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Details for Patent: 5,929,184

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Details for Patent: 5,929,184

Title: Hydrophilic nonamine-containing and amine-containing copolymers and their use as bile acid sequestrants
Abstract:The present invention relates to polymer compositions and methods of using said compositions for sequestering bile acids in a patient. The polymer compositions of this invention comprise a copolymer characterized by one or more hydrophilic nonamine-containing monomers or repeat units and one or more amine-containing monomers or repeat units. The amine-containing monomers or repeat units of the polymer compositions have one or more substituents bound to a portion of the amine nitrogens. The substituent or substituents which are bound to the amine nitrogens of the polymer composition can include a hydrophobic moiety and/or a quaternary amine-containing moiety. Suitable amine-containing monomers or repeat units include, but are not limited to, for example, vinylamine, allylamine, diallylamine, diallylmethylamine, and ethyleneimine, which are appropriately substituted, as described above. The hydrophilic nonamine-containing monomer can be, but is not limited to, for example, allyl alcohol, vinyl alcohol, ethylene oxide, propylene oxide, hydroxyethylacrylate, hydroxyethylmethacrylate, hydroxypropylacrylate, hydroxypropylmethacrylate, poly(propyleneglycol) monomethacrylate, poly(ethyleneglycol) monomethacrylate, acrylic acid, carbon dioxide, and sulfur dioxide. Typically, the hydrophilic nonamine-containing monomer or repeat unit comprises from about 10 to about 90 mole percent of the polymer composition.
Inventor(s): Holmes-Farley; Stephen Randall (Arlington, MA), Petersen; John S. (Acton, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Filing Date:Dec 29, 1997
Application Number:08/999,029
Claims:1. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a polymer composition comprising a copolymer characterized by:

(1) one or more hydrophilic non-amine containing monomers; and

(2) one or more amine-containing monomers wherein one or more substituents are bound to a portion of the amine nitrogens, and include a hydrophobic moiety and/or a quaternary amine-containing moiety.

2. The method of claim 1, wherein the amine-containing monomer is selected from the group consisting of: allylamine, diallylamine, diallylmethylamine, vinylamine, and ethyleneimine.

3. The method of claim 1 wherein said hydrophilic non-amine containing monomer is selected from the group consisting of allyl alcohol, vinyl alcohol, ethylene oxide, propylene oxide, hydroxyethylacrylate, hydroxypropylmethacrylate, poly(propyleneglycol) monomethacrylate, and poly(ethyleneglycol) monomethacrylate, acrylic acid, carbon dioxide, and sulfur dioxide.

4. The method of claim 1 wherein said polymer composition comprises one or more exchangeable counterions.

5. The method of claim 4 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CH.sub.3 SO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-, acetate, lactate, succinate, propionate, butyrate, ascorbate, citrate, maleate, folate, an amino acid derivative, or a nucleotide.

6. The method of claim 1 wherein said hydrophobic moiety is a substituted or unsubstituted, normal, branched or cyclic alkyl group having at least six carbon atoms.

7. The method of claim 6, wherein the hydrophobic moiety is an alkyl group of between about eight and twelve carbons.

8. The method of claim 6 wherein the hydrophobic moiety is an alkyl group of about ten carbons.

9. The method of claim 1 wherein the copolymer is crosslinked.

10. The method of claim 9 wherein the copolymer is crosslinked prior to substitution of the amine nitrogens.

11. The method of claim 9 wherein said polymer composition is crosslinked by means of a multifunctional crosslinking co-monomer, said co-monomer being present in an amount from about 0.5% to about 25% by weight, based upon total monomer weight.

12. The method of claim 11 wherein said crosslinking co-monomer is present in an amount from about 1% to about 10% by weight, based upon total monomer weight.

13. The method of claim 1, wherein the quaternary amine-containing moiety has the following formula: ##STR3## wherein, R.sup.1, R.sup.2 and R.sup.3 represent an alkyl group, wherein each R, independently, is a normal or branched, substituted or unsubstituted alkyl group having a carbon atom chain length of between about one to about twenty four carbon atoms,

n is an integer having a value of three or more, and

Y is a negatively-charged counterion.

14. The method of claim 13, wherein R.sup.1, R.sup.2 and R.sup.3 are all methyl groups and n has a value between about three and about twelve carbons.

15. The method of claim 14, wherein n is 6.

16. The method of claim 14, wherein n is 8.

17. The method of claim 14, wherein n is 10.

18. The method of claim 13 wherein at least one of R.sup.1, R.sup.2 and R.sup.3 is a hydrophobic alkyl group having from six to about twenty-four carbons the remainder of which each independently having from one to twenty-four carbons.

