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Last Updated: April 25, 2024

Claims for Patent: 6,858,203


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Summary for Patent: 6,858,203
Title: Method of making phosphate-binding polymers for oral administration
Abstract:Phosphate-binding polymers are provided for removing phosphate from the gastrointestinal tract. The polymers are orally administered, and are useful for the treatment of hyperphosphatemia.
Inventor(s): Holmes-Farley; Stephen Randall (Arlington, MA), Mandeville, III; W. Harry (Lynnfield, MA), Whitesides; George M. (Newton, MA)
Assignee: Genzyme Corporation (Cambridge, MA)
Application Number:10/322,904
Patent Claims: 1. A method for removing phosphate from a patient comprising orally administering to said patient a therapeutically effective amount of a composition comprising at least one polymer characterized by a repeat unit having the formula: ##STR28##

or a copolymer thereof, wherein each n is an integer, each R, independently, is H or a lower alkyl, alkylamino, or aryl group, and each X.sup.- is a carbonate or bicarbonate anion.

2. The method of claim 1 wherein said polymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.

3. The method of claim 2 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.

4. The method of claim 2 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

5. The method of claim 1 wherein the polymer is a copolymer comprising a second repeat unit having the formula: ##STR29##

wherein each n, independently, is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.

6. The method of claim 5 wherein said copolymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.

7. The method of claim 6 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.

8. The method of claim 6 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

9. A method for removing phosphate from a patient comprising orally administering to said patient a therapeutically effective amount of a composition comprising a copolymer characterized by a repeat unit having the formula: ##STR30##

and a second repeat unit having the formula: ##STR31##

wherein said copolymer is crosslinked with epichlorohydrin, wherein epichlorohydrin is present in said composition from about 2% to about 20% by weight and wherein each n is an integer, each R is H, and each X.sup.- 0 is a carbonate or bicarbonate anion.

10. A pharmaceutical composition comprising a carrier and a therapeutically effective amount of at least one polymer characterized by a repeat unit having the formula: ##STR32##

or a copolymer thereof, wherein each n is an integer, each R, independently, is H or a lower alkyl, alkylamino, or aryl group, and each X.sup.- is a carbonate or bicarbonate anion.

11. The pharmaceutical composition of claim 10 wherein said polymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.

12. The pharmaceutical composition of claim 11 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.

13. The pharmaceutical composition of claim 11 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

14. The pharmaceutical composition of claim 10 wherein the polymer is a copolymer comprising a second repeat unit having the formula: ##STR33##

wherein each n, independently, is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.

15. The pharmaceutical composition of claim 14 wherein said copolymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.

16. The pharmaceutical composition of claim 15 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.

17. The pharmaceutical composition of claim 15 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

18. A pharmaceutical composition comprising a carrier and a therapeutically effective amount of a copolymer characterized by a repeat unit having the formula: ##STR34##

and a second repeat unit having the formula: ##STR35##

wherein said copolymer is crosslinked with epichlorohydrin, wherein epichlorohydrin is present in said composition from about 2% to about 20% by weight and wherein each n is an integer, each R is H, and each X.sup.- is a carbonate or bicarbonate anion.

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