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Claims for Patent: 8,796,299

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Claims for Patent: 8,796,299

Title:NK1 antagonists
Abstract: A NK.sub.1 antagonist having the formula (I), ##STR00001## wherein Ar.sup.1 and Ar.sup.2 are optionally substituted phenyl or heteroaryl, X.sup.1 is an ether, thio or imino linkage, R.sup.4 and R.sup.5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
Inventor(s): Paliwal; Sunil (Monroe Township, NJ), Reichard; Gregory A. (Ann Arbor, MI), Wang; Cheng (Summit, NJ), Xiao; Dong (Warren, NJ), Tsui; Hon-Chung (East Brunswick, NJ), Shih; Neng-Yang (Warren, NJ), Arredondo; Juan D. (Montclair, NJ), Wrobleski; Michelle Laci (Whitehouse Station, NJ), Palani; Anandan (Bridgewater, NJ)
Assignee: OPKO Health, Inc. (Miami, FL)
Application Number:13/625,799
Patent Claims: 1. A method for treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of at least one compound of Formula I: ##STR00253## or a pharmaceutically-acceptable salt thereof, wherein Ar.sup.1 is phenyl; ##STR00254## X.sup.2 is --O--; R.sup.1 and R.sup.2 are each independently selected from the group consisting of H, C.sub.1-C.sub.6 alkyl, hydroxy(C.sub.1-C.sub.3alkyl), C.sub.3-C.sub.8 cycloalkyl, --CH.sub.2F, --CHF.sub.2 and --CF.sub.3; or R.sup.1 and R.sup.2, together with the carbon atom to which they are both attached, form a C.sub.3 to C.sub.6 alkylene ring; or R.sup.1 and R.sup.2, together with the carbon atom to which they are both attached, form a C.dbd.O group; R.sup.3 is selected from the group consisting of H, C.sub.1-C.sub.6 alkyl, hydroxy(C.sub.1-C.sub.3 alkyl), C.sub.3-C.sub.8 cycloalkyl, --CH.sub.2F, --CHF.sub.2 and --CF.sub.3; each R.sup.6 is independently selected from the group consisting of H, C.sub.1-C.sub.6 alkyl and --OH; each R.sup.7 is independently selected from the group consisting of H and C.sub.1-C.sub.6 alkyl; n.sub.2 is 2; R.sup.4 and R.sup.5, together with the carbon atom to which they are both attached, form a 5- or 6-membered heterocycloalkyl ring selected from the group consisting of: ##STR00255## wherein said 5- or 6-membered heterocycloalkyl ring is optionally substituted with from 1 to 6 substitutents independently selected from the group consisting of R.sup.30 and R.sup.31; R.sup.18 is H, C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.8 cycloalkyl, (C.sub.3-C.sub.8)cycloalkyl(C.sub.1-C.sub.6)alkyl, hydroxy(C.sub.2-C.sub.6)alkyl or --P(O)(OH).sub.2; R.sup.30 and R.sup.31 are each independently selected from the group consisting of H and C.sub.1-C.sub.2 alkyl, or R.sup.30 and R.sup.31, together with the carbon atom to which they are both attached, form .dbd.O; R.sup.32 and R.sup.33 are each independently selected from the group consisting of H and C.sub.1-C.sub.6 alkyl; or a, where the physiological disorder, symptom or disease is asthma, emesis, nausea, depression, anxiety, cough or migraine.

2. The method according to claim 1, wherein the compound is selected from: ##STR00256## ##STR00257## or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1, wherein the compound is: ##STR00258## or a pharmaceutically acceptable salt thereof.

4. The method according to claim 1, wherein the physiological disorder, symptom or disease is emesis and nausea.

5. The method according to claim 1, wherein the physiological disorder, symptom or disease is cough.

6. The method according to claim 1, wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of H and C.sub.1-C.sub.6 alkyl.

7. The method according to claim 6, wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of H and CH.sub.3.

8. The method according to claim 1, wherein R.sup.3 is H or C.sub.1-C.sub.6 alkyl.

9. The method according to claim 8, wherein R.sup.3 is H.

10. The method according to claim 1, wherein each R.sup.6 is independently H or C.sub.1-C.sub.6 alkyl.

11. The method according to claim 10, wherein each R.sup.6 is H.

12. The method according to claim 1, wherein each R.sup.7 is H.

13. The method according to claim 1, wherein R.sup.18 is H or C.sub.1-C.sub.6 alkyl.

14. The method according to claim 13, wherein R.sup.18 is H.

15. The method according to claim 1, wherein R.sup.32 and R.sup.33 are each H.
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