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Claims for Patent: 5,693,675

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Claims for Patent: 5,693,675

Title: Alkylated amine polymers
Abstract:The invention relates to alkylated amine polymers and a method for removing bile salts from a patient that includes administering to the patient a therapeutically effective amount of product produced by a process comprising alkylating one or more crosslinked amine polymers, salts or copolymers thereof with at least one alkylating agent. The reaction product is characterized in that: (i) at least some of the nitrogen atoms are unreacted with alkylating agent; and (ii) less than 10 mol % of the nitrogen atoms in the polymer react with the alkylating agent to form quaternary ammonium units.
Inventor(s): Mandeville, III; W. Harry (Lynnfield, MA), Holmes-Farley; Stephen Randall (Arlington, MA)
Assignee: GelTex Pharmaceuticals Inc. (Waltham, MA)
Application Number:08/461,298
Patent Claims: 1. An alkylated crosslinked polymer comprising the reaction product of:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of: ##STR3## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group; and

b) at least one aliphatic alkylating agent, said reaction product characterized in that:

(i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent; and

(ii) less than 10 mol % of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.

2. An alkylated crosslinked polymer comprising the reaction product of:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit having the formula ##STR4## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group; and

b) at least one aliphatic alkylating agent, said reaction product characterized in that:

(i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent; and

(ii) less than 10 mol % of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.

3. The polymer of claim 2 wherein said polymer is crosslinked by means of a multifunctional crosslinking agent, said agent being present in an amount from about 0.5-25% by weight, based upon the combined weight of monomer and crosslinking agent.

4. The polymer of claim 2 wherein said crosslinking agent is present in an amount from about 2.5-20% by weight, based upon the combined weight of monomer and crosslinking agent.

5. The polymer of claim 2 wherein said crosslinking agent comprises epichlorohydrin.

6. The polymer of claim 2 wherein said polymer, salt or copolymer thereof is characterized by a repeat unit having the formula ##STR5##

7. The polymer of claim 2 wherein said alkylating agent has the formula RX where R is a C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 hydroxyalkyl, C.sub.1 -C.sub.20 alkylammonium, or C.sub.1 -C.sub.20 alkylamido group and X is one or more electrophilic leaving groups.

8. The polymer of claim 7 wherein X is a halide, epoxy, tosylate, or mesylate.

9. The polymer of claim 2 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents has the formula RX where R is a C.sub.1 -C.sub.20 alkyl group and X is one or more electrophilic leaving groups, and the other of said alkylating agents has the formula R'X where R' is a C.sub.1 -C.sub.20 alkyl ammonium group and X is one or more electrophilic leaving groups.

10. The polymer of claim 9 wherein one of said alkylating agents having the formula RX is an alkyl halide and the other of said alkylating agents having the formula R'X is an alkyl halide ammonium salt.

11. The polymer of claim 10 wherein said alkyl halide is a C.sub.4 -C.sub.20 alkyl halide and said alkyl halide ammonium salt is a C.sub.4 -C.sub.18 alkyl halide ammonium salt.

12. The polymer of claim 10 wherein said alkyl halide is a C.sub.10 alkyl halide and said alkyl halide ammonium salt is a C.sub.6 alkyl halide ammonium salt.

13. The polymer of claim 2 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents has the formula RX where R is a C.sub.1 -C.sub.20 alkyl group and X is one or more electrophilic leaving groups, and the other of said alkylating agents has the formula R'X where R' is a C.sub.1 -C.sub.20 hydroxyalkyl group and X is one or more electrophilic leaving groups.

14. The polymer of claim 13 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is a hydroxy alkyl halide.

15. The polymer of claim 2 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents is a C.sub.1 -C.sub.20 dihaloalkane and the other of said alkylating agents is a C.sub.1 -C.sub.20 alkylammonium salt.

16. The polymer of claim 1 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl halide.

17. The polymer of claim 16 wherein said alkyl halide is a C.sub.4 -C.sub.18 alkyl halide.

18. The polymer of claim 1 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 dihaloalkane.

19. The polymer of claim 18 wherein said dihaloalkane is a 1,10-dihalodecane.

20. The polymer of claim 1 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 hydroxyalkyl halide.

21. The polymer of claim 20 wherein said hydroxyalkyl halide is an 11-halo-1-undecanol.

22. The polymer of claim 1 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl halide ammonium salt.

23. The polymer of claim 22 wherein said alkyl halide ammonium salt is a C.sub.4 -C.sub.12 haloalkyl trimethylammonium salt.

24. The method of claim 1 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl epoxy ammonium salt.

25. The polymer of claim 24 wherein said alkyl epoxy ammonium salt is a (glycidylpropyl)trimethylammonium salt.

26. The polymer of claim 1 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 epoxy alkylamide.

27. The polymer of claim 26 wherein said epoxy alkylamide is selected from the group consisting of N-(2,3-epoxypropane)butyramide, N-(2,3-epoxypropane)hexanamide, and combinations thereof.

28. The polymer of claim 1 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents has the formula RX where R is a C.sub.1 -C.sub.20 alkyl group and X is one or more electrophilic leaving groups, and the other of said alkylating agents has the formula R'X where R' is a C.sub.1 -C.sub.20 alkyl ammonium group and X is one or more electrophilic leaving groups.

29. The polymer of claim 28 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is an alkyl halide ammonium salt.

30. The polymer of claim 29 wherein said alkyl halide is a C.sub.4 -C.sub.20 alkyl halide and said alkyl halide ammonium salt is a C.sub.4 -C.sub.18 alkyl halide ammonium salt.

31. The polymer of claim 29 wherein said alkyl halide is a C.sub.10 alkyl halide and said alkyl halide ammonium salt is a C.sub.6 alkyl halide ammonium salt.

32. The polymer of claim 1 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents has the formula RX where R is a C.sub.1 -C.sub.20 alkyl group and X is one or more electrophilic leaving groups, and the other of said alkylating agents has the formula R'X where R' is a C.sub.1 -C.sub.20 hydroxyalkyl group and X is one or more electrophilic leaving groups.

33. The polymer of claim 32 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is a hydroxyalkyl halide.

34. The polymer of claim 1 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents is a C.sub.1 -C.sub.20 dihaloalkane and the other of said alkylating agents is a C.sub.1 -C.sub.20 alkylammonium salt.

35. The polymer of claim 6 wherein said polymer is reacted with at least two of said alkylating agent, one of said alkylating agents is a C.sub.10 alkyl halide and the other of said alkylating agents is a C.sub.6 alkyl halide ammonium salt.

36. An alkylated crosslinked polymer comprising the reaction product of:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of: ##STR6## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group; and

b) at least one aliphatic alkylating agent, said reaction product characterized in that:

(i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent;

(ii) less than 10 mol % of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units; and

(iii) said polymer is crosslinked by means of a multifunctional crosslinking agent, said agent being present in an amount from 1-10% by weight based upon the combined weight of monomer and crosslinking agent.

37. An alkylated crosslinked polymer comprising the reaction product of:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of: ##STR7## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group; and

b) at least one hydrophobic aliphatic alkylating agent, said reaction product characterized in that:

(i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent; and

(ii) less than 10 mol % of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.

38. An alkylated crosslinked polymer comprising the reaction product of:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of: ##STR8## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group; and

b) at least one alkylating agent, having the formula RX wherein R is a C.sub.1 -C.sub.20 alkylammonium group and X is an electrophilic leaving group, said reaction product characterized in that:

(i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent; and

(ii) less than 10 mol % of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.
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