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Last Updated: April 19, 2024

Claims for Patent: 9,956,205


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Summary for Patent: 9,956,205
Title:Polymorphic forms of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)ace- tic acid and uses thereof
Abstract: Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
Inventor(s): Treiber; Laszlo R. (San Diego, CA), Zamansky; Irina (Oceanside, CA), Girardet; Jean-Luc (San Diego, CA)
Assignee: Ardea Biosciences, Inc. (San Diego, CA)
Application Number:15/150,053
Patent Claims: 1. A method for treating hyperuricemia associated with gout, comprising administering an effective amount of a crystalline polymorph of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)ace- tic acid: ##STR00009## characterized by peaks at 10.46, 18.76, and 19.83 .degree.2.theta..+-.0.1.degree.2.theta..

2. The method of claim 1, wherein the crystalline polymorph is further characterized by at least one further peak at 18.21 or 23.08 .degree.2.theta..+-.0.1.degree.2.theta..

3. The method of claim 1, wherein the crystalline polymorph exhibits an x-ray powder diffraction pattern substantially the same as the x-ray powder diffraction pattern shown in FIG. 5.

4. The method of claim 1, wherein the crystalline polymorph is prepared by a method comprising the step of crystallizing 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)ace- tic acid from a mixture of water and ethyl acetate.

5. The method of claim 1, further comprising administering allopurinol.

6. The method of claim 1, further comprising administering febuxostat.

7. A method of treating hyperuricemia associated with gout, comprising administering an effective amount of a crystalline polymorph of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)ace- tic acid: ##STR00010## characterized by peaks at 10.32, 18.84, and 20.75 .degree.2.theta..+-.0.1.degree.2.theta..

8. The method of claim 7, wherein the crystalline polymorph is further characterized by at least two further peaks at 6.80, 21.54, 24.97, 25.53, 27.28 or 27.60 .degree.2.theta..+-.0.1.degree.2.theta..

9. The method of claim 7, wherein the crystalline polymorph exhibits an x-ray powder diffraction pattern substantially the same as the x-ray powder diffraction pattern shown in FIG. 1.

10. The method of claim 7, wherein the crystalline polymorphic form of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)ace- tic acid is prepared by a method comprising the step of crystallizing 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)ace- tic acid from a mixture of water and acetic acid.

11. The method of claim 7, further comprising administering allopurinol.

12. The method of claim 7, further comprising administering febuxostat.

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