Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2006-08-22
2006-08-22
Bernhardt, Emily (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S233500, C514S252110, C514S252130, C514S253040, C514S253090, C514S254060, C514S254090, C514S255010, C544S061000, C544S121000, C544S357000, C544S362000, C544S364000, C544S371000, C544S373000, C544S389000, C544S391000, C544S403000, C544S376000
Reexamination Certificate
active
07094779
ABSTRACT:
The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH3, CF3, OCH3, halogen, cyano and 5-CF3-tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1–3C); n has the value 0–3; m has the value 0–2; R1represents NH2, NH-alkyl (1–3C), dialkyl (1–3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH3-piperazinyl; R2is hydrogen, alkyl (1–4C) or phenyl, or R2together with (CH2)mwherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R3and R4independently represent hydrogen or methyl, or R3and R4together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved
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Bakker Wouter I. Iwema
Coolen Hein K. A. C.
Herremans Arnoldus H. J.
Mccreary Andrew C.
Tulp Martinus Th. M.
Bernhardt Emily
Solvay Pharmaceuticals B.V.
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