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Details for Patent: 6,129,910

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Details for Patent: 6,129,910

Title: Water-insoluble noncrosslinked bile acid sequestrants
Abstract:The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises the step of orally administering to a mammal, such as a human, a therapeutically effective amount of a new class of water-insoluble noncrosslinked amine polymers. The water-insoluble noncrosslinked amine polymer comprises an amine-containing monomer or repeat unit which has one or more substituents bound to an amine nitrogen of the amine polymer. The substituent or substituents which are bound to the amine nitrogens of the amine polymer include a hydrophobic moiety and/or a quaternary amine-containing moiety.
Inventor(s): Holmes-Farley; Stephen Randall (Arlington, MA), Mandeville, III; W. Harry (Lynnfield, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Filing Date:Dec 29, 1997
Application Number:08/999,351
Claims:1. A method for binding bile salts in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of a water-insoluble noncrosslinked amine polymer having a substituent bound to an amine nitrogen of the amine polymer, the substituent including a quaternary amine-containing moiety.

2. The method of claim 1 wherein said quaternary amine-containing moiety has the chemical formula: ##STR3## 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.

3. The method of claim 2 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is three.

4. The method of claim 2 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is four.

5. The method of claim 2 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is six.

6. A method for binding bile salts in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of a water-insoluble noncrosslinked amine polymer having a first substituent, bound to an amine nitrogen of the amine polymer, that includes a hydrophobic moiety and a second substituent bound to an amine nitrogen of the amine polymer, the second substituent including a quaternary amine-containing moiety.

7. The method of claim 6 wherein said hydrophobic moiety is a decyl group.

8. The method of claim 6 wherein said quaternary amine-containing moiety has the chemical formula: ##STR4## 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.

9. A method for binding bile salts in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of a water-insoluble noncrosslinked amine polymer having a substituent bound to an amine nitrogen of the amine polymer, the substituent including a hydrophobic moiety.

10. A method for reducing blood cholesterol in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of a water-insoluble noncrosslinked amine polymer having a substituent bound to an amine nitrogen of the amine polymer, the substituent including a quaternary amine-containing moiety.

11. The method of claim 10 wherein said quaternary amine-containing moiety has the chemical formula: ##STR5## 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.

12. The method of claim 11 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is three.

13. The method of claim 11 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is four.

14. The method of claim 11 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecycl group, the remaining groups are methyl groups and n is six.

15. A method for reducing blood cholesterol in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of a water-insoluble noncrosslinked amine polymer having a first substituent, bound to an amine nitrogen of the amine polymer, that includes a hydrophobic moiety and a second substituent bound to an amine of the amine polymer, the second substituent including a quaternary amine-containing moiety.

16. The method of claim 15 wherein said hydrophobic moiety is a decyl group.

17. The method of claim 15 wherein said quaternary amine-containing moiety has the chemical formula: ##STR6## 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.

18. A method for reducing blood cholesterol in a mammal, comprising the step of orally administering to the mammal a therapeutic amount of a water-insoluble noncrosslinked amine polymer having a substituent bound to an amine nitrogen of the amine polymer, the substituent including a hydrophobic moiety.

19. A water-insoluble noncrosslinked amine polymer having a substituent bound to an amine nitrogen of the amine polymer, the substituent including a quaternary amine-containing moiety.

20. The polymer of claim 19 wherein said quaternary amine-containing moiety has the chemical formula: ##STR7## 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.

21. The polymer of claim 20 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is three.

22. The polymer of claim 20 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is four.

23. The polymer of claim 20 wherein one of R.sup.1, R.sup.2, and R.sup.3 is a dodecyl group, the remaining groups are methyl groups and n is six.

24. A water-insoluble noncrosslinked amine polymer having a first substituent, bound to an amine nitrogen of the amine polymer, that includes a hydrophobic moiety and a second substituent bound to an amine nitrogen of the amine polymer, the second substituent including a quaternary amine-containing moiety.

25. The polymer of claim 24 wherein said hydrophobic moiety is a decyl group.

26. The polymer of claim 24 wherein said quaternary amine-containing moiety has the chemical formula: ##STR8## R.sup.1, R.sup.2 and R.sup.3 represent 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.

27. A water-insoluble noncrosslinked amine polymer having a substituent bound to an amine nitrogen of the amine polymer, the substituent including a hydrophobic moiety.
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