Claims
- 1. An iron uptake inhibitor comprising a tetra-positively charged porphyrin having the formula 5,10,15,20-tetrakis(1-alkyl-4-pyridyl)-21H,23H-porphine, wherein the alkyl is selected from the group consisting of methyl, ethyl, propyl, and butyl.
- 2. The iron uptake inhibitor of claim 1, wherein propyl is n-propyl or isopropyl.
- 3. The iron uptake inhibitor of claim 1, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 4. The iron uptake inhibitor of claim 1, wherein the porphyrin is a metal chelated porphyrin.
- 5. The iron uptake inhibitor of claim 4, wherein the metal chelated porphyrin is a metal chelate of a metal selected from the group consisting of Cu(II), Zn(II), Ni(II), Cr(III), Fe(III), Co(III), Ga(III), Eu(III), Mn(III), and Sn(IV).
- 6. The iron uptake inhibitor of claim 5, wherein propyl is n-propyl, or isopropyl.
- 7. The iron uptake inhibitor of claim 5, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 8. A therapeutic composition for treating a disorder or condition that may be treated by inhibiting heme-iron uptake in a mammal comprising a pharmaceutically-acceptable carrier and a tetra-positively charged porphyrin having the formula 5,10,15,20-tetrakis(1-alkyl-4-pyridyl)-21H,23H-porphine or a pharmaceutically acceptable salt thereof, wherein the alkyl is selected from the group consisting of methyl, ethyl, propyl, and butyl.
- 9. The therapeutic composition of claim 8, wherein propyl is n-propyl or isopropyl.
- 10. The therapeutic composition of claim 8, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 11. The therapeutic composition of claim 8, wherein the porphyrin is a metal chelated porphyrin.
- 12. The therapeutic composition of claim 11, wherein the metal chelated porphyrin is a metal chelate of a metal selected from the group consisting of Cu(II), Zn(II), Ni(II), Cr(III), Fe(III), Co(III), Ga(III), Eu(III), Mn(III), and Sn(IV).
- 13. The therapeutic composition of claim 12, wherein propyl is n-propyl or isopropyl.
- 14. The therapeutic composition of claim 12, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 15. The therapeutic composition of claim 8, wherein the tetra-positively charged porphyrin is provided as a pharmaceutically-acceptable salt.
- 16. The therapeutic composition of claim 15, wherein the pharmaceutically-acceptable salt is the product of a reaction of the tetra-positively charged porphyrin with a pharmaceutically-acceptable mineral or organic acid selected from the group consisting of hydrochloric acid, phosphoric acid, sulfuric acid, hydrobromic acid, hydroiodic acid, phosphorous acid, aliphatic mono and dicarboxylic acids, such as oxalic acid, carbonic acid, citric acid, succinic acid, phenyl-substituted alkanoic acids, aliphatic and aromatic sulfuric acids and the like.
- 17. The therapeutic composition of claim 15, wherein the pharmaceutically-acceptable salt is the product of a reaction of the tetra-positively charged porphyrins of the invention with a pharmaceutically acceptable organic base selected from the group consisting of: methylamine, ethylamine, ethanolamine, lysine, and ornithine.
- 18. The therapeutic composition of claim 15, wherein the counterion of the pharmaceutically-acceptable salt is chloride.
- 19. The therapeutic composition of claim 8, wherein the therapeutic composition is presented in a solid oral dosage form.
- 20. The therapeutic composition of claim 19, wherein the solid oral dosage form is selected from the group consisting of tablets, capsules, granules, and powders.
- 21. The therapeutic composition of claim 19, wherein the solid oral dosage form further includes a suitable carrier or excipient.
- 22. The therapeutic composition of claim 21, wherein the carrier or excipient is selected from the group consisting of starches, gelatin, sugars, acacia, microcrystalline cellulose, kaolin, sodium chloride, and alginic acid.
- 23. The therapeutic composition of claim 19, wherein the solid oral dosage form further includes a disintegrator agent.
- 24. The therapeutic composition of claim 23, wherein the disintegrator agent is selected from the group consisting of: microcrystalline cellulose, corn starch, sodium starch glycolate, and alginic acid.
- 25. The therapeutic composition of claim 19, wherein the solid oral dosage form further includes a binding agent.
