Polymers containing spirobicyclic ammonium moieties as bile acid sequestrants
First Claim
1. A method for removing bile acids from a patient comprising administering to said patient a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer, copolymer or salt thereof comprising a repeat unit having the structural formula:
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whereinY is a negatively-charged counter ion;
m is a integer from zero to about seven; and
Ring A and Ring B are each, independently, substituted or unsubstituted.
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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 administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.
54 Citations
22 Claims
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1. A method for removing bile acids from a patient comprising administering to said patient a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer, copolymer or salt thereof comprising a repeat unit having the structural formula:
-
wherein Y is a negatively-charged counter ion;
m is a integer from zero to about seven; and
Ring A and Ring B are each, independently, substituted or unsubstituted. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
wherein, R3, R4 and R5 are independently substituted or unsubstituted, normal or branched alkyl groups comprising about one to twenty-four carbon atoms;
n is an integer from one to about twenty; and
Y is a negatively-charged counter ion.
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12. The method of claim 11 wherein:
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R3, R4 and R5 are methyl groups, and n is an integer from about three to twelve.
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13. The method of claim 12 wherein at least one of R3, R4 and R5 is a hydrophobic alkyl group having from four to about twenty-four carbon atoms, the remainder of which each, independently, have from one to twenty-four carbon atoms.
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14. The method of claim 13 wherein at least two of R3, R4 and R5 are hydrophobic alkyl groups having from four to about twenty-four carbon atoms, the remainder having from one to twenty-four carbon atoms.
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15. The method of claim 13 wherein all three of R3, R4 and R5 are hydrophobic alkyl groups having from four to about twenty-four carbon atoms.
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16. The method of claim 10 wherein said hydrophobic group is a substituted or unsubstituted, normal, branched or cyclic alkyl group comprising four to about thirty carbon atoms.
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17. The method of claim 16 wherein said hydrophobic group comprises four to about fourteen carbon atoms.
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18. The method of claim 5 wherein said additional monomer is an ammonium-containing monomer.
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19. The method of claim 18 wherein said ammonium-containing monomer is:
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or a combination thereof;
whereinY is a negatively-charged counter ion; and
R1 and R2 can each, independently, be hydrogen, a C1-C30 aliphatic group, C1-C30 alkyl group, a quaternary ammonium-containing group or an aromatic group.
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20. The method of claim 19 wherein R1 and R2 are each independently hydrogen or a C1-C12 alkyl group.
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21. A method for removing bile acids from a patient, comprising administering to said patient a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer, copolymer or salt thereof comprising a repeat unit having the structural formula:
-
wherein Y is a negatively-charged counter ion.
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22. A method for removing bile acids from a patient, comprising administering to said patient a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer, copolymer or salt thereof comprising a repeat unit having the structural formula:
-
wherein R1 and R2 can each independently be hydrogen, a C1-C30 aliphatic group, C1-C30 alkyl group, an aromatic group, a quaternary ammonium-containing group or a hydrophobic group, and Y is a negatively-charged counter ion.
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Specification