US 7,368,448 B2
2-(arylalkoxy)-1-phenylethylamine derivatives as NK1 antagonist and serotonin reuptake inhibitors
Cathy Dantzman, Wilmington, Del. (US)
Assigned to AstraZeneca AB, Sodertalje (Sweden)
Appl. No. 10/599,824
PCT Filed Apr. 06, 2005, PCT No. PCT/SE2005/000499
§ 371(c)(1), (2), (4) Date Oct. 11, 2006,
PCT Pub. No. WO2005/100324, PCT Pub. Date Oct. 27, 2005.
Claims priority of application No. 0400968 (SE), filed on Apr. 14, 2004.
Prior Publication US 2007/0185127 A1, Aug. 09, 2007
Int. Cl. A61K 31/497 (2006.01); C07D 241/04 (2006.01); C04D 295/00 (2006.01); C07C 211/00 (2006.01)
U.S. Cl. 514—252.12  [544/398; 564/428] 10 Claims
 
1. A compound according to structural diagram I:

OG Complex Work Unit Drawing
wherein:
R1 and R2 are independently selected from C1-6alkyl or C1-6alkenyl, or together with the N to which they are bound, form a heterocycle containing 6, 7 or 8 atoms or such a heterocycle substituted with moieties independently selected from hydrogen, halogen, C1-4alkyl, C1-4alkoxy, and C1-4alkyl substituted with 1, 2 or 3 halo or amino; wherein said amino is optionally substituted with C1-4alkyl, C1-4alkoxy or C1-4alkyl substituted with 1, 2, or 3 halo;
R4 is hydrogen;
n is 0, 1 or 2;
Ar1 is phenyl or phenyl substituted with moieties independently selected from hydrogen, halogen, —S—C1-4alkyl, C1-4alkyl, C1-4alkoxy and C1-4alkyl substituted with 1, 2 or 3 halo; and
Ar2 is naphthyl or tetralin, or naphthyl or tetralin substituted with moieties independently selected from hydrogen, halogen, cyano, nitro, C1-4alkoxy, and C1-4alkyl substituted with 1, 2 or 3 halo moieties;
or an in vivo hydrolysable precursor or a pharmaceutically-acceptable salt thereof.