.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,679,717

« Back to Dashboard

Claims for Patent: 5,679,717

Title: Method for removing bile salts from a patient with alkylated amine polymers
Abstract: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:08/460,980
Patent Claims: 1. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:

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 with

b) at least one aliphatic alkylating agent, said 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. The method 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% weight, based upon the combined weight of monomer and crosslinking agent.

3. The method 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.

4. The method of claim 2 wherein said crosslinking agent comprises epichlorohydrin.

5. The method of claim 1 wherein said polymer, salt or copolymer thereof is characterized by a repeat unit having the formula ##STR4##

6. The method of claim 1 wherein said polymer, salt or copolymer thereof is characterized by a repeat unit having the formula

7. The method of claim 1 wherein said polymer, salt or copolymer thereof is characterized by a repeat unit having the formula

8. The method 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.

9. The method of claim 8 wherein X is a halide, epoxy, tosylate, or mesylate group.

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

11. The method of claim 10 wherein said alkyl halide is a C.sub.4 -C.sub.18 alkyl halide.

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

13. The method of claim 12 wherein said dihaloalkane is a 1,10-dihalodecane.

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

15. The method of claim 14 wherein said hydroxyalkyl halide is an 11-halo-1-undecanol.

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

17. The method of claim 16 wherein said alkyl halide ammonium salt is a C.sub.4 -C.sub.12 haloalkyl trimethyl-ammonium salt.

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

19. The method of claim 18 wherein said alkyl epoxy ammonium salt is a (glycidylpropyl)trimethyl- ammonium salt.

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

21. The method of claim 20 wherein said epoxy alkylamide is selected from the group consisting of N-(2,3-epoxypropane)butyramide, N-(2,3-epoxy- propane) hexanamide, and combinations thereof.

22. The method of claim 1 wherein said polymer is reacted with at least two alkylating agents, one of said alkylating agents having 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 having 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.

23. The method of claim 22 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is an alkyl halide ammonium salt.

24. The method of claim 1 wherein said polymer is reacted with at least two alkylating agents, one of said alkylating agents having 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 having 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.

25. The method of claim 24 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is a hydroxy alkyl halide.

26. The method of claim 1 wherein said polymer is reacted with at least two alkylating agents, 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.

27. A method of removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit having the formula ##STR5## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group with

b) at least one alkylating agent, said 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.

28. The method of claim 27 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.

29. The method of claim 28 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.

30. The method of claim 28 wherein said crosslinking agent comprises epichlorohydrin.

31. The method of claim 27 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.19 -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.

32. The method of claim 31 wherein X is a halide, epoxy, tosylate, or mesylate groups.

33. The method of claim 27 wherein said polymer is reacted with at least two alkylating agents, one of said alkylating agents having 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 having 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.

34. The method of claim 33 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is an alkyl halide ammonium salt.

35. The method of claim 34 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.

36. The method of claim 35 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.

37. The method of claim 27 wherein said polymer is reacted with at least two alkylating agents, one of said alkylating agents having 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 having 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.

38. The method of claim 37 wherein one of said alkylating agents is an alkyl halide and the other of said alkylating agents is a hydroxy alkyl halide.

39. The method of claim 27 wherein said polymer is reacted with at least two alkylating agents, 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.

40. The method of claim 10 wherein said alkyl halide is selected from the group consisting of: n-butyl halides, n-hexyl halides, n-octyl halides, n-decyl halides, n-dodecyl halides, n-tetradecyl halides, n-octadecyl halides and combinations thereof.

41. The method of claim 16 wherein said alkyl halide ammonium salt is selected from the group consisting of: (4-halobutyl)trimethylammonium salts, (6-halohexyl)-trimethylammonium salts, (8-halooctyl)trimethylammonium salts, (10-halodecyl)trimethylammonium salts, (12-halododecyl)trimethylammonium salts and combinations thereof.

42. A method of removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit having the formula ##STR6## where n is a positive integer and each R, independently, is H or a Cm-C.sub.s alkyl group with

b) at least one aliphatic alkylating agent, said 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.

43. The method of claim 42 wherein said polymer, salt or copolymer thereof is reacted with at least two aliphatic alkylating agents, one of said alkylating agents having 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 having 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.

44. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:

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 with

b) at least one aliphatic alkylating agent, said 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.

45. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:

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 with

b) at least one hydrophobic aliphatic alkylating agent, said 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.

46. A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:

a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of: ##STR9##

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

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 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.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc