Claims for Patent: 5,607,669

Summary for Patent: 5,607,669

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 R. (Arlington, MA)
Assignee:	GelTex Pharmaceuticals, Inc. (Waltham, MA)
Application Number:	08/471,769
Patent Claims:	1. A method for binding bile salts in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of an amine polymer having a first substituent, bound to a first amine of the amine polymer, that includes a hydrophobic aliphatic moiety, and a second substituent, bound to a second amine of the amine polymer, that includes an aliphatic quaternary amine-containing moiety. 2. A method for reducing blood cholesterol in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of an amine polymer having a first substituent, bound to a first amine of the amine polymer, that includes a hydrophobic aliphatic moiety, and a second substituent, bound to a second amine of the amine polymer, that includes an aliphatic quaternary amine-containing moiety. 3. A method for treating atherosclerosis in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of an amine polymer having a first substituent, bound to a first amine of the amine polymer, that includes a hydrophobic aliphatic moiety, and a second substituent, bound to a second amine of the amine polymer that includes an aliphatic quaternary amine-containing moiety. 4. A method for treating hypercholesterolemia in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of an amine polymer having a first substituent, bound to a first amine of the amine polymer, that includes a hydrophobic aliphatic moiety, and a second substituent, bound to a second amine of the amine polymer, that includes an aliphatic quaternary amine-containing moiety. 5. The method of claim 1, wherein said amine polymer is cross-linked. 6. The method of claim 5, wherein said amine polymer is cross-linked prior to substitution by said first and second substituents. 7. The method of claim 6, wherein said amine polymer comprises a crosslinking moiety that is present in a range of between about 0.5 and twenty percent of amines of the polymer. 8. The method of claim 7, wherein the crosslinking moiety is present in a range of between about 0.5 and six percent of amines of the polymer. 9. The method of claim 7, wherein the hydrophobic moiety is an alkyl group of at least six carbons. 10. The method of claim 9, wherein the hydrophobic moiety is an alkyl group of between about eight and twelve carbons. 11. The method of claim 10, wherein the hydrophobic moiety is an alkyl group of about ten carbons. 12. The method of claim 9, wherein the quaternary amine-containing moiety is an alkyltrialkyl ammonium. 13. The method of claim 12, wherein said alkyltrialkyl ammonium is an alkyltrimethyl ammonium wherein said alkyl has between about two and twelve carbons. 14. The method of claim 13, wherein said alkyl is a hexyl group. 15. The method of claim 13, wherein said alkyl is an octyl group. 16. The method of claim 13, wherein said alkyl is a decyl group. 17. The method of claim 12, wherein said amine polymer is poly(ethylenimine). 18. The method of claim 12, wherein said amine polymer has a hydrocarbon backbone. 19. The method of claim 18, wherein said amine polymer is poly(vinylamine). 20. The method of claim 17, wherein said amine polymer is poly(allylamine). 21. The method of claim 20, wherein the hydrophobic moiety of said first amino substituent is a decyl group. 22. The method of claim 21, wherein the quaternary amine-containing moiety of said second amino substituent is hexyltrimethylammonium. 23. The method of claim 22, wherein the amine polymer is crosslinked by a crosslinking moiety that is present in a range of between about 0.5 and twenty percent of the amines of the polymer. 24. The method of claim 23, wherein said crosslinking moiety is epichlorohydrin. 25. A method of reducing cholesterol in a mammal comprising the step of orally administering to the mammal a therapeutic amount of a crosslinked poly(allylamine) polymer 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 includes hexyltrimethylammonium, 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 poly(allylamine).