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Last Updated: April 19, 2024

Details for Patent: 7,750,023


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Title:Quinuclidine derivatives and medicinal compositions containing the same
Abstract: The invention provides 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo- [2.2.2]octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders, in association with .beta..sub.2 agonist.
Inventor(s): Fernandez Forner; Maria Dolors (Barcelona, ES), Prat Quinones; Maria (Barcelona, ES), Buil Albero; Maria Antonia (Barcelona, ES)
Assignee: Almirall, S.A. (N/A)
Filing Date:Mar 07, 2008
Application Number:12/074,929
Claims:1. A pharmaceutical composition comprising: (i) 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo- [2.2.2]octane, wherein an anion X.sup.- is associated with the positive charge of the nitrogen atom and wherein X.sup.- is a pharmaceutically acceptable anion of a mono- or polyvalent acid; and (ii) a .beta..sub.2 agonist.

2. The composition of claim 1 comprising 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo- [2.2.2]octane bromide.

3. The composition of claim 1 in admixture with a pharmaceutically acceptable carrier or diluent.

4. The composition of claim 3 comprising 3(S)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicy- clo[2.2.2]octane, wherein an anion X.sup.- is associated with the positive charge of the nitrogen atom and wherein X.sup.- is a pharmaceutically acceptable anion of a mono- or polyvalent acid.

5. The composition of claim 4 comprising 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicy- clo[2.2.2]octane, wherein an anion X.sup.- is associated with the positive charge of the nitrogen atom and wherein X.sup.- is a pharmaceutically acceptable anion of a mono- or polyvalent acid.

6. The composition of claim 1 wherein the pharmaceutical composition is suitable for inhalation.

7. The pharmaceutical composition according to claim 1 further comprising a steroid or phosphodiesterase IV inhibitor.

8. A method for treating chronic obstructive pulmonary disease, chronic bronchitis, bronchial hyperreactivity, asthma, or rhinitis which method comprises administering to a human or animal patient in need of such treatment an effective amount of: (i) 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo- [2.2.2]octane, wherein an anion X.sup.- is associated with the positive charge of the nitrogen atom and wherein X.sup.- is a pharmaceutically acceptable anion of a mono- or polyvalent acid; and (ii) a .beta..sub.2 agonist.

9. The method according to claim 8, wherein the anion X.sup.- is Br.sup.-.

10. The method of claim 8 comprising administering an effective amount of 3(S)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicy- clo[2.2.2]octane, wherein an anion X.sup.- is associated with the positive charge of the nitrogen atom and wherein X.sup.- is a pharmaceutically acceptable anion of a mono- or polyvalent acid.

11. The method of claim 10 comprising administering an effective amount of 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniab- icyclo[2.2.2]octane, wherein an anion X.sup.- is associated with the positive charge of the nitrogen atom and wherein X.sup.- is a pharmaceutically acceptable anion of a mono- or polyvalent acid.

12. The method of claim 8 wherein administration is by inhalation.

13. The method of claim 8 comprising administering an effective amount of a steroid or phosphodiesterase IV inhibitor.

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