Solvay Pharmaceuticals, B.v.

Dirk De Boer

Wouter I Iwema Bakker

Gustaaf J M Van Scharrenburg

Hein K A C Coolen

Andrew C McCreary

Jan H Van Maarseveen

Mayke B Hesselink

Gijsbert D Kuil

The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NKreceptor antagonistic activity represented by the general formula (1) wherein: Rrepresents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1&#x2013;3C), Rand Rindependently represent halogen, H, OCH, CHand CF, R, Rand Rindependently represent H, OH, O-alkyl(1&#x2013;4C), CHOH, NH, dialkyl(1&#x2013;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; Rand Rtogether 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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Weesp, Netherlands

Dirk De Boer