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Details for Patent: 5,969,090

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Details for Patent: 5,969,090

Title: Hydrophobic sequestrant for cholesterol depletion
Abstract:The present invention relates to a poly(allylamine) polymer and, more generally, a hydrocarbon amine polymer. Preferably, these polymers are crosslinked. The present invention also relates to methods of forming these polymers and methods for their use. Further, the present invention relates to alkylating agents that can be employed to form the polymers and to methods for forming the alkylating agents. Generally, the polymer sequestrant includes a substituent bound to an amine of the polymer. The substituent includes a quaternary amine-containing moiety having one, two or three terminal hydrophobic substituents. A method of preparing quaternary amine-containing alkylating agents includes reacting an unsymmetrical dihalide with a tertiary amine having at least one hydrophobic substituent. A method for binding bile salts of bile acids in a mammal includes orally administering to the mammal a therapeutically-effective amount of the polymer sequestrant.
Inventor(s): Mandeville, III; W. Harry (Lynnfield, MA), Holmes-Farley; Stephen Randall (Arlington, MA), Petersen; John S. (Acton, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Filing Date:Nov 03, 1998
Application Number:09/185,157
Claims:1. A hydrocarbon amine polymer, comprising a substituent bound to an amine of the hydrocarbon amine polymer, the substituent including a quaternary amine-containing moiety that is bound to said amine of the hydrocarbon amine polymer by an alkylene linking group having three or more carbons, said quaternary amine-containing moiety also including at least one terminal hydrophobic alkyl substituent, having between about 6 and 20 carbons.

2. The hydrocarbon amine polymer of claim 1, wherein the terminal hydrophobic alkyl substituent includes between about eight and twenty carbons.

3. The hydrocarbon amine polymer of claim 1, wherein the terminal hydrophobic alkyl substituent includes about ten carbons.

4. The hydrocarbon amine polymer of claim 1, wherein the terminal hydrophobic alkyl substituent includes about twelve carbons.

5. The hydrocarbon amine polymer of claim 1, wherein the terminal hydrophobic alkyl substituent includes about fourteen carbons.

6. The hydrocarbon amine polymer of claim 1, wherein said hydrocarbon amine polymer is crosslinked.

7. The hydrocarbon amine polymer of claim 6, wherein said hydrocarbon amine polymer includes a crosslinking moiety that is present in a range of between about 0.5 and twenty percent of amines of the polymer.

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

9. The hydrocarbon amine polymer of claim 1, wherein said hydrocarbon amine polymer is poly(vinylamine).

10. The hydrocarbon amine polymer of claim 1, wherein said hydrocarbon amine polymer is poly(ethyleneimine).

11. The hydrocarbon amine polymer of claim 1, wherein said hydrocarbon amine polymer is poly(allylamine).

12. A crosslinked poly(allylamine), comprising a substituent bound to an amine of the amine polymer, the substituent including a quaternary amine-containing moiety that is bound to said amine of the poly(allylamine) by an alkylene linking group having three or more carbons, said quaternary amine-containing moiety also including at least one terminal hydrophobic alkyl substituent, having between about 6 and 20 carbons wherein the poly(allylamine) is crosslinked by epichlorohydrin that is present in a range of between about 0.5 and six percent of the amines of the polymer.
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