USRE37534EExpiredUtilityPatentIndex 73
Pharmaceutical compositions

Assignee: BTG INT LTDPriority: Oct 22, 1982Filed: Jan 31, 1997Granted: Jan 29, 2002
Est. expiryOct 22, 2002(expired)· nominal 20-yr term from priority
Inventors:HIDER ROBERT C KONTOGHIORGHES GEORGE STOCKHAM MICHAEL A
A61K 33/26C07D 309/40A61K 31/35
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Claims
Abstract

Pharmaceutical compositions containing an iron complex of 3-hydroxy-4-pyrone or of a 3-hydroxy-4-pyrone in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by an aliphatic hydrocarbon group of 1 to 6 carbon atoms, are of value for the treatment of iron deficiency anaemia.
Claims

exact text as granted — not AI-modified
We clam:  
     
       1. A pharmaceutical composition comprising a compound being a tissue permeable, neutral 3:1 hydroxypyrone:iron(III) complex of 3-hydroxy-4-pyrone or of a 3-hydroxy-4-pyrone in which at least one of the hydrogen atoms attached to ring carbon atoms is replaced by an aliphatic hydrocarbon group of 1 to 6 carbon atoms, wherein said complex is encapsulated by a material resistant to dissociation under aqueous acidic conditions. 
     
     
       2. A pharmaceutical composition according to  claim 1 , in which the iron complex is encapsulated by a solid material which is resistant to dissociation under acidic aqueous conditions but which is adapted for dissociation under non-acidic aqueous conditions. 
     
     
       3. A pharmaceutical composition according to  claim 2  in capsule form. 
     
     
       4. A pharmaceutical composition according to  claim 2 , in which each aliphatic hydrocarbon group is an acyclic group of 1 to 4 carbon atoms. 
     
     
       5. A pharmaceutical composition according to  claim 2 , in which each aliphatic hydrocarbon group is an alkyl group. 
     
     
       6. A pharmaceutical composition according to  claim 2 , in which the compound is an iron complex of a 3l-hydroxy-4-pyrone in which at least one of the hydrogen atoms attached to ring carbon atoms is replaced by a substituent selected from the group consisting of methyl, ethyl, n-propyl and isopropyl. 
     
     
       7. A pharmaceutical composition according to  claim 6 , in which each substituent is a methyl group. 
     
     
       8. A pharmaceutical composition according to  claim 6 , in which the substituted 3-hydroxy-4-pyrone has a single substituent at the 2- or 6-position. 
     
     
       9. A pharmaceutical composition according to  claim 2 , in which the compound is the 3:1 iron complex of 3-hydroxy-4-pyrone, 3-hydroxy-2-methyl-4-pyrone, 3-hydroxy-6-methyl-4-pyrone or 2-ethyl-3-hydroxy-4-pyrone. 
     
     
       10. A pharmaceutical composition according to  claim 2 , in which the compound is the 3:1 iron complex of 3-hydroxy-2-methyl-4-pyrone. 
     
     
       11. A pharmaceutical composition according to  claim 2 , in which the compound is the 3:1 iron complex of 2-ethyl-3-hydroxy-4-pyrone. 
     
     
       12. A pharmaceutical composition according to  claim 2 , in which the neutral 3:1 complex is substantially free from complexes containing other proportions of the hydroxypyrone and iron(III). 
     
     
       13. A pharmaceutical composition according to  claim 2 , in which the iron complex is in substantially pure form. 
     
     
       14. A pharmaceutical composition according to  claim 2  which additionally contains an iron chelating agent. 
     
     
       15. A pharmaceutical composition according to  claim 14 , in which the iron chelating agent is uncomplexed 3-hydroxy-4-pyrone or an uncomplexed 3-hydroxy-4-pyrone in which at least one of the hydrogen atoms attached to ring carbon atoms is replaced by an aliphatic hydrocarbon group of 1 to 6 carbon atoms, or a salt thereof containing a physiologically acceptable cation. 
     
     
       16. A pharmaceutical composition according to  claim 15 , which contains a complexed hydroxypyrone together with the same hydroxypyrone or a salt thereof in uncomplexed form. 
     
     
       17. A pharmaceutical composition according to  claim 16 , which comprises the 3:1 iron complex of 3-hydroxy-2-methyl-4-pyrone and uncomplexed 3-hydroxy-2-methyl-4-pyrone or a salt thereof containing a physiologically acceptable cation. 
     
     
       18. A pharmaceutical composition according to  claim 2  which additionally contains folic acid. 
     
     
       19. A method for the treatment of a patient to effect an increase in the level of iron in the patient&#39;s bloodstream, which comprises administering to said patient in need thereof a composition according to  claim 1 , in an amount which is effective to achieve said increase. 
     
