2-(arylalkoxy)-1-phenylethylamine derivatives as NK 1...

Details 2-(arylalkoxy)-1-phenylethylamine derivatives as NK 1... 2-(arylalkoxy)-1-phenylethylamine derivatives as NK 1...

2008-05-06

2008-05-06

Wilson, James O. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S398000, C564S428000

Reexamination Certificate

active

07368448

ABSTRACT:
Compounds of the following formula (I) wherein R1R2, n, Ar1and A2are 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

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Ryckmans, et al., Dual NK1 Antagonists—Serotonin Reuptake Inhibitors as Potential Antidepressants. Part 2: SAR and Activity of Benzyloxyphenethyl Piperazine Derivatives, Bioorganic & Medicinal Chemistry Letters, 12, 3195-3198 (2002).
Genicot, C. et al., “Discovery of orally bioavailable NK1 receptor antagonists”; Bioorg. Med. Chem. Lett. 2003, 13(3), pp. 437-442.
Ryckmans, T. et al., “Dual NK1 antagonists-serotonin reuptake . . . SAR and activity of benzyloxyphenethyl piperazine derivatives”; Bioorg. Med Chem Lett., 2002, 12(21), 3195-3198.

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