19. The method of claim 18 wherein the quaternary amine-containing moiety is 3-(dodecyldimethylammonio)propyl.

20. The method of claim 13 wherein at least two of R.sup.1, R.sup.2 and R.sup.3 are hydrophobic alkyl groups having from six to about twenty-four carbons the remainder having from one to twenty-four carbons.

21. The method of claim 20 wherein the quaternary amine-containing moiety is 4-(dioctylmethylammonio)butyl.

22. The method of claim 13 wherein all three of R.sup.1, R.sup.2 and R.sup.3 are hydrophobic alkyl groups having from six to about twenty-four carbons.

23. A polymer composition comprising a copolymer characterized by:

(1) one or more a hydrophilic non-amine containing monomers; and

(2) one or more amine-containing monomers wherein one or more substituents are bound to a portion of the amine nitrogens, and include a hydrophobic moiety and/or a quaternary amine-containing moiety.

24. The polymer composition of claim 23, wherein the amine-containing monomer is selected from the group consisting of: allylamine, vinylamine, diallylamine, diallylmethylamine, and ethyleneimine.

25. The polymer composition of claim 23 wherein said hydrophilic non-amine containing monomer is selected from the group consisting of allyl alcohol, vinyl alcohol, ethylene oxide, propylene oxide, hydroxyethylacrylate, hydroxyethylmethacrylate, hydroxypropylacrylate, hydroxypropylmethacrylate, poly(propyleneglycol) monomethacrylate, and poly(ethyleneglycol) monomethacrylate, acrylic acid, carbon dioxide, and sulfur dioxide.

26. The polymer composition of claim 23 wherein said polymer composition comprises one or more exchangeable counterions.

27. The polymer composition of claim 26 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CH.sub.3 SO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-, acetate, lactate, succinate, propionate, butyrate, ascorbate, citrate, maleate, folate, an amino acid derivative, or a nucleotide.

28. The polymer composition of claim 23 wherein said hydrophobic moiety is a substituted or unsubstituted, normal, branched or cyclic alkyl group having at least six carbon atoms.

29. The polymer composition of claim 28, wherein the hydrophobic moiety is an alkyl group of between about eight and twelve carbons.

30. The polymer composition of claim 28 wherein the hydrophobic moiety is an alkyl group of about ten carbons.

31. The polymer composition of claim 23 wherein the copolymer is crosslinked.

32. The polymer composition of claim 31 wherein the copolymer is crosslinked prior to substitution of the amine nitrogens.

33. The polymer composition of claim 31 wherein said polymer composition is crosslinked by means of a multifunctional crosslinking co-monomer, said co-monomer being present in an amount from about 0.5% to about 25% by weight, based upon total monomer weight.

34. The polymer composition of claim 33 wherein said crosslinking co-monomer is present in an amount from about 1% to about 10% by weight, based upon total monomer weight.

35. The polymer composition of claim 23, wherein the quaternary amine-containing moiety has the following formula: ##STR4## wherein, R.sup.1, R.sup.2 and R.sup.3 represent an alkyl group, wherein each R, independently, is a normal or branched, substituted or unsubstituted alkyl group having a carbon atom chain length of between about one to about twenty four carbon atoms,

n is an integer having a value of three or more, and

Y is a negatively-charged counterion.

36. The polymer composition of claim 35, wherein R.sup.1, R.sup.2 and R.sup.3 are all methyl groups and n has a value between about three and about twelve carbons.

37. The polymer composition of claim 36, wherein n is 6.

38. The polymer composition of claim 36, wherein n is 8.

39. The polymer composition of claim 36, wherein n is 10.

40. The polymer composition of claim 35 wherein at least one of R.sup.1, R.sup.2 and R.sup.3 is a hydrophobic alkyl group having from six to about twenty-four carbons the remainder of which each independently having from one to twenty-four carbons.

41. The polymer composition of claim 40 wherein the quaternary amine- containing moiety is 3-(dodecyldimethylammonio)propyl.

42. The polymer composition of claim 35 wherein at least two of R.sup.1, R.sup.2 and R.sup.3 are hydrophobic alkyl groups having from six to about twenty-four carbons the remainder having from one to twenty-four carbons.

43. The polymer composition of claim 42 wherein the quaternary amine-containing moiety is 4-(dioctylmethylammonio)butyl.

44. The polymer composition of claim 35 wherein all three of R.sup.1, R.sup.2 and R.sup.3 are hydrophobic alkyl groups having from six to about twenty-four carbons.
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