IP Library Granted Patent US 11,179,386
Granted Patent B2
US 11,179,386 · App. 16/582,362 · Granted Nov 23, 2021

Analogs of deutetrabenazine, their preparation and use

Inventors: Chengzhi Zhang (San Diego, CA); James Kerr (North Wales, PA)
Assignee: AUSPEX PHARMACEUTICALS, INC.
A61K31/4745A61K31/473A61P25/14A61P25/28C07D471/04
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Quick Facts
Patent No.
US 11,179,386
App. No.
16/582,362
Granted
Nov 23, 2021
Kind
B2
Abstract

The disclosure is directed to deutetrabenazine analogs, compositions comprising same and methods of detecting same in compositions comprising deutetrabenazine.

Claims (23)

1. A pharmaceutical composition in the form of a tablet comprising an admixture of a deutetrabenazine drug substance and a pharmaceutically acceptable carrier, wherein the deutetrabenazine drug substance comprises 5 mg to 30 mg of deutetrabenazine; and

Compound 2 in an amount that is not more than 0.15 area %, relative to the concentration of the deutetrabenazine in the tablet, based on a determination by an HPLC method comprising a C18, 150×4.6 mm, 3.5 μm column and a photodiode array/ultraviolet detector at 220 nm

2. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 does not increase to more than 0.4 area-% relative to the concentration of the deutetrabenazine in the tablet, based on a determination by the HPLC method, after storage of the tablet at room temperature for twenty-four months.

3. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 is 0.3 area-% or less, relative to the concentration of the deutetrabenazine in the tablet, based on a determination by the HPLC method, after storage of the tablet at room temperature for one month.

4. The pharmaceutical composition of claim 1 , comprising 0.25 area-% or less of the Compound 2, relative to the concentration of the deutetrabenazine in the tablet, based on a determination by the HPLC method, after storage of the tablet at room temperature for one month.

5. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 is 0.2 area-% or less, relative to the concentration of the deutetrabenazine in the tablet, based on a determination by the HPLC method, after storage of the tablet at room temperature for one month.

6. The pharmaceutical composition of claim 1 , comprising 6-24 mg deutetrabenazine.

7. The pharmaceutical composition of claim 1 , prepared for once daily administration.

8. The pharmaceutical composition of claim 1 , prepared for more than once daily administration.

9. A method of treating a subject afflicted with a hyperkinetic movement disorder comprising administering to the subject the pharmaceutical composition of claim 1 .

10. The method of claim 9 , wherein the hyperkinetic movement disorder is Huntington's disease.

11. The method of claim 9 , wherein the hyperkinetic movement disorder is chorea related to Huntington's disease.

12. The method of claim 9 , wherein the hyperkinetic movement disorder is tardive dyskinesia.

13. The method of claim 9 , wherein the hyperkinetic movement disorder is a tic associated with Tourette syndrome.

14. The pharmaceutical composition of claim 1 , comprising 6 mg of deutetrabenazine.

15. The pharmaceutical composition of claim 1 , comprising 9 mg of deutetrabenazine.

16. The pharmaceutical composition of claim 1 , comprising 12 mg of deutetrabenazine.

17. The pharmaceutical composition of claim 1 , comprising 24 mg of deutetrabenazine.

18. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 does not increase to more than 0.4 area-% relative to the concentration of the deutetrabenazine in the tablet, based on a determination by the HPLC method, after storage of the tablet at room temperature for two months.

19. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 does not increase to more than 0.4 area-% relative to the concentration of the deutetrabenazine, based on a determination by the HPLC method, after storage at room temperature for three months.

20. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 does not increase to more than 0.4 area-% relative to the concentration of the deutetrabenazine, based on a determination by the HPLC method, after storage at room temperature for six months.

21. The pharmaceutical composition of claim 1 , wherein the concentration of the Compound 2 is 0.4 area-% or less, relative to the concentration of the deutetrabenazine, based on a determination by the HPLC method, after storage at room temperature for one month.

22. The pharmaceutical composition of claim 1 , comprising 18 mg of deutetrabenazine.

Assignments (2)
CHANGE OF NAME Recorded Oct 13, 2025
From: AUSPEX PHARMACEUTICALS, INC.
To: AUSPEX PHARMACEUTICALS LLC
Reel/Frame 073081/0526 →
CHANGE OF ASSIGNEE ADDRESS Recorded Feb 2, 2021
From: AUSPEX PHARMACEUTICALS, INC.
To: AUSPEX PHARMACEUTICALS, INC.
Reel/Frame 055194/0412 →
Continuity (3)
Division 15922329 · Mar 15, 2018
Provisional Application 62471484 · Mar 15, 2017
Related Publication 20200016148A1 · Jan 16, 2020