发明公开
EP0289070A1 Tertiary arylethyl amine derivatives having opiate-antagonistic activity
失效
TertiäreArylethylamin-Derivate mit opiat-antagonistischer Wirkung。
- 专利标题： Tertiary arylethyl amine derivatives having opiate-antagonistic activity
- 专利标题（中）： TertiäreArylethylamin-Derivate mit opiat-antagonistischer Wirkung。
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申请号： EP88200648.9申请日： 1988-04-06
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公开(公告)号： EP0289070A1公开(公告)日： 1988-11-02
- 发明人: Van Wijngaarden, Ineke , Den Hartog, Jacobus A. J. , Tulp, Martinus T. M. , Lobbezoo, Marinus W.
- 申请人： DUPHAR INTERNATIONAL RESEARCH B.V
- 申请人地址： C.J. van Houtenlaan 36 NL-1381 CP Weesp NL
- 专利权人： DUPHAR INTERNATIONAL RESEARCH B.V
- 当前专利权人： DUPHAR INTERNATIONAL RESEARCH B.V
- 当前专利权人地址： C.J. van Houtenlaan 36 NL-1381 CP Weesp NL
- 代理机构： Muis, Maarten
- 优先权： NL8700842 19870410
- 主分类号： C07C215/52
- IPC分类号： C07C215/52 ; C07C215/60 ; C07C225/00 ; C07C237/20 ; C07D207/335 ; C07D231/12 ; A61K31/135 ; A61K31/16 ; A61K31/40 ; A61K31/415
摘要：
The invention relates to a group of tertiary arylethyl amine derivatives having opiate-antagonistic activity. The compounds have the general formula 1
wherein
R 1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group -NHRs or -CONHR 9 , wherein R s is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 1-7 C-atoms;
R 2 is hydrogen or, when R 1 is hydrogen, one of the other meanings of Ri, or
R 1 and R 2 together with the 2 carbon atoms of the benzene ring constitute a heterocyclic group which consists of five or six ring atoms and which comprises a group -NH-and, optionally may comprise an oxygen atom, sulphur atom or nitrogen atom as a second hetero atom;
R 3 is hydrogen, alkyl, alkoxy or alkylthio having 1-4 C-atoms, amino, mono-or dialkylamino having 1-4 C-atoms per alkyl group, hydroxyalkyl, alkyl-, alkylamino-or alkoxycarbonyl having 1-4 C-atoms in the alkyl group, nitro, cyano, halogen, trifluoromethyl, trifluoromethoxy, alkylsulphonyl having 1-4 C-atoms, or aminosulphonyl;
m has the value 1, 2 or 3;
R 4 is hydrogen, alkyl or alkoxy having 1-3 C-atoms, or hydroxyl;
R s is hydrogen; alkyl, phenylalkyl, hydroxyalkyl, methoxyalkyl, alkylcarbonyl, alkoxycarbonyl or alkylaminocarbonyl having 1-6 C-atoms in the optionally branched alkyl group;
R 6 is straight or branched alkyl, alkenyl or cycloalkylalkyl or cycloalkyl, having at most 8 C-atoms;
Y is a group R 7 -X-R 8 , wherein R 7 is a straight or branched alkylene chain having 3-8 C-atoms with at least 3 C-atoms between the nitrogen atom and group X; X is the carbonyl group or ketalised carbonyl group, or the group CHOH, CHC 6 H 5 , CH 2 , -CONH-or -CO-NCH 3 or an oxygen atom or sulphur atom; and R 8 is an alkyl group, cycloalkyl group or cycloalkylalkyl group having at most 10 C-atoms a phenyl group or phenylalkyl group having 1-4 C-atoms in the alkyl group, which groups Rs can be substituted with one or more groups R 3 ; or Y is a group of the formula 2a-2e
wherein R 10 may have the meanings given for R 3 .
wherein
R 1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group -NHRs or -CONHR 9 , wherein R s is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 1-7 C-atoms;
R 2 is hydrogen or, when R 1 is hydrogen, one of the other meanings of Ri, or
R 1 and R 2 together with the 2 carbon atoms of the benzene ring constitute a heterocyclic group which consists of five or six ring atoms and which comprises a group -NH-and, optionally may comprise an oxygen atom, sulphur atom or nitrogen atom as a second hetero atom;
R 3 is hydrogen, alkyl, alkoxy or alkylthio having 1-4 C-atoms, amino, mono-or dialkylamino having 1-4 C-atoms per alkyl group, hydroxyalkyl, alkyl-, alkylamino-or alkoxycarbonyl having 1-4 C-atoms in the alkyl group, nitro, cyano, halogen, trifluoromethyl, trifluoromethoxy, alkylsulphonyl having 1-4 C-atoms, or aminosulphonyl;
m has the value 1, 2 or 3;
R 4 is hydrogen, alkyl or alkoxy having 1-3 C-atoms, or hydroxyl;
R s is hydrogen; alkyl, phenylalkyl, hydroxyalkyl, methoxyalkyl, alkylcarbonyl, alkoxycarbonyl or alkylaminocarbonyl having 1-6 C-atoms in the optionally branched alkyl group;
R 6 is straight or branched alkyl, alkenyl or cycloalkylalkyl or cycloalkyl, having at most 8 C-atoms;
Y is a group R 7 -X-R 8 , wherein R 7 is a straight or branched alkylene chain having 3-8 C-atoms with at least 3 C-atoms between the nitrogen atom and group X; X is the carbonyl group or ketalised carbonyl group, or the group CHOH, CHC 6 H 5 , CH 2 , -CONH-or -CO-NCH 3 or an oxygen atom or sulphur atom; and R 8 is an alkyl group, cycloalkyl group or cycloalkylalkyl group having at most 10 C-atoms a phenyl group or phenylalkyl group having 1-4 C-atoms in the alkyl group, which groups Rs can be substituted with one or more groups R 3 ; or Y is a group of the formula 2a-2e
wherein R 10 may have the meanings given for R 3 .
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