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US 2007/0185127 A1Published application
2-(Arylalkoxy)-1-phenylethylamine derivatives as nk1 antagonist and serotonin reuptake inhibitors
AssigneeAstraZeneca AB
InventorCathy Dantzman
Life of this patent
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Abstract
Compounds of the following formula (I) wherein R1 R2, n, A1 and A2 are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. The example compounds are 1-(2-(naphthylmethoxy)-1-phenylethyl)piperazine derivatives. The compounds are neurokinin 1 (NK1) receptor antagonist and/or serotonin reuptake inhibitors, with medical indications for depression and other disorders.
Claims13
A compound according to structural diagram I:
- wherein:
- R1 and R2 are independently selected from C1-6alkyl or C16alkenyl, 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 or C1-4alkyl substituted with 1, 2 or 3 halo moieties, amino, or amino substituted with C1-4alkyl, C1-4alkoxy or C1-4alkyl, substituted with 0, 1, 2, or 3 halo moieties;
- 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 or C1-4alkyl substituted with 1, 2 or 3 halo moieties;
- and
- Ar2 phenyl, naphthyl, tetralin, or phenyl, naphthyl or tetralin substituted with moieties independently selected from hydrogen, halogen, cyano, nitro, C1-4alkyl, C1-4alkoxy or C1-4alkyl substituted with 1, 2 or 3 halo moieties;
- in vivo hydrolysable precursors and pharmaceutically-acceptable salts thereof.
5 more elements
8-9. (canceled)
Dependencies are inferred from the claim text.