- 26. The therapeutic composition of claim 25, wherein the binding agent is selected from the group consisting of acacia, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone (Povidone™), hydroxylpropyl methylcellulose, sucrose, starch, and ethylcellulose.
- 27. The therapeutic composition of claim 19, wherein the solid oral dosage form further includes a lubricant.
- 28. The therapeutic composition of claim 27, wherein the lubricant is selected from the group consisting of magnesium stearates, stearic acid, silicone fluid, talc, waxes, oils, and colloidal silica.
- 29. The therapeutic composition of claim 8, wherein the therapeutic composition is presented in a liquid oral dosage form.
- 30. The therapeutic composition of claim 29, wherein the liquid oral dosage form is selected from the group consisting of solutions, suspensions, and elixirs.
- 31. The therapeutic composition of claim 29, wherein the liquid oral dosage form further includes at least one pharmaceutical medium selected from the group consisting of water, glycols, oils, alcohols, wetting agents, flavoring agents, preservatives, and coloring agents.
- 32. The therapeutic composition of claim 30, wherein the liquid oral dosage form is a suspension.
- 33. The therapeutic composition of claim 32, wherein the suspension further includes a suspending agent.
- 34. The therapeutic composition of claim 33, wherein the suspending agent is selected from the group consisting of methylcellulose, alginates, tragacanth, pectin, kelgin, carrageenan, acacia, polyvinylpyrrolidone, and polyvinylalcohol.
- 35. The therapeutic composition of claim 8, presented in a granular form as part of a seasoning for food.
- 36. The therapeutic composition of claim 8, presented as a dressing or condiment for use with food.
- 37. The therapeutic composition of claim 8, presented as a beverage.
- 38. A method for inhibiting the absorption of iron in a human or a non-human mammal, comprising the step of administering a tetra-positively charged porphyrin having the formula 5,10,15,20-tetrakis(1-alkyl-4-pyridyl)-21H,23H-porphine, wherein the alkyl is selected from the group consisting of methyl, ethyl, propyl, and butyl; to a mammal in need of such treatment.
- 39. The method of claim 38, wherein propyl is n-propyl or isopropyl.
- 40. The method of claim 38, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 41. The method of claim 38, wherein the porphyrin is a metal chelated porphyrin.
- 42. The method of claim 41, wherein the metal chelated porphyrin is a metal chelate of a metal selected from the group consisting of Cu(II), Zn(II), Ni(II), Cr(II), Fe(III), Co(III), Ga(III), Eu(III), Mn(III), and Sn(IV).
- 43. The method of claim 42, wherein propyl is n-propyl or isopropyl.
- 44. The method of claim 42, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 45. A method of treating an iron-overload disease in a human or a non-human mammal, comprising the steps of administering a primary de-ironing treatment and administering a tetra-positively charged porphyrin having the formula 5,10,15,20-tetrakis(1-alkyl-4-pyridyl)-21H,23H-porphine, wherein the alkyl is selected from the group consisting of methyl, ethyl, propyl, and butyl; to the human or non-human mammal in need of such treatment.
- 46. The method of claim 45, wherein the primary de-ironing treatment is serial phlebotomy.
- 47. The method of claim 45, wherein the primary de-ironing treatment is chelation therapy conducted using a chelating agent.
- 48. The method of claim 47, wherein the chelating agent is deferoxamine.
- 49. The method of claim 45, wherein propyl is n-propyl or isopropyl.
- 50. The method of claim 45, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 51. The method of claim 45, wherein the porphyrin is a metal chelated porphyrin.
- 52. The method of claim 51, wherein the metal chelated porphyrin is a metal chelate of a metal selected from the group consisting of Cu(II), Zn(II), Ni(II), Cr(III), Fe(III), Co(III), Ga(III), Eu(III), Mn(III), and Sn(IV).
- 53. The method of claim 52, wherein propyl is n-propyl or isopropyl.
- 54. The method of claim 52, wherein butyl is n-butyl, isobutyl, or t-butyl.
- 55. The method of claim 52, wherein the porphyrin is a metal chelated porphyrin.
CROSS-REFERENCED RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Provisional Application No. 60/477,178, filed Jun. 10, 2003.
Provisional Applications (1)
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Number |
Date |
Country |
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60477178 |
Jun 2003 |
US |