Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2007-04-10
2007-04-10
Tucker, Zachary C. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S249000, C540S579000, C540S580000, C544S349000
Reexamination Certificate
active
10490364
ABSTRACT:
The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK1receptor antagonistic activity represented by the general formula (1) wherein: R1represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1–3C), R2and R3independently represent halogen, H, OCH3, CH3and CF3, R4, R5and R6independently represent H, OH, O-alkyl(1–4C), CH2OH, NH2, dialkyl(1–3C)N, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or morpholin-4-yl substituted with one or two methyl or methoxymethyl groups, morpholin-4-ylamino, morpholin-4-ylmethyl, imidazol-1-yl, thiomorpholin-4-yl, 1,1-dioxothiomorpholin-4-yl or 3-oxa-8-azabicyclo[3.2.1]oct-8-yl; R4and R5together may represent a keto, a 1,3-dioxan-2-yl or a 1,3-dioxolan-2-yl group, X represents either O or S, n has the value of 1, 2 or 3, a is the asymmetrical carbon atom 8a, 9a or 10a when n equals 1, 2 or 3 respectively The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient
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Bakker Wouter I. Iwema
Coolen Hein K. A. C.
de Boer Dirk
Hesselink Mayke B.
Kuil Gijsbert D.
Finnegan Henderson Farabow Garrett & Dunner L.L.P.
Solvay Pharmaceuticals B.V.
Tucker Zachary C.
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