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Claims for Patent: 6,235,735

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Claims for Patent: 6,235,735

Title: Morpholine and thiomorpholine tachykinin receptor antagonists
Abstract:Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
Inventor(s): Dorn; Conrad P. (Plainfield, NJ), Hale; Jeffrey J (Westfield, NJ), Finke; Paul E. (Milltown, NJ), Maccoss; Malcolm (Freehold, NJ), Mills; Sander G. (Woodbridge, NJ), Shah; Shrenik K. (Metuchen, NJ), Chambers; Mark Stuart (Watford, GB), Ladduwahetty; Tamara (Buckhurst Hill, GB), Harrison; Timothy (Great Dunmow, GB), Williams; Brian John (Great Dunnow, GB)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:09/526,843
Patent Claims: 1. A method for the prevention or treatment of nausea or emesis induced by radiation or by a cancer chemotherapeutic agent in a mammal in need thereof which comprises the administration to the mammal of an effective amount of a compound which is 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, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein the mammal is a human.

3. The method of claim 1 wherein the nausea or emesis is induced by radiation.

4. The method of claim 1 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is cisplatin.

5. The method of claim 1 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is cyclophosphamide.

6. The method of claim 1 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is doxorubicin.

7. The method of claim 1 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is daunorubicin.

8. The method of claim 1 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is etoposide.

9. A method for the prevention or treatment of nausea or emesis induced by radiation or by a cancer chemotherapeutic agent in a mammal in need thereof which comprises the administration to the mammal of an effective amount of: a compound which is ##STR28##

or a pharmaceutically acceptable salt thereof.

10. The method of claim 9 wherein the mammal is a human.

11. The method of claim 9 wherein the nausea or emesis is induced by radiation.

12. The method of claim 9 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is cisplatin.

13. The method of claim 9 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is cyclophosphamide.

14. The method of claim 9 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is doxorubicin.

15. The method of claim 9 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is daunorubicin.

16. The method of claim 9 wherein the nausea or emesis is induced by a cancer chemotherapeutic agent which is etoposide.

17. A method for the prevention or treatment of post-operative nausea and vomiting in a mammal in need thereof which comprises the administration to the mammal of an effective amount of a compound which is 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, or a pharmaceutically acceptable salt thereof.

18. A method for the prevention or treatment of post-operative nausea and vomiting in a mammal in need thereof which comprises the administration to the mammal of an effective amount of a compound which is: ##STR29##

or a pharmaceutically acceptable salt thereof.
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