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Last Updated: September 18, 2020

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Claims for Patent: 9,550,780

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Summary for Patent: 9,550,780
Title:Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
Abstract: The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.
Inventor(s): Sommer; Andreas (Carlsbad, CA), Zhang; Chengzhi (San Diego, CA), Carter; John (Vista, CA), Arthur; John (Vista, CA), Bradbury; Margaret (Vista, CA), Gant; Thomas (Carlsbad, CA), Shahbaz; Manouchehr (San Diego, CA)
Assignee: Auspex Pharmaceuticals, Inc. (LaJolla, CA)
Application Number:15/071,797
Patent Claims: 1. A compound that is crystalline d.sub.6-tetrabenazine Form I having deuterium enrichment of no less than about 1%, and having an X-ray diffractogram comprising peaks, in terms of 2.theta..+-.0.2, at 6.5, 12.2, 14.4, 22.4 and 23.4; or a pharmaceutically acceptable salt or hydrate thereof.

2. The compound of claim 1, having an X-ray diffractogram comprising peaks, in terms of 2.theta..+-.0.2, at 6.5, 10.8, 12.2, 13.0, 14.4, 17.1, 18.0, 21.4, 22.4 and 23.4.

3. The compound of claim 1, having an X-ray diffractogram in accordance with FIG. 9.

4. The compound of claim 1, having a differential calorimetry trace comprising an endotherm between about 115 and about 135.degree. C.

5. The compound of claim 1, having a differential calorimetry trace in accordance with FIG. 8.

6. The compound of claim 1, having a thermogravimetric analysis profile showing about 1.5% weight loss below about 150.degree. C.

7. The compound of claim 1, having a thermogravimetric analysis profile in accordance with FIG. 7.

8. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and crystalline d.sub.6-tetrabenazine Form I having deuterium enrichment of no less than about 90%, and having an X-ray diffractogram comprising peaks, in terms of 2.theta..+-.0.2, at 6.5, 12.2, 14.4, 22.4 and 23.4, or a pharmaceutically acceptable salt or hydrate thereof.

9. The pharmaceutical composition as recited in claim 8, wherein crystalline d.sub.6-tetrabenazine Form I has deuterium enrichment of no less than 98%.

10. The pharmaceutical composition as recited in claim 8, wherein the crystalline d.sub.6-tetrabenazine Form I has an X-ray diffractogram comprising peaks, in terms of 2.theta..+-.0.2, at 6.5, 10.8, 12.2, 13.0, 14.4, 17.1, 18.0, 21.4, 22.4 and 23.4.

11. The pharmaceutical composition as recited in claim 8, wherein the crystalline d.sub.6-tetrabenazine Form I has an X-ray diffractogram in accordance with FIG. 9.

12. The pharmaceutical composition as recited in claim 8, wherein the crystalline d.sub.6-tetrabenazine Form I has a differential calorimetry trace comprising an endotherm between about 115 and about 135.degree. C.

13. The pharmaceutical composition as recited in claim 8, wherein the crystalline d.sub.6-tetrabenazine Form I has a differential calorimetry trace in accordance with FIG. 8.

14. The pharmaceutical composition as recited in claim 8, wherein the crystalline d.sub.6-tetrabenazine Form I has a thermogravimetric analysis profile showing about 1.5% weight loss below about 150.degree. C.

15. The pharmaceutical composition as recited in claim 8, wherein the crystalline d.sub.6-tetrabenazine Form I has a thermogravimetric analysis profile in accordance with FIG. 7.

16. The pharmaceutical composition as recited in claim 8, wherein the pharmaceutically acceptable carrier comprises polyoxide.

17. The pharmaceutical composition of claim 8, wherein the pharmaceutically acceptable carrier consists of polyoxide.

18. A method of treating a VMAT2-mediated disorder comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1.

19. The method as recited in claim 18, wherein the VMAT2-mediated disorder is a hyperkinetic movement disorder.

20. The method as recited in claim 19, wherein the hyperkinetic movement disorder is a chronic hyperkinetic movement disorder.

21. The method as recited in claim 20, wherein the chronic hyperkinetic movement disorder is selected from the group consisting of Huntington's chorea, tardive dyskinesia, Tourette's syndrome, and a tic.

22. The method as recited in claim 18, wherein the crystalline d.sub.6-tetrabenazine Form I, pharmaceutically acceptable salt, or hydrate thereof has deuterium enrichment of no less than about 90%.

23. The method as recited in claim 18, wherein the crystalline d.sub.6-tetrabenazine Form I, pharmaceutically acceptable salt, or hydrate thereof has deuterium enrichment of no less than about 98%.

24. A method of treating a VMAT2-mediated disorder comprising: administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition of claim 8.

25. The method as recited in claim 24, wherein the VMAT2-mediated disorder is a hyperkinetic movement disorder.

26. The method as recited in claim 25, wherein the hyperkinetic movement disorder is a chronic hyperkinetic movement disorder.

27. The method as recited in claim 26, wherein the chronic hyperkinetic movement disorder is selected from the group consisting of Huntington's chorea, tardive dyskinesia, Tourette's syndrome, and a tic.

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