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US 8,273,895 B2Granted
NK1 antagonists
AssigneeOPKO Health, Inc.
InventorsSunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Abstract
A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 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.
Claims3
A compound having the formula (I):
- or a pharmaceutically acceptable salt thereof, wherein
- Ar1 is phenyl, wherein said phenyl can be unsubstituted or substituted with 1 to 3 fluoro;
- Ar2 is bis(trifluoromethyl)phenyl;
- X1 is —O—;
- R1 and R2 are independently selected from the group consisting of H, C1-C6 alkyl or hydroxyl(C1-C3 alkyl), C3-C8 cycloalkyl, —CH2F, —CHF2, —CF3;
- R3 is H, C1-C6 alkyl, hydroxyl(C1-C3 alkyl), C3-C8 cycloalkyl, —CH2F, —CF2H, or —CF3;
- R6 and R7 are independently selected from H or C1-C6 alkyl;
- n2 is 1 or 2;
- R4 and R5 together are ═O;
- R18 is C1-C6 alkyl, Cbz or H;
- R32 and R33 are each H;
- or a diaseteromer, enantiomer, stereoisomer, regioisomer, rotamer, or tautomer thereof.
9 more elements
Dependencies are inferred from the claim text.