     
       20. A method for the treatment of a patient to effect an increase in the level of iron in the patient&#39;s bloodstream, which comprises administering to said patient in need thereof a composition according to  claim 2 , in an amount which is effective to achieve said increase. 
     
     
       21. A method according to  claim 20 , in which the compound is the 3:1 iron complex of a 3-hydroxy-4-pyrone, 3-hydroxy-2-methyl-4-pyrone, 3 hydroxy-6-methyl-4-pyrone or 2-ethyl-3-hydroxy-pyrone. 
     
     
       22. A method according to  claim 20  in which the compound is the 3:1 iron complex of 3-hydroxy-2-methyl-4-pyrone. 
     
     
       23. A method for the treatment of a patient to effect an increase in the level of iron in the patient&#39;s bloodstream which comprises administering to said patient in need thereof a compound being a  2 : 1  hydroxypyrone:iron (III) complex of  3 -hydroxy- 4 -pyrone or of a  3 -hydroxy- 4 -pyrone in which at least one of the hydrogen atoms attached to the ring carbon atoms is replaced by an aliphatic hydrocarbon group of  1  to  6  carbon atoms, in an amount which is effective to achieve said increase. 
     
     
       24. A method according to  claim 23 , in which each aliphatic hydrocarbon group is an acyclic group of  1  to  4  carbon atoms. 
     
     
       25. A method according to  claim 23 , in which each aliphatic hydrocarbon group is an alkyl group. 
     
     
       26. A method according to  claim 23 , in which the compound is an iron complex of a  3 -hydroxy- 4 -pyrone in which at least one of the hydrogen atoms attached to ring carbon atoms is replaced by a substituent selected from the group consisting of methyl, ethyl, n-propyl and isopropyl. 
     
     
       27. A method according to  claim 23 , in which each substituent is a methyl group. 
     
     
       28. A method according to  claim 23 , in which the substituted  3 -hydroxy- 4 -pyrone has a single substituent at the  2 - or  6 -position. 
     
     
       29. A method according to  claim 23 , in which the compound is a  2 : 1  iron complex of  3 -hydroxy- 4 -pyrone,  3 -hydroxy- 3 -methyl- 4 -pyrone,  3 -hydroxy- 6 -methyl- 4 -pyrone or  2 -ethyl- 3 -hydroxy- 4 -pyrone. 
     
     
       30. A method according to  claim 23 , in which the compound is a  2 : 1  iron complex of  3 -hydroxy- 2 -methyl- 4 -pyrone. 
     
     
       31. A method according to  claim 23 , in which the compound is a  2 : 1  iron complex of  2 -ethyl- 3 -hydroxy- 4 -pyrone. 
     
     
       32. A method for the treatment of a patient to effect an increase in the level of iron in the patient&#39;s bloodstream, which comprises administering to said patient in need thereof a compound being a  1 : 1  hydroxypyrone:iron (III) complex of  3 -hydroxy- 4 -pyrone or of a  3 -hydroxy- 4 -pyrone in which at least one of the hydrogen atoms attached to ring carbon atoms is replaced by an aliphatic hydrocarbon group of  1  to  6  carbon atoms, in an amount which is effective to achieve said increase. 
     
     
       33. A method according to  claim 32  in which each aliphatic hydrocarbon group is an acyclic group of  1  to  4  carbon atoms. 
     
     
       34. A method according to  claim 32 , in which each aliphatic hydrocarbon group is an alkyl group. 
     
     
       35. A method according to  claim 32 , in which the compound is an iron complex of a  3 -hydroxy- 4 -pyrone in which at least one of the hydrogen atoms attached to ring carbon atoms is replaced by a substituent selected from the group consisting of methyl, ethyl, n-propyl and isopropyl. 
     
     
       36. A method according to  claim 32 , in which each substituent is a methyl group. 
     
     
       37. A method according to  claim 32 , in which the substituted  3 -hydroxy- 4 -pyrone has a single substituent at the  2 - or  6 -position. 
     
     
       38. A method according to  claim 32 , in which the compound is a  1 : 1  iron complex of  3 -hydroxy- 4 -pyrone,  3 -hydroxy- 2 -methyl- 4 -pyrone,  3 -hydroxy- 6 -methyl- 4  -pyrone or  2 -ethyl- 3 -hydroxy- 4 -pyrone. 
     
     
       39. A method according to  claim 32 , in which the compound is a  1 : 1  iron complex of  3 -hydroxy- 2 -methyl- 4 -pyrone. 
     
     
       40. A method according to  claim 32 , in which the compound is  1 : 1  iron complex of  2 -ethyl- 3 -hydroxy- 4 -pyrone.
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