Claims for Patent: 5,667,775

Summary for Patent: 5,667,775

Title:	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:	GelTex Pharmaceuticals, Inc. (Waltham, MA)
Application Number:	08/471,747
Patent Claims:	1. A method for removing phosphate from a patient by ion exchange 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 n is an integer, and each R, independently, is H, an unsubstituted alkyl, alkylamino, or aryl group, or a substituted alkyl, alkylamino or aryl group, wherein the substituents are selected from the group consisting of quaternary ammonium, amino, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea and carboxylic acid ester. 2. The method of claim 1 wherein said polymer is crosslinked with a crosslinking agent, wherein said 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 is selected from the group consisting of 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 and pyromellitic dianhydride. 4. The method of claim 2 wherein said polymer is crosslinked with a crosslinking agent, 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 R is a substituted or unsubstituted alkyl, alkylamino, or aryl group. 6. The method of claim 5 wherein said polymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 1% to about 75% by weight. 7. The method of claim 6 wherein said crosslinking agent is epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence 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 by ion exchange 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 ##STR30## or a copolymer thereof, wherein n is an integer, and each R.sub.1 and R.sub.2, independently, is H, an unsubstituted alkyl, alkylamino, or aryl group, or a substituted alkyl, alkylamino or aryl group, wherein the substituents are selected from the group consisting of quaternary ammonium, amino, hydroxy, alkoxy, carboxamide, sulfanamide, halogen, alkyl, aryl, hydrazine, guanidine, urea and carboxylic acid ester; and each X is an exchangeable negatively charged counterion. 10. The method of claim 9 wherein at least one of said R groups is a hydrogen group. 11. The method of claim 9 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight. 12. The method of claim 11 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin, 1,4-butanedioldiglycidyl ether, 1,2-ethanedioldiglycidylether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride and pyromellitic dianhydride. 13. The method of claim 11 wherein said polymer is crosslinked with a crosslinking agent, wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight. 14. A method for removing phosphate from a patient by ion exchange 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 ##STR31## or a copolymer thereof, wherein n is an integer, each R.sub.1 and R.sub.2, independently, is H, a substituted or unsubstituted alkyl group containing 1 to 20 carbon atoms, wherein the substituents are selected from the group consisting of quaternary ammonium, amino, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, urea and carboxylic acid ester. 15. The method of claim 14 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight. 16. The method of claim 15 wherein said crosslinking agent is selected from the group consisting of epichlorohydrine 1,4-butanedioldiglycidyl ether, 1,2-ethanedioldiglycidylether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride and pyromellitic dianhydride. 17. The method of claim 15 wherein said polymer is crosslinked with a crosslinking agent, wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight. 18. A method for removing phosphate from a patient by ion exchange 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 ##STR32## or a copolymer thereof, wherein n is an integer, each R.sub.1, R.sub.2 and R.sub.3, independently, is H, an unsubstituted C.sub.1 -C.sub.20 -alkyl, alkylamino, or aryl group, or a substituted C.sub.1 -C.sub.20 -alkyl, alkylamino or aryl group, wherein the substituents are selected from the group consisting of quaternary ammonium, amino, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea and carboxylic acid ester, and each X.sup.- is an exchangeable negatively charged counterion. 19. The method of claim 18 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight. 20. The method of claim 19 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin, 1,4-butanedioldiglycidyl ether, 1,2-ethanedioldiglycidylether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride and pyromellitic dianhydride. 21. The method of claim 19 wherein said polymer is crosslinked with a crosslinking agent, wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight. 22. A method for removing phosphate from a patient by ion exchange, comprising orally administering to said patient a therapeutically effective amount of a composition comprising at least one hydrophilic cross-linked aliphatic amine polymer.