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Claims for Patent: 6,537,983

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Claims for Patent: 6,537,983

Title: Anti-inflammatory androstane derivatives
Abstract:According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), ##STR1## wherein R.sub.1 represents C.sub.1-6 alkyl or C.sub.1-6 haloalkyl; R.sub.2 represents --C(.dbd.O)-aryl or --C(.dbd.O)-heteroaryl; R.sub.3 represents hydrogen, methyl (which may be in either the .alpha. or .beta. configuration) or methylene; R.sub.4 and R.sub.5 are the same or different and each represents hydrogen or halogen; and ----- represents a single or a double bond; and salts and solvates thereof together with a long-acting .beta..sub.2 -adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.
Inventor(s): Biggadike; Keith (Stevenage, GB), Jones; Paul Spencer (Stevenage, GB), Payne; Jeremy John (Stevenage, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:10/066,961
Patent Claims: 1. A pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), ##STR25##

wherein R.sub.1 represents C.sub.1-6 alkyl or C.sub.1-6 haloalkyl; R.sub.2 represents --C(.dbd.O)-aryl or --C(.dbd.O)-heteroaryl; R.sub.3 represents hydrogen, methyl (which may be in either the .alpha. or .beta. configuration) or methylene; R.sub.4 and R.sub.5 are the same or different and each represents hydrogen or halogen; and ----- represents a single or a double bond;

or a salt or solvate thereof, together with a long-acting .beta..sub.2 -adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.

2. A pharmaceutical formulation according to claim 1 wherein the compound of formula (I) or a solvate thereof and the long-acting .beta..sub.2 -adrenoreceptor agonist are both present in particulate form.

3. A pharmaceutical formulation according to claim 2 further comprising a particulate carrier.

4. A pharmaceutical formulation according to claim 3 wherein the carrier is lactose.

5. A pharmaceutical formulation according to claim 1 further comprising a liquified propellant gas.

6. A pharmaceutical formulation according to claim 2 further comprising a liquified propellant gas.

7. A pharmaceutical formulation according to claim 1 wherein the inflammatory disorder of the respiratory tract is asthma.

8. A method of treatment of a inflammatory disorder of the respiratory tract once-per-day which comprises administration of a pharmaceutical formulation according to claim 1.

9. A method of treatment according to claim 8 wherein the inflammatory disorder of the respiratory tract is asthma.

10. An inhaler containing a plurality of doses of a pharmaceutical formulation comprising a compound of formula (I) ##STR26##

wherein R.sub.1 represents C.sub.1-6 alkyl or C.sub.1-6 haloalkyl; R.sub.2 represents --C(.dbd.O)-aryl or --C(.dbd.O)-heteroaryl; R.sub.3 represents hydrogen, methyl (which may be in either the .alpha. or .beta. configuration) or methylene; R.sub.4 and R.sub.5 are the same or different and each represents hydrogen or halogen; and ----- represents a single or a double bond;

or a salt or solvate thereof, together with a long-acting .beta..sub.2 -adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more, and which doses are suitable for once-per-day administration of the formulation by inhalation.

11. An inhaler according to claim 10 wherein the compound of formula (I) or a solvate thereof and the long-acting .beta..sub.2 -adrenoreceptor agonist are both present in particulate form.

12. An inhaler according to claim 11 wherein the formulation further comprises a particulate carrier.

13. An inhaler according to claim 12 wherein the carrier is lactose.

14. An inhaler according to claim 10 wherein the formulation further comprises a liquefied propellant gas.

15. An inhaler according to claim 11 wherein the formulation further comprises a liquefied propellant gas.

16. An inhaler containing a plurality of doses of a pharmaceutical formulation comprising a particulate compound of formula (I) ##STR27##

wherein R.sub.1 represents C.sub.1-6 alkyl or C.sub.1-6 haloalkyl; R.sub.2 represents --C(.dbd.O)-aryl or --C(.dbd.O)-heteroaryl; R.sub.3 represents hydrogen, methyl (which may be in either the .alpha. or .beta. configuration) or methylene; R.sub.4 and R.sub.5 are the same or different and each represents hydrogen or halogen; and ----- represents a single or a double bond;

or a salt or solvate thereof, together with a long-acting .beta..sub.2 -adrenoreceptor, a particulate long-acting .beta..sub.2 -adrenoreceptor agonist and a carrier each drug being present in an amount adequate to provide a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more following once-per-day dosing by inhalation.

17. An inhaler according to claim 10 wherein wherein the inflammatory disorder of the respiratory tract is asthma.

18. An inhaler according to claim 16 wherein wherein the inflammatory disorder of the respiratory tract is asthma.

19. A formulation according to claim 1 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

20. A formulation according to claim 2 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

21. A formulation according to claim 3 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

22. A formulation according to claim 4 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

23. A formulation according to claim 5 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

24. A formulation according to claim 6 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

25. A formulation according to claim 7 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

26. A method according to claim 8 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

27. A method according to claim 9 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

28. An inhaler according to claim 10 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

29. An inhaler according to claim 11 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

30. An inhaler according to claim 12 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-triiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-car bothioic acid S-fluoromethyl ester or a salt or solvate thereof.

31. An inhaler according to claim 13 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

32. An inhaler according to claim 14 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

33. An inhaler according to claim 15 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

34. An inhaler according to claim 16 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

35. An inhaler according to claim 17 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.

36. An inhaler according to claim 18 wherein the compound of formula (I) is 6.alpha.,9.alpha.-Difluoro-11.beta.-hydroxy-16.alpha.-methyl-17.alpha.-[(4 -methyl-1,3-thiazole-5-carbonyl)oxy]-3-oxo-androsta-1,4-diene-17.beta.-carb othioic acid S-fluoromethyl ester or a salt or solvate thereof.
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