Crosslinked polydiallymine copolymers for the treatment of type 2 diabetes
AssigneeGenzyme Corporation
InventorsPradeep K. Dhal, Robert J. Miller, Steven C. Polomoscanik, Philip Just Larsen, Thomas Huebschle, Thorsten Schmidt, Ian Davison, Peter D. McDonnell, Chinyere Agbugba
Life of this patent
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Abstract
Polydiallylamine copolymers are copolymers comprising monomers of polydiallylamine and either polyvinlyamine or polyallylamine. Polydiallylamine copolymers are often crosslinked. The polydiallyamine copolymers are useful as pharmaceutical compositions and may be used in the treatment of type 2 diabetes and for mitigating the complications of type 2 diabetes.
Claims7
A polydiallylamine block copolymer comprising a plurality of polymer chains, wherein each polymer chain is according to Formula (I):
- wherein:
- u, and v are each independently an integer from 0 to 200,000;
- and
- w is an integer from 1 to 200,000;
- A, B, C and D are each independently repeat units selected from Formula (II) or Formula (III);
- wherein Formula (II) is according to the structural formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- m is 0 or 1;
- n is an integer from 1 to 200,000;
- and Formula (III) is according to the structural formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- o is 0 or 1;
- p is an integer from 1 to 200,000;
- R1 and R2 and R3 and R4 are each independently selected from a group consisting of
- H, (C1-C10)alkyl, (C2-C9)heteroalkyl, (C3-C10)cycloalkyl,
- (C2-C9)heterocycloalkyl, (C6-C14)aryl, (C2-C9)heteroaryl,
- (C1-C10)alkylamine, —O(O)C—(C1-C10)alkyl, (C1-C10)alkyl-COOH,
- (C3-C10)cycloalkyl-COOH, —(O)CH3, —OH, amide,
- a guanidino group represented by Formula (A)
- wherein a is an integer from 0 to 25,
- a guanidinium chloride group represented by Formula (B),
- wherein b is an integer from 0 to 25,
- a guanidinobenzene group represented by Formula (C),
- wherein c is an integer from 0 to 25,
- a dihydroxy group, represented by Formula (D),
- wherein d is an integer from 0 to 25,
- a polyethylene glycol group, represented by Formula (E)
- wherein e is an integer from 1 to 400,
- a group represented by Formula (F)
- wherein Rz and Ry are each independently selected from the group consisting of H, (C1-C10)alkyl, (C2-C9)heteroalkyl,
- (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, (C6-C14)aryl,
- (C2-C9)heteroaryl, (C1-C10)alkylamine, —O(O)C-(C1-C10)alkyl,
- (C1-C10)alkyl-COOH, (C3-C10)cycloalkyl-COOH, —(O)CH3, —OH and
- amide,
- a group represented by Formula (G)
- wherein Rx and Rw are each independently selected from the group consisting of H, (C1-C10)alkyl, (C2-C9)heteroalkyl,
- (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, (C6-C14)aryl,
- (C2-C9)heteroaryl, (C1-C10)alkylannine, —O(O)C—(C1-C10)alkyl,
- (C1-C10)alkyl-COOH, (C3-C10)cycloalkyl-COOH, —(O)CH3, cyano, cyano(C1-C10)alkyl, —OH and
- amide,
- and a point of attachment to another repeat unit of the copolymer;
- and wherein:
- (a) each polymer chain must be cross-linked with at least one other polymer chain, and
- (b) each polymer chain may be internally cross-linked;
- and
- wherein the molar ratio of Formula (II) monomer:Formula (III) monomer in the polydiallylamine copolymer is from 99:1 to 1:99, and the ratio of cross-linked repeat units:un-cross-linked repeat units is from 1:99 to 50:50.
Dependencies are inferred from the claim text.