发明名称 |
BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY |
摘要 |
The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2 or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino. |
申请公布号 |
WO9940067(A2) |
申请公布日期 |
1999.08.12 |
申请号 |
WO1999EP00852 |
申请日期 |
1999.02.05 |
申请人 |
DUPHAR INTERNATIONAL RESEARCH B.V.;DEN HARTOG, JACOBUS A., J.;VISSER, GERBEN, M.;VAN STEEN, BARTHOLOMEUS, J.;TULP, MARTINUS, T., M.;RONKEN, ERIC;KRUSE, CORNELIS, G.;LANGE, JOSEPