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Details for Patent: 5,840,766

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Details for Patent: 5,840,766

Title: Process for removing bile salts from a patient and compositions therefor
Abstract:A method for removing bile salts from a patient by ion exchange by administering to the patient a therapeutically effective amount of one or more highly crosslinked polymers characterized by a repeat unit having the formula ##STR1## or copolymer thereof, where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group: M is ##STR2## Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR3## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group.
Inventor(s): Mandeville, III; W. Harry (Lynnfield, MA), Holmes-Farley; Stephen Randall (Arlington, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Filing Date:Oct 28, 1997
Application Number:08/959,471
Claims:1. The therapeutic composition effective for removing bile salts comprising a therapeutic amount of a crosslinked polymer comprising

(1) a monoreactive hydrophobic co-monomer and

(2) a repeat unit having the formula ##STR24## or copolymer thereof, where n-is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR25## Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR26## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group.

2. A therapeutic composition effective for removing bile salts comprising a therapeutic amount of the reaction product of:

(a) one or more crosslinked polymers, salts or copolymers thereof comprising a repeat unit having the formula: ##STR27## where n is an-integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR28## or --Z--R.sup.2 ; Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR29## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group; and

(b) at least one alkylating agent having the formula RX where R is a C.sub.1 -C.sub.20 alkylammonium and X is one or more electrophilic leaving groups.

3. A polymer composition effective for removing bile salts comprising a therapeutic amount of the reaction product of:

(a) one or more crosslinked polymers, salts or copolymers thereof comprising a repeat unit having the formula: ##STR30## where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR31## or --Z--R.sup.2 ; Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR32## where p=0-10, and each R.sup.4, R.sup.5, and R6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group; and

(b) at least one alkylating agent having the formula RX where R is a C.sub.1 -C.sub.20 alkylammonium and X is one or more electrophilic leaving groups.

4. The polymer composition of claim 3 wherein said polymer is crosslinked by means of a multifunctional crosslinking co-monomer, said co-monomer being present in an amount from about 0.5-25% by weight, based upon total monomer weight.

5. The polymer composition of claim 4 wherein said crosslinking co-monomer is present in an amount from about 1-10% by weight, based upon total monomer weight.

6. The polymer composition of claim 3 wherein said reaction product is a pharmaceutically acceptable salt further comprising one or more counterions.

7. The polymer composition of claim 6 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CH.sub.3 OSO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-, acetate, lactate, succinate, propionate, butyrate, ascorbate, citrate, maleate, folate an amino acid derivative, a nucleotide, a lipid or a phospholipid.

8. The polymer composition of claim 3 wherein said repeat unit has the formula ##STR33## or salt or copolymer thereof, wherein Z is NR.sup.3 or (CH.sub.2).sub.m, R.sup.2 is ##STR34## R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n, m, and p are as defined in claim 3.

9. The polymer composition of claim 3 wherein said reaction product is a pharmaceutically acceptable salt comprising one or more counterions.

10. The polymer composition of claim 9 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CH.sub.3 OSO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-, acetate, lactate, succinate, propionate, butyrate, ascorbate, citrate, maleate, folate an amino acid derivative, a nucleotide, a lipid or a phospholipid.

11. The polymer composition of claim 3 wherein X is a halide, epoxy, tosylate, or mesylate group.

12. A polymer composition effective for removing bile salts comprising a therapeutic amount of the reaction product of:

(a) one or more crosslinked polymers, salts or copolymers thereof comprising a repeat unit having the formula: ##STR35## where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR36## or --Z--R.sup.2 ; Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR37## where p=0-10, R.sup.4, R.sup.5 are H, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group; and

(b) at least one alkylating agent, wherein 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.

13. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of the reaction product of:

(a) one or more crosslinked polymers, salts or copolymers thereof comprising a repeat unit having the formula: ##STR38## where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR39## or --Z--R.sup.2 ; Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR40## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group; and

(b) at least one alkylating agent having the formula RX where R is a C.sub.1 -C.sub.20 alkylammonium and X is one or more electrophilic leaving groups.

14. The method of claim 13 wherein said polymer is crosslinked by means of a multifunctional crosslinking co-monomer, said co-monomer being present in an amount from about 0.5-25% by weight, based upon total monomer weight.

15. The method of claim 14 wherein said crosslinking co-monomer is present in an amount from about 1-10% by weight, based upon total monomer weight.

16. The method of claim 13 wherein said reaction product is a pharmaceutically acceptable salt further comprising one or more counterions.

17. The method of claim 16 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CH.sub.3 OSO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-, acetate, lactate, succinate, propionate, butyrate, ascorbate, citrate, maleate, folate an amino acid derivative, a nucleotide, a lipid or a phospholipid.

18. The method of claim 13 wherein said repeat unit has the formula ##STR41## or copolymer thereof, wherein Z is NR.sup.3 or (CH.sub.2).sub.m, R.sup.2 is ##STR42## R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n, m, and p are as defined in claim 13.

19. The method of claim 13 wherein X is a halide, epoxy, tosylate, or mesylate group.

20. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of the reaction product of:

(a) one or more crosslinked polymers, salts or copolymers thereof comprising a repeat unit having the formula: ##STR43## where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR44## or --Z--R.sup.2 ; Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR45## where p=0-10, R.sup.4 and R5 are H, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group; and

(b) at least one alkylating agent, wherein 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.

21. The method of claim 20 wherein said repeat unit has the formula ##STR46## or copolymer thereof, wherein Z is NR.sup.3 or (CH.sub.2).sub.m, R.sup.2 is ##STR47## R.sup.1, R.sup.3, R.sup.4, R.sup.5, R6, n, m, and p are as defined in claim 20.

22. The method of claim 20 wherein said reaction product is a pharmaceutically acceptable salt further comprising one or more counterions.

23. The method of claim 20 wherein at least one of said counterions is Cl.sup.-, Br.sup.-, CH.sub.3 OSO.sub.3.sup.-, HSO.sub.4.sup.-, SO.sub.4.sup.2-, HCO.sub.3.sup.-, CO.sub.3.sup.2-, acetate, lactate, succinate, propionate, butyrate, ascorbate, citrate, maleate, folate an amino acid derivative, a nucleotide, a lipid or a phospholipid.

24. The method of claim 20 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 hydroxy alkyl, C.sub.1 -C.sub.20 aralkyl, 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.

25. The method of claim 24 wheein X is halide, epoxy, tosylate or mesylate group.

26. The method of claim 25 wherein said alkylating agent is a C.sub.1 -C.sub.20 alkyl halide.

27. The method of claim 25 wherein said alkylating agent is a C.sub.1 -C.sub.20 alkyl halide ammonium salt.

28. The method of claim 25 wherein said alkylating agent is a C.sub.1 -C.sub.20 dihaloalkane, C.sub.1 -C.sub.20 hydroxyalkyl halide, C.sub.1 -C.sub.20 aralkyl halide, C.sub.1 -C.sub.20 alkyl epoxy ammonium salt or C.sub.1 -C.sub.20 epoxy alkylamide.
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