Mammalian metabolites of a tachykinin receptor antagonist
AssigneeMerck & Co., Inc.
InventorsSu-er Wu Huskey, Shuet-Hing Lee Chiu
Life of this patent
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Abstract
This invention is concerned with mammalian metabolites of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist that is useful in the prevention and treatment of certain disorders, including emesis and psychiatric disorders such as depression and anxiety.
Claims11
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 the administration to the mammal of a mammalian metabolite of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in an amount that is effective for antagonizing the effect of substance P at its receptor site in the mammal.
A method of treating or preventing depression in a mammal in need thereof which comprises the administration to the mammmal of an effective amount of a mammalian metabolite of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine.
A method of treating or preventing anxiety in a mammal in need thereof which comprises the administration to the mammmal of an effective amount of a mammalian metabolite of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine.
A method for the treatment or prevention of emesis in a mammal in need thereof which comprises the administration to the mammal of an effective amount of a mammalian metabolite of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)-methylmorpholine.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a mammalian metabolite of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)-methylmorpholine.
A compound which is selected from the group consisting of:
- 12 13 14 15 16 17 18
- and pharmaceutically acceptable salts and individual diasteromers thereof.
Dependencies are inferred from the claim text.