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Claims for Patent: 8,420,663

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Claims for Patent: 8,420,663

Title:Peripheral opioid receptor antagonists and uses thereof
Abstract: The present invention provides a compound of formula I: ##STR00001## wherein X.sup.-, R.sup.1, and R.sup.2 are as defined herein, and compositions thereof.
Inventor(s): Bazhina; Nataliya (Tappan, NY), Donato, III; George Joseph (Swarthmore, PA), Fabian; Steven R. (Barnegat, NJ), Lokhnauth; John (Fair Lawn, NJ), Megati; Sreenivasulu (New City, NY), Melucci; Charles K. (Highland Mills, NY), Ofslager; Christian (Newburgh, NY), Patel; Niketa (Lincoln Park, NJ), Radebaugh; Galen (Chester, NJ), Shah; Syed M. (East Hanover, NJ), Szeliga; Jan (Croton on Hudson, NY), Zhang; Huyi (Garnerville, NY), Zhu; Tianmin (Monroe, NY)
Assignee: Wyeth (Madison, NJ)
Application Number:13/570,836
Patent Claims: 1. A method of treating a gastrointestinal disorder in a subject, comprising administering to the subject a compound of formula III ##STR00031## contained within a packaged composition substantially free of tungsten, wherein A.sup.- is a suitable anion; wherein the packaged composition comprises less than about 190 ppm of a compound of formula II ##STR00032## wherein X.sup.- is a suitable anion.

2. The method of claim 1, wherein the gastrointestinal disorder is constipation.

3. The method of claim 2, wherein the constipation is opioid-induced.

4. The method of claim 1, wherein the compound of formula III is provided in a solution.

5. The method of claim 1, wherein the compound of formula III is of formula III-1 ##STR00033##

6. The method of claim 5, wherein the compound of formula III is provided in solution.

7. The method of claim 5, wherein the gastrointestinal disorder is constipation.

8. The method of claim 7, wherein the constipation is opioid-induced.

9. The method of claim 1, wherein the subject is receiving opioids chronically.

10. The method of claim 9, wherein the subject is a cancer patient.

11. The method of claim 1, wherein the packaged composition is selected from the group consisting of a syringe, a vial, a sachet and an ampoule.

12. The method of claim 1, wherein the packaged composition is a syringe.

13. The method of claim 1, wherein the compound of formula III is in the form of a tablet, a capsule, a powder, a solution, a suspension, an emulsion, a granule, and a suppository.

14. The method of claim 1, wherein the solution comprises less than about 190 ppm total of the compound of formula II and a compound of formula IV: ##STR00034## wherein R1 and R2 are each independently C1-6 aliphatic; and X is a suitable anion.

15. The method of claim 6, wherein the compound of formula III is administered by injection or infusion.

16. The method of claim 15, wherein the compound of formula III is administered by subcutaneous injection.

17. The method of claim 1, wherein the subject is receiving an opioid at a morphine equivalent dose of between about 30 and about 100 oral mg/day of methadone.

18. The method of claim 1, wherein the tungsten is present in an amount of less than 50 parts per billion.

19. The method of claim 1, wherein the tungsten is present in an amount of less than 12 parts per billion.

20. The method of claim 6, wherein the solution further comprises edetate calcium disodium and glycine hydrochloride.

21. The method of claim 6, wherein the solution comprises about 8 mg of the compound of formula III in about 0.4 mL water.

22. The method of claim 21, wherein the compound of formula III is of formula III-1 ##STR00035##

23. The method of claim 6, wherein the solution comprises about 12 mg of the compound of formula III in about 0.6 mL water.

24. The method of claim 23, wherein the compound of formula III is of formula III-1 ##STR00036##

25. The method of claim 1, wherein the compound of formula III is stable under ambient storage conditions.

26. The method of claim 25, wherein the compound of formula III is stable for at least 24 months.

27. A method of treating opioid induced constipation in a subject, comprising administering to the subject a compound of formula III-1 ##STR00037## contained within a packaged composition substantially free of tungsten; wherein the packaged composition comprises less than about 190 ppm of a compound of formula II: ##STR00038## wherein X.sup.- is a suitable anion.

28. A method of treating constipation in a subject, comprising administering to the subject a unit dosage of a compound of formula III-1 ##STR00039## wherein the compound of formula III-1 is administered with a syringe that is substantially free of tungsten; wherein the syringe comprises less than about 190 ppm of a compound of formula II ##STR00040## wherein X.sup.- is a suitable anion.

29. A method of treating constipation in a subject, comprising administering to the subject a unit dosage of a compound of formula III ##STR00041## wherein the compound of formula III is administered with a syringe that is substantially free of tungsten, wherein A.sup.- is a suitable anion; and wherein the syringe comprises less than about 190 ppm of a compound of formula II: ##STR00042## wherein X.sup.- is a suitable anion.
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