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Last Updated: April 19, 2024

Details for Patent: 7,439,393


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Title:Phenethanolamine derivatives for treatment of respiratory diseases
Abstract: The invention relates to 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyet- hyl}-2-(hydroxymethyl)phenol; and salts and solvates thereof, including those which are pharmaceutically acceptable, along with formulations thereof, combinations thereof, and methods for the treatment or prophylaxis of mammals by administering such compounds.
Inventor(s): Box; Philip Charles (Stevenage, GB), Coe; Diane Mary (Stevenage, GB), Looker; Brian Edgar (Stevenage, GB), Mann; Inderjit Singh (Stevenage, GB), Procopiou; Panayiotis Alexandrou (Stevenage, GB)
Assignee: Glaxo Group Limited (Greenford, Middlesex, GB)
Filing Date:Dec 04, 2006
Application Number:11/566,346
Claims:1. A compound which is 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyet- hyl}-2-(hydroxymethyl)phenol; or a salt or solvate thereof.

2. A compound according to claim 1 wherein said salt or solvate is pharmaceutically acceptable.

3. A compound according to claim 1, wherein the salt is selected from the group consisting of a phenylcinnamate salt, a naphthoate salt, and a mandelate salt.

4. A pharmaceutical formulation comprising 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyet- hyl}-2-(hydroxymethyl)phenol or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or excipient, and optionally one or more other therapeutic ingredients.

5. A combination comprising a 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyet- hyl}-2-(hydroxymethyl)phenol or a pharmaceutically acceptable salt or solvate thereof, and one or more other therapeutic ingredients.

6. A combination according to claim 5 wherein the one or more other therapeutic ingredients is selected from the group consisting of a PDE4 inhibitor, a corticosteroid and an anti-cholinergic agent.

7. A combination according to claim 5 wherein the one or more other therapeutic ingredients is 6.alpha.,9.alpha.-difluoro-17.alpha.-[(2-furanylcarbonyl)oxy]-11.beta.-hy- droxy-16.alpha.-methyl-3-oxo-androsta-1,4-diene-17.beta.-carbothioic acid S-fluoromethyl ester.

8. A combination according to claim 5 wherein the one or more other therapeutic ingredients is 6,9-difluoro-11-hydroxy-16-methyl-17-[(4-methyl-1,3-thiazole-5-carbonyl)o- xy]-3-oxo-androsta-1,4-diene-17-carbothioic acid S-fluoromethyl ester.

9. A method for the treatment of a clinical condition in a mammal, for which a selective .beta..sub.2-adrenoreceptor agonist is indicated, which comprises administering a therapeutically effective amount of 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyet- hyl}-2-(hydroxymethyl)phenol, or a pharmaceutically acceptable salt or solvate thereof.

10. A method according to claim 9 wherein the mammal is a human.

11. A method according to claim 10 wherein the clinical condition is asthma.

12. A method according to claim 10 wherein the clinical condition is COPD.

13. A compound which is 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyet- hyl}-2-(hydroxymethyl)phenol-triphenyl acetate.

14. A pharmaceutical formulation comprising a compound according to claim 13, and a pharmaceutically acceptable carrier or excipient, and optionally one or more other therapeutic ingredients.

15. A combination comprising a compound according to claim 13, and one or more other therapeutic ingredients.

16. A combination according to claim 15 wherein the one or more therapeutic ingredients is selected from the group consisting of a PDE4 inhibitor, a corticosteroid, and an anti-cholinergic agent.

17. A combination according to claim 15 wherein the one or more therapeutic ingredients is 6.alpha.,9.alpha.-difluoro-17.alpha.-[(2-furanylcarbonyl)oxy]-11.beta.-hy- droxy-16.alpha.-methyl-3-oxo-androsta-1,4-diene-17.beta.-carbothioic acid S-fluoromethyl ester.

18. A combination according to claim 15 wherein the one or more therapeutic ingredients is 6,9-difluoro-11-hydroxy-16-methyl-17-[(4-methyl-1,3-thiazole-5-carbonyl)o- xy]-3-oxo-androsta-1,4-diene-17-carbothioic acid S-fluoromethyl ester.

19. A method for the treatment of a clinical condition in a mammal, for which a selective .beta..sub.2-adrenoreceptor agonist is indicated, which comprises administering a therapeutically effective amount of a compound according to claim 13.

20. A method according to claim 19 wherein the mammal is a human.

21. A method according to claim 20 wherein the clinical condition is asthma.

22. A method according to claim 20 wherein the clinical condition is COPD.

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