SUBSTITUTED beta-DIKETONES AND THEIR USE

摘要

1. Compounds of general formula I wherein one of X1 and X2 is MeSO2 and the other one is halogen and X3 is hydrogen or halogen. 2. The compound of formula I wherein X1 is halogen, X2 is MeSO2 and X3 is hydrogen. 3. 3-{[3-Fluoro-4-(methylsulfonyl)-phenyl]methylene}-2,4-pentanedione. 4. 3-{[3-Cloro-4-(methylsulfonyl)-phenyl]methylene}-2,4-pentanedione. 5. 3-{[3-Bromo-4-(methylsulfonyl)-phenyl]methylene}-2,4-pentanedione. 6. 3-{[3,5-Dichloro-4-(methylsulfonyl)phenyl)methylene)-2,4-pentanedione. 7. 3-{[4-Chloro-3-(methylsulfonyl)phenyl)methylene)-2,4-pentanedione. 8. An inhalable pharmaceutical formulation containing a compound of formula I wherein one of X1 and X2 is MeSO2 and the other one is halogen and X3 is hydrogen or halogen, having about 100 % of its particle size below 10 μm, optionally in a suitable carrier or diluent. 9. The formulation according to claim 8, wherein the carrier is lactose. 10. The formulation according to claim 8, wherein it is a dry inhalation formulation. 11. Use of a compound of general formula I' wherein one of X1 and X2 is MeSO2 and the other one is hydrogen or halogen and X3 is hydrogen or halogen in the manufacture of a medicament for use in the prevention or treatment of respiratory diseases. 12. The use of claim 11, wherein the disease is asthma. 13. The use of claim 11, wherein the disease is steroid-resistant asthma. 14. The use of claim 11, wherein the disease is Acute Respiratory Distress Syndrome. 15. The use of claim 11, wherein the disease is chronic obstructive pulmonary disease. 16. The use of claim 11, wherein the compound is 3-[(4-methylsulfonylphenyl)methylene]-2,4-pentanedione. 17. The use of claim 11, wherein the compound is 3-[(3-chloro-4-methylsulfonylphenyl)methylene]-2,4-pentanedione. 18. An intermediate of formula II' wherein one of X1 and X2 is MeSO2 and the other one bromo or fluoro and X3 is hydrogen or halogen. 19. 3-Fluoro-4-methylsulfonylbenzaldehyde. 20. 3-Bromo-4-methylsulfonylbenzaldehyde.