AMIDO-AMINE POLYMER COMPOSITIONS

• US 20120237470A1
• Filed: 03/12/2012
• Published: 09/20/2012
• Est. Priority Date: 12/14/2006
• Status: Active Grant

• Current Assignee: Genzyme Corporation (Sanofi )
• Original Assignee: Genzyme Corporation (Sanofi )
• Inventors: Dhal, Pradeep K., Holmes-Farley, Stephen Randall, Huval, Chad C.
• Granted Patent: US 8,889,738 B2
• Time in Patent Office: Days
• US Class Current: 424/78.01
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/23 of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• CPC Class Codes: A61K 31/785 Polymers containing nitrogen
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 13/12 of the kidneys
• CPC Class Codes: A61P 3/12 for electrolyte homeostasis

Abstract

Compounds, polymers, crosslinked polymers and pharmaceutical compositions comprising the same may be derived from multi-amine monomers and multi-functional monomers having two or more amine reactive groups. Such compounds, polymers, crosslinked polymers and compositions may be used to treat hyperphosphatemia or to remove ions from the gastrointestinal tract of animals, including humans.

Claims

1-43. -43. (canceled)

44. A method of removing a compound or ion from the gastrointestinal tract of an animal comprising administering an effective amount of a pharmaceutical composition comprising:

a) a copolymer derived from compounds according to the following Formulas I and II;

49. The method of claim 44, wherein said copolymer has a degree of branching of from 0.10 to 0.95.

50. The method of claim 44, wherein from 10-95% of the nitrogen atoms in the copolymer are the nitrogen in a secondary amine moiety.

51. The method of claim 44, wherein said copolymer has a polydispersity greater than about 1.2.

52. The method of claim 44, wherein the intrinsic viscosity of said branched copolymer has no maximum (versus viscosity averaged molecular weight).

53. The method of claim 44, wherein said copolymer has random, variable length branching.

54. The method of claim 44, wherein the compound according to Formula I is selected from the group consisting of:

55. The method of claim 44, wherein the compound according to Formula I is selected from the group consisting of:

56. The method of claim 44, wherein the compound according to Formula II is selected from the group consisting of:

45. A method of removing a compound or ion from the gastrointestinal tract of an animal comprising administering an effective amount of a pharmaceutical composition comprising:

a) a hyperbranched copolymer derived from;

(i) a multi-amine monomer; and

(ii) a multifunctional monomer comprising two or more amine-reactive groups; and

b) a pharmaceutically acceptable excipient.

47. The method of claim 45, wherein the amine reactive groups are independently selected from the group consisting of vinyl groups, carboxylic acid groups, ester groups and/or combinations thereof.

48. The method of claim 45, wherein the multifunctional monomer is selected from the group consisting of:

57. The method of claim 45, wherein the multi-amine is selected from the group consisting of:

46. A method of removing a compound or ion from the gastrointestinal tract of an animal comprising administering a pharmaceutical composition comprising:

a) a copolymer comprising

i) at least one multi-amine or residue thereof; and

ii) at least one ester or multi-ester or residue thereof;

wherein said copolymer has a degree of branching of from 0.10 to 0.95; and

b) a pharmaceutically acceptable excipient.

58. The method of claim 46, wherein the multi-ester is selected from the group consisting of: