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Claims for Patent: 5,919,832

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Claims for Patent: 5,919,832

Title: Amine polymer sequestrant and method of cholesterol depletion
Abstract:An amine polymer includes first and second substituents bound to amines of the polymer. The first substituent includes a hydrophobic moiety. The second substituent includes a quaternary amine-containing moiety. A method for binding bile salts of bile acids in a mammal includes orally administering to the mammal a therapeutically-effective amount of the amine polymer.
Inventor(s): Mandeville, III; W. Harry (Lynnfield, MA), Holmes-Farley; Stephen Randall (Arlington, MA)
Assignee: Geltex Pharmaceuticals Inc. (Waltham, MA)
Application Number:08/779,779
Patent Claims: 1. An amine polymer, comprising:

a) a first substituent, bound a first amine of the amine polymer, that includes a hydrophobic aliphatic moiety which is an alkyl group of at least six carbons; and

b) a second substituent, bound to a second amine of the amine polymer, that includes an aliphatic quaternary amine-containing moiety.

2. The amine polymer of claim 1, wherein the hydrophobic moiety is an alkyl group of between about eight and twelve carbons.

3. The amine polymer of claim 1, wherein the hydrophobic moiety is an alkyl group of about ten carbons.

4. The amine polymer of claim 1, wherein said amine polymer is crosslinked prior to substitution by said first and second substituents.

5. The amine polymer of claim 4, wherein said amine polymer comprises a crosslink moiety that is present in a range of between about 0.5 and twenty mole percent of amines of the polymer.

6. The amine polymer of claim 5, wherein said crosslinking moiety is present in a range of between about 0.5 and six mole percent of amines of the polymer.

7. The amine polymer of claim 5, wherein the quaternary amine-containing moiety is an alkyltrimethyl ammonium.

8. The amine polymer of claim 7, wherein said alkyltrimethyl ammonium has an alkyl component having between about two and twelve carbons.

9. The amine polymer of claim 8, wherein said alkyl component is a hexyl group.

10. The amine polymer of claim 8, wherein said alkyl component is an octyl group.

11. The amine polymer of claim 8, wherein the alkyl component is a decyl group.

12. A crosslinked poly(allylamine), comprising:

a) a first substituent, bound to an amine of the amine polymer, that includes a hydrophobic decyl moiety; and

b) a second substituent, bound to an amine of the amine polymer, that include hexyltrimerhylammonium

wherein the poly(allylamine) is crosslinked by epichlorohydrin prior to substitution by (a) and (b), and said epichlorohydrin is present in a range of between about 0.5 and twenty mole percent of the amines of the polymer.

13. The amine polymer of claim 6, wherein the hydrophobic moiety is an alkyl group of at least six carbons.

14. The amine polymer of claim 5 wherein the hydrophobic moiety is an alkyl group of between about eight and twelve carbons.

15. The amine polymer of claim 5, wherein the hydrophobic moiety is an alkyl group of about ten carbons.

16. The amine polymer of claim 13, wherein the quaternary amine containing moiety is an alkyltrialkyl ammonium.

17. The amine polymer of claim 16, wherein said amine polymer is poly(ethylenimine).

18. The method of claim 16, wherein said amine polymer has a hydrocarbon backbone.

19. The amine polymer of claim 18, wherein said amine polymer is poly(vinylamine).

20. The amine polymer of claim 18, wherein said amine polymer is a poly(allylamine).

21. The amine polymer of claim 20, wherein the hydrophobic moiety of said first amine substituent is a decyl group.

22. The amine polymer of claim 21, wherein the quaternary amine-containing moiety of said second amino substituent is hexyltrimethylammonium.

23. The amine polymer of claim 22, wherein the amine polymer is crosslinked by a crosslinking moiety that is present in a range of between about two and six mole percent of the amines of the polymer.

24. The amine polymer of claim 23, wherein said crosslinking moiety is epichlorohydrin.
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