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Details for Patent: 8,436,017

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Details for Patent: 8,436,017

Title:Beta-2-adrenoreceptor agonists
Abstract: Compounds of formula ##STR00001## in free or salt or solvate form, where Ar is a group of formula ##STR00002## Y is carbon or nitrogen and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
Inventor(s): Cuenoud; Bernard (Horsham, GB), Bruce; Ian (Horsham, GB), Fairhurst; Robin Alec (Horsham, GB), Beattie; David (Horsham, GB)
Assignee: Novartis AG (Basel, CH)
Filing Date:Jul 23, 2012
Application Number:13/555,536
Claims:1. An inhalable pharmaceutical composition comprising: (a) (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quin- olin-2-one in free or salt or solvate form; (b) a steroid; and (c) a pharmaceutically acceptable carrier in inhalable form.

2. An inhalable pharmaceutical composition according to claim 1, that contains a daily dose of (a).

3. An inhalable pharmaceutical composition according to claim 2, in which the daily dose of (a) is from 1 .mu.g to 5000 .mu.g.

4. An inhalable pharmaceutical composition according to claim 3, which is a dry powder formulation.

5. An inhalable pharmaceutical composition according to claim 1, in which (a) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-- 1H-quinolin-2-one maleate.

6. An inhalable pharmaceutical composition according to claim 5, that contains a daily dose of (R)-5[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quino- lin-2-one maleate.

7. An inhalable pharmaceutical composition according to claim 6, in which the daily dose of (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quin- olin-2-one maleate is from 1 .mu.g to 5000 .mu.g.

8. An inhalable pharmaceutical composition according to claim 7, which is a dry powder formulation.

9. An inhalable pharmaceutical composition according to claim 1, in which (b) is steroid selected from the group consisting of budesonide, beclamethasone, fluticasone or mometasone.

10. An inhalable pharmaceutical composition according to claim 9, in which (b) is mometasone.

11. An inhalable pharmaceutical composition according to claim 1, in which (a) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quin- olin-2-one in free or salt or solvate form and (b) is mometasone.

12. An inhalable pharmaceutical composition according to claim 11, in which (a) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quin- olin-2-one maleate and (b) is mometasone.

13. An inhalable pharmaceutical composition according to claim 11, in which (a) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quin- olin-2-one acetate and (b) is mometasone.

14. An inhalable pharmaceutical composition according to claim 11, in which (a) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quin- olin-2-one 1-hydroxy-2-naphthoate and (b) is mometasone.

15. An inhalable pharmaceutical composition according to claim 11, which is a dry powder formulation.

16. An inhalable pharmaceutical composition according to any one of claims 12, 13 and 14, which is a dry powder formulation.

17. A method of treating a patient with an obstructive or inflammatory airways disease which comprises administering to the patient in need of such treatment an inhalable pharmaceutical composition according to claim 1.

18. A method of treating a patient according to claim 17, in which the obstructive or inflammatory airways disease is chronic obstructive pulmonary or airways disease.

19. A method of treating a patient according to claim 18, in which the obstructive or inflammatory airways disease is asthma.

20. A method of treating a patient with an obstructive or inflammatory airways disease which comprises administering to the patient in need of such treatment an inhalable pharmaceutical composition according to claim 11.
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