Functionalized Water-Soluble Polyphosphazenes and Uses Thereof as Modifiers of Biological Agents

• US 20150306228A1
• Filed: 07/09/2015
• Published: 10/29/2015
• Est. Priority Date: 04/13/2004
• Status: Abandoned Application

• Current Assignee: Alexander K. Andrianov
• Original Assignee: Alexander K. Andrianov
• Inventors: Andrianov, Alexander K.
• Application Number:
  US14/795,425
• Publication Number:
  US 20150306228A1
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/795 Polymers containing sulfur
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C08G 79/025 Polyphosphazenes

Abstract

A polyphosphazene polymer which includes hydrophilic side groups and interacting side groups which are capable of bonding with a biological agent of interest. The bonding may be by non-covalent bonding.

Claims

1. A polyphosphazene polymer having the following structural formula:

2. The polymer of claim 1 wherein R₁ has a structural formula selected from the group consisting of:

3. The polymer of claim 2 wherein R₁ has the formula:

-A-(B₁)x-(C₁)y-(B₂)z,

and C₁ is alkyleneoxy.

4. The polymer of claim 3 wherein A is nitrogen.

5. The polymer of claim 3 wherein A is oxygen.

6. The polymer of claim 3 wherein C₁ is methyleneoxy.

7. The polymer of claim 3 wherein C₁ is ethyleneoxy.

8. The polymer of claim 3 wherein x is 0 and z is 1.

9. The polymer of claim 3 wherein x is 1 and z is 1.

10. The polymer of claim 2 wherein R₁ has the formula:

-A-(B₁)x-(C₁)y-(B₂)z,

and C₁ is a substituted or unsubstituted heterocyclic group.

11. The polymer of claim 10 wherein C₁ has the following structural formula:

wherein q is from 1 to 5.

12. The polymer of claim 10 wherein x is 1 and z is 0.

13. The polymer of claim 10 wherein C₁ has the following structural formula:

14. The polymer of claim 10 wherein A is oxygen.

15. The polymer of claim 10 wherein A is nitrogen.

16. The polymer of claim 1 wherein R₂ includes (i) an ionic moiety or an ionizable moiety, (ii) a hydrophobic moiety, or (iii) a hydrogen bond forming moiety.

17. The polymer of claim 16 wherein R₂ includes an ionic moiety or an ionizable moiety.

18. The polymer of claim 17 wherein said ionic moiety or ionizable moiety is selected from the group consisting of carboxylic acid moieties, sulfonic acid moieties, sulfate moieties, amino moieties, and salts thereof.

19. The polymer of claim 18 wherein said ionic moiety or ionizable moiety is a carboxylic acid moiety.

20. The polymer of claim 18 wherein said ionic moiety or ionizable moiety is a sulfonic acid moiety.

21. The polymer of claim 18 wherein said ionic moiety or ionizable moiety is an amino moiety.

22. The polymer of claim 1 wherein at least a portion of said R groups are biodegradable side groups R₃.

23. The polymer of claim 22 wherein said biodegradable side groups R₃ are selected from the group consisting of chlorine, amino acids, amino acid esters, imidazolyl groups, glycinyl groups, glyceryl groups, glucosyl groups, and ethoxy groups.

24. The polymer of claim 1 wherein at least a portion of said R groups are targeting side groups R₄.

25. The polymer of claim 24 wherein said targeting side groups R₄ are selected from the group consisting of antibodies, lectins, triantennary glycosides, tetraantennary glycosides and transferrin.

26. A composition, comprising:

the polyphosphazene polymer of claim 1; and

at least one biological agent of interest.

27. The composition of claim 26 wherein the molar ratio of said polyphosphazene polymer to said at least one biological agent in said composition is from about 1:

10 to about 10;

1.

28. The composition of claim 27 wherein the molar ratio said polyphosphazene polymer to said at least one biological agent in said composition is about 1:

1.

29. The polymer of claim 1 wherein at least 80 mole % of the R groups are R₁ groups.