Invention Grant
- Patent Title: Diazabicyclo alkane derivatives with NK1 antagonistic activity
- Patent Title (中): 具有NK1拮抗活性的二氮杂双环烷烃衍生物
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Application No.: US10490364Application Date: 2003-04-02
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Publication No.: US07202238B2Publication Date: 2007-04-10
- Inventor: Dirk de Boer , Hein K. A. C. Coolen , Mayke B. Hesselink , Wouter I. Iwema Bakker , Gijsbert D. Kuil , Jan H. van Maarseveen , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
- Applicant: Dirk de Boer , Hein K. A. C. Coolen , Mayke B. Hesselink , Wouter I. Iwema Bakker , Gijsbert D. Kuil , Jan H. van Maarseveen , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
- Applicant Address: NL
- Assignee: Solvay Pharmaceuticals B.V.
- Current Assignee: Solvay Pharmaceuticals B.V.
- Current Assignee Address: NL
- Agency: Finnegan, Henderson, Farabow, Garrett & Dunner, L.L.P.
- Priority: EP02076405 20020404
- International Application: PCT/EP03/50086 WO 20030402
- International Announcement: WO03/084955 WO 20031016
- Main IPC: A01N43/00
- IPC: A01N43/00 ; A01N43/58 ; A01N43/50 ; A61K31/55 ; C07D241/36

Abstract:
The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK1 receptor antagonistic activity represented by the general formula (1) wherein: R1 represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1–3C), R2 and R3 independently represent halogen, H, OCH3, CH3 and CF3, R4, R5 and R6 independently 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; R4 and R5 together 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
Public/Granted literature
- US20050119267A1 Diazabicyclo alkane derivatives with nk1 antagonistic activity Public/Granted day:2005-06-02
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