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Details for Patent: 6,432,953

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Details for Patent: 6,432,953

Title: Polymorphic form of a tachykinin receptor antagonist
Abstract:This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,1-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Inventor(s): Crocker; Louis (Belle Mead, NJ), McCauley; James (Belle Mead, NJ)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:May 07, 2001
Application Number:09/850,370
Claims:1. A method for the treatment or prevention of a disorder selected from: single episodic major depressive disorder, recurrent major depressive disorder, dysthymic disorder, bipolar disorder and cyclothymic disorder in a human in need thereof which comprises administering to the human an effective amount of a polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)pheny l-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine characterized by an X-ray powder diffraction pattern with key reflections at approximately: 12.0, 15.3, 16.6, 17.0, 17.6, 19.4, 20.0, 21.9, 23.6, 23.8, and 24.8.degree. (2 theta) which is substantially free of a polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phen yl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine characterized by an X-ray powder diffraction pattern with key reflections at approximately: 12.6, 16.7, 17.1, 17.2, 18.0, 20.1, 20.6, 21.1, 22.8, 23.9, and 24.8.degree. (2 theta).

2. The method of claim 1 wherein the disorder is single episodic major depressive disorder.

3. The method of claim 1 wherein the disorder is recurrent major depressive disorder.

4. The method of claim 1 wherein the disorder is dysthymic disorder.

5. The method of claim 1 wherein the disorder is bipolar disorder.

6. The method of claim 1 wherein the disorder is bipolar I disorder.

7. The method of claim 1 wherein the disorder is bipolar II disorder.

8. The method of claim 1 wherein the disorder is cyclothymic disorder.

9. A method for the treatment or prevention of a disorder selected from: panic disorder with agoraphobia, panic disorder without agoraphobia, agoraphobia without history of panic disorder, specific phobia, social phobia, obsessive-compulsive disorder, stress disorder and generalised anxiety disorder in a human in need thereof which comprises administering to the human an effective amount of a polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)pheny l-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine characterized by an X-ray powder diffraction pattern with key reflections at approximately: 12.0, 15.3, 16.6, 17.0, 17.6, 19.4, 20.0, 21.9, 23.6, 23.8, and 24.8.degree. (2 theta) which is substantially free of a polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phen yl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine characterized by an X-ray powder diffraction pattern with key reflections at approximately: 12.6, 16.7, 17.1, 17.2, 18.0, 20.1, 20.6, 21.1, 22.8, 23.9, and 24.8.degree. (2 theta).

10. The method of claim 9 wherein the disorder is panic disorder with agoraphobia.

11. The method of claim 9 wherein the disorder is panic disorder without agoraphobia.

12. The method of claim 9 wherein the disorder is agoraphobia without history of panic disorder.

13. The method of claim 9 wherein the disorder is specific phobia.

14. The method of claim 9 wherein the disorder is social phobia.

15. The method of claim 9 wherein the disorder is obsessive-compulsive disorder.

16. The method of claim 9 wherein the disorder is stress disorder.

17. The method of claim 9 wherein the stress disorder is post-traumatic stress disorder.

18. The method of claim 9 wherein the stress disorder is acute stress disorder.

19. The method of claim 9 wherein the disorder is generalised anxiety disorder.
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