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Details for Patent: 6,225,355

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Details for Patent: 6,225,355

Title: Process for removing bile salts from a patient and alkylated compositions therefor
Abstract:The invention relates to a method for removing bile salts from a patient in need thereof and compositions use full in the method. The method comprises administering to the patient a therapeutically effective amount of a salt of an alkylated and crosslinked polymer. The alkylated and crosslinked polymer salt comprises the reaction product of polymers, or salts and copolymers thereof having amine containing repeat units, with at least one aliphatic alkylating agent and a crosslinking agent.
Inventor(s): Mandeville, III; W. Harry (Lynnfield, MA), Holmes-Farley; Stephen Randall (Arlington, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Filing Date:Mar 22, 2000
Application Number:09/532,984
Claims:1. The salt of an alkylated and crosslinked polymer comprising the reaction product of:

(a) one or more polymers, or salts and copolymers thereof having a repeat unit selected from the group consisting of: ##STR3##

and

where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group;

(b) at least one aliphatic alkylating agent; and

(c) a crosslinking agent, wherein said reaction product has:

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

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

(iii) a fixed positive charge and one or more counterions and wherein the polymer is alkylated prior to crosslinking.

2. The polymer salt of claim 1 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CHOSO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-.

3. The polymer salt of claim 1 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 salt of claim 1 wherein the crosslinking agent comprises epichlorohydrin.

5. The polymer salt of claim 1 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.

6. The polymer salt of claim 5 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl halide.

7. The polymer salt of claim 5 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl halide ammonium salt.

8. The polymer salt of claim 7 wherein said alkyl halide ammonium salt is a C.sub.4 -C.sub.12 haloalkyl trimethylammonium salt.

9. The polymer salt 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.

10. The polymer salt 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 salt of claim 10 wherein said alkyl halide is a C.sub.4 -C.sub.20 alkyl halide band said alkyl halide ammonium salt is a C.sub.4 -C.sub.8 alkyl halide ammonium salt.

12. The polymer salt of claim 11 wherein said alkyl halide is a C.sub.10 alkyl halide and said alkyl halide ammonium salt is a C.sub.6 alkyl halide trimethyl ammonium salt.

13. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of the salt of an alkylated and crosslinked polymer comprising the reaction product of:

(a) one or more polymers, or salts and copolymers thereof having a repeat unit selected from the group consisting of: ##STR4##

and

where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group;

(b) at least one aliphatic alkylating agent; and

(c) a crosslinking agent, wherein in the reaction product has:

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

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

(iii) a fixed positive charge and one or more counterions and wherein the polymer is alkylated prior to crosslinking.

14. The method of claim 1 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CHOSO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-.

15. The method of claim 13 wherein said polymer salt 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.

16. The method of claim 15 wherein the crosslinking agent comprises epichlorohydrin.

17. The method of claim 13 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.

18. The method of claim 17 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl halide.

19. The method of claim 17 wherein said alkylating agent comprises a C.sub.1 -C.sub.20 alkyl halide ammonium salt.

20. The method of claim 19 wherein said alkyl halide ammonium salt is a C.sub.4 -C.sub.12 haloalkyl trimethylarnmonium salt.

21. The method of claim 13 wherein said polymer salt 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.

22. The method of claim 21 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.

23. The method of claim 22 wherein said alkyl halide is a C.sub.4 -C.sub.20 alkyl halide and said alkyl halide ammionium salt is a C.sub.4 -C.sub.18 alkyl halide ammonium salt.

24. The method of claim 23 wherein said alkyl halide is a C.sub.10 alkyl halide and said alkyl halide ammonium salt is a C.sub.6 alkyl halide trimethyl ammonium salt.
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