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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 7202238 B1

PDFFull Text
Date of Patent:
Apr. 10, 2007

Filed:

Apr. 02, 2003

[object object]

Applicants:

Dirk DE Boer, Weesp, NL;

Hein K. A. C. Coolen, Weesp, NL;

Mayke B. Hesselink, Weesp, NL;

Wouter I. Iwema Bakker, Weesp, NL;

Gijsbert D. Kuil, Weesp, NL;

Jan H. Van Maarseveen, Weesp, NL;

Andrew C. Mccreary, Weesp, NL;

Gustaaf J. M. Van Scharrenburg, Weesp, NL;

Inventors:

Dirk de Boer, Weesp, NL;

Hein K. A. C. Coolen, Weesp, NL;

Mayke B. Hesselink, Weesp, NL;

Wouter I. Iwema Bakker, Weesp, NL;

Gijsbert D. Kuil, Weesp, NL;

Jan H. van Maarseveen, Weesp, NL;

Andrew C. McCreary, Weesp, NL;

Gustaaf J. M. van Scharrenburg, Weesp, NL;

Assignee:

Solvay Pharmaceuticals B.V., , NL;

Attorney:

Finnegan, Henderson, Farabow, Garrett & Dunner, L.L.P.

Primary Examiner:

Zachary C Tucker

Int. Cl.
CPC ...
A01N 43/00 (2006.01); A01N 43/58 (2006.01); A01N 43/50 (2006.01); A61K 31/55 (2006.01); C07D 241/36 (2006.01);
U.S. Cl.
CPC ...
Abstract

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 (1–3C), Rand Rindependently represent halogen, H, OCH, CHand CF, R, Rand Rindependently represent H, OH, O-alkyl(1–4C), CHOH, NH, 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; 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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