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Generated: September 21, 2017

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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 (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)
Filing Date:Jul 11, 2012
Application Number:13/546,500
Claims:1. A compound of formula I: ##STR00031## wherein: R.sup.1 and R.sup.2 are each independently C.sub.1-6 aliphatic; and X.sup.- is a suitable anion.

2. The compound according to claim 1, wherein X.sup.- is the anion of a suitable Bronsted acid.

3. The compound according to claim 2, wherein the Bronsted acid is a hydrogen halide, a carboxylic acid, a sulfonic acid, a sulfuric acid, or a phosphoric acid.

4. The compound according to claim 2, wherein X.sup.- is chloride, bromide, iodide, fluoride, sulfate, bisulfate, tartrate, nitrate, citrate, bitartrate, carbonate, phosphate, malate, maleate, fumarate, sulfonate, methylsulfonate, formate, carboxylate, methylsulfate, trifluoroacetate, or succinate.

5. The compound according to claim 4, wherein X.sup.- is bromide.

6. The compound according to claim 1, wherein R.sup.1 is C.sub.1-4 aliphatic and R.sup.2 is lower alkyl.

7. The compound according to claim 6, wherein R.sup.1 is a (cycloalkyl)alkyl group or alkenyl group.

8. The compound according to claim 7, wherein R.sup.1 is cyclopropyl methyl or allyl and R.sup.2 is methyl.

9. The compound according to claim 1, wherein said compound is of formula II or II': ##STR00032## wherein, each X.sup.- is a suitable anion.

10. The compound according to claim 1, wherein said compound is compound II-1 or II-2: ##STR00033##

11. A crystalline form of compound II-1 according to claim 10 ##STR00034##

12. A method comprising the steps of: (a) providing a sample of (R)--N-methylnaltrexone bromide; (b) performing an analysis of the sample of (R)--N-methylnaltrexone bromide; and (c) determining the amount of compound II-1 according to claim 10 in the sample of (R)--N-methylnaltrexone bromide.

13. The method according to claim 12, wherein step (c) further comprises the step of determining the amount of compound IV-1 ##STR00035## in the sample of (R)--N-methylnaltrexone bromide.

14. The method according to claim 13, wherein step (c) comprises determining that the amount of compound II-1 and compound IV-1 in the sample of (R)--N-methylnaltrexone bromide is less than about 60 ppm, about 10 ppm, about 5 ppm, about 3.3 ppm, about 2.5 ppm, or about 1 ppm total.

15. The method according to claim 13, wherein step (c) comprises determining that the amount of compound II-1 and compound IV-1 in the sample of (R)--N-methylnaltrexone bromide is less than about 25, about 100, about 125, about 150, about 185, about 187, or about 190 ppm total.

16. A method comprising the steps of: (a) providing a sample of (R)--N-methylnaltrexone bromide; (b) providing a sample of the compound II-1 according to claim 10 ##STR00036## (c) performing HPLC analysis of the sample of (R)--N-methylnaltrexone bromide and the sample of compound II-1; and (d) determining the amount of compound II-1 in the sample of (R)--N-methylnaltrexone bromide.

17. A method comprising the steps of: (a) providing an HPLC chromatogram of a sample of (R)--N-methylnaltrexone bromide; (b) providing an HPLC chromatogram of a sample of compound II-1: ##STR00037## (c) comparing the HPLC chromatograms and determining the amount of compound II-1 in the sample of (R)--N-methylnaltrexone bromide.

18. A kit comprising the compound of formula I according to claim 1 ##STR00038## wherein: R.sup.1 and R.sup.2 are each independently C.sub.1-6 aliphatic; and X.sup.- is a suitable anion, and a container containing the compound of formula I.
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Queensland Health
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US Department of Justice
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