Claims
- 1. A polymer conjugate of artelinic acid comprising a water soluble and non-peptidic polymer backbone having at least one terminus bonded to the following structure:
- 2. The polymer conjugate of claim 1, wherein the polymer backbone is selected from the group consisting of poly(alkylene glycol), poly(oxyethylated polyol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxypropylmethacrylamide), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, poly(N-acryloylmorpholine), and copolymers, terpolymers, and mixtures thereof.
- 3. The polymer conjugate of claim 1, wherein the polymer backbone is poly(ethylene glycol).
- 4. The polymer conjugate of claim 3, wherein the poly(ethylene glycol) has an average molecular weight from about 200 Da to about 100,000 Da.
- 5. The polymer conjugate of claim 1, wherein Z is O or NH.
- 6. The polymer conjugate of claim 1, wherein the polymer backbone has about 2 to about 300 termini.
- 7. The polymer conjugate of claim 1, having the following structure:
- 8. The polymer conjugate of claim 7, wherein POLY is selected from the group consisting of poly(alkylene glycol), poly(oxyethylated polyol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxypropylmethacrylamide), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, poly(N-acryloylmorpholine), and copolymers, terpolymers, and mixtures thereof.
- 9. The polymer conjugate of claim 7, wherein POLY is poly(ethylene glycol).
- 10. The polymer conjugate of claim 9, wherein the poly(ethylene glycol) has an average molecular weight from about 200 Da to about 100,000 Da.
- 11. The polymer conjugate of claim 7, wherein Z is O or NH.
- 12. The polymer conjugate of claim 7, wherein X is selected from the group consisting of alkoxy, hydroxyl, protected hydroxyl, active ester, active carbonate, acetal, aldehyde, aldehyde hydrates, alkenyl, acrylate, methacrylate, acrylamide, active sulfone, amine, protected amine, hydrazide, protected hydrazide, thiol, protected thiol, carboxylic acid, protected carboxylic acid, isocyanate, isothiocyanate, maleimide, vinylsulfone, dithiopyridine, vinylpyridine, iodoacetamide, epoxide, glyoxals, diones, mesylates, tosylates, and tresylate.
- 13. The polymer conjugate of claim 7, wherein X has the structure:
- 14. The polymer conjugate of claim 13, wherein Z′ is O or NH.
- 15. The polymer conjugate of claim 1, having the structure:
- 16. The polymer conjugate of claim 15, wherein n is about 3 to about 20.
- 17. The polymer conjugate of claim 15, wherein each Y and Z are independently selected from the group consisting of O and NH.
- 18. The polymer conjugate of claim 15, wherein R is derived from a molecule selected from the group consisting of polyols, polyamines, and molecules having a combination of alcohol and amine groups.
- 19. The polymer conjugate of claim 15, wherein R is derived from a molecule selected from the group consisting of glycerol, glycerol oligomers, pentaerythritol, sorbitol, and lysine.
- 20. The polymer conjugate of claim 15, wherein POLY is selected from the group consisting of poly(alkylene glycol), poly(oxyethylated polyol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxypropylmethacrylamide), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, poly(N-acryloylmorpholine), and copolymers, terpolymers, and mixtures thereof.
- 21. The polymer conjugate of claim 15, wherein POLY is poly(ethylene glycol).
- 22. The polymer conjugate of claim 21, wherein the poly(ethylene glycol) has an average molecular weight from about 200 Da to about 100,000 Da.
- 23. The polymer conjugate of claim 15, having the structure:
- 24. The polymer conjugate of claim 15, having the structure:
- 25. A method of forming a polymer conjugate of artelinic acid, comprising:
providing a water soluble and non-peptidic polymer backbone having at least one terminus bonded to a functional group reactive with a carboxylic acid group; and reacting the polymer backbone with artelinic acid to form a polymer conjugate of artelinic acid.
- 26. The method of claim 25, wherein the functional group is selected from the group consisting of hydroxyl and amine.
- 27. The method of claim 25, wherein said reacting step comprises reacting the polymer backbone with artelinic acid in the presence of a catalytic amount of N,N-dimethylaminopyridine.
- 28. The method of claim 25, wherein the polymer backbone is selected from the group consisting of poly(alkylene glycol), poly(oxyethylated polyol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxypropylmethacrylamide), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, poly(N-acryloylmorpholine), and copolymers, terpolymers, and mixtures thereof.
- 29. The method of claim 25, wherein the polymer backbone is poly(ethylene glycol).
- 30. The method of claim 29, wherein the poly(ethylene glycol) has an average molecular weight from about 200 Da to about 100,000 Da.
- 31. A method of treating malaria in a mammal, the method comprising administering to the mammal an effective amount of a polymer conjugate of artelinic acid comprising a water soluble and non-peptidic polymer backbone having at least one terminus bonded to the following structure:
- 32. The method of claim 31, wherein the polymer backbone is selected from the group consisting of poly(alkylene glycol), poly(oxyethylated polyol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxypropylmethacrylamide), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, poly(N-acryloylmorpholine), and copolymers, terpolymers, and mixtures thereof.
- 33. The method of claim 31, wherein the polymer backbone is poly(ethylene glycol).
- 34. The method of claim 33, wherein the poly(ethylene glycol) has an average molecular weight from about 200 Da to about 100,000 Da.
- 35. The method of claim 31, wherein Z is O or NH.
- 36. The method of claim 31, wherein the polymer backbone has about 2 to about 300 termini.
- 37. The method of claim 31, wherein said administering step comprises administering the compound subcutaneously, transdermally, intravenously, orally, or by inhalation.
- 38. The method of claim 31, wherein said administering step comprises administering the compound in the form of a hydrogel.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Provisional Application No. 60/185,544, filed Feb. 28, 2000, which is incorporated by reference herein in its entirety.
Provisional Applications (1)
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Number |
Date |
Country |
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60185544 |
Feb 2000 |
US |