.3-C.sub.10 alcohol.

6. The process of claim 5, wherein the solvent is n-propanol, i-propanol, n-butanol, i-butanol, s-butanol, or t-butanol.

7. The process of claim 2, comprising two or more solvents.

8. The process of claim 7, wherein one solvent is a C.sub.3-C.sub.10 alcohol and one solvent is a hydrocarbon.

9. The process of claim 8, wherein the alcohol solvent is n-propanol, propanol, n-butanol, i-butanol, s-butanol, or t-butanol.

10. The process of claim 8, wherein the hydrocarbon solvent is n-pentane, n-heptane or n-hexane, cyclohexane, or methylcyclohexane.

11. The process of claim 8, wherein one solvent is i-propanol and one solvent is n-heptane.

12. The process of claim 2, wherein the isolated solid material is dried at a temperature of 30.degree. C. or higher.

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