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Claims for Patent: 6,096,742

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Claims for Patent: 6,096,742

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)-(3,5-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)
Application Number:09/212,511
Patent Claims: 1. 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. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)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: 12.0, 15.3, 16.6, 17.0, 17.6, 19.4, 20.0, 21.9, 23.6, 23.8, and 24.8.degree. (2 theta) and 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).

3. A method for antagonizing the effect of substance P at its receptor site or for the blockade of neurokinin-1 receptors in a mammal which comprises administering to the mammal the polymorphic form of claim 1 in an amount that is effective for antagonizing the effect of substance P at its receptor site or for the blockade of neurokinin-1 receptors in the mammal.

4. A method for the treatment or prevention of emesis in a mammal in need thereof which comprises administering to the mammal an effective amount of the polymorphic form of claim 1.

5. A method for the treatment or prevention of depression in a human in need thereof which comprises administering to the human an effective amount of the polymorphic form of claim 1.

6. A method for the treatment or prevention of anxiety in a human in need thereof which comprises administering to the human an effective amount of the polymorphic form of claim 1.

7. A method for the treatment or prevention of psychosis in a human in need thereof which comprises administering to the human an effective amount of the polymorphic form of claim 1.

8. A method for the treatment or prevention of schizophrenia in a human in need thereof which comprises administering to the human an effective amount of the polymorphic form of claim 1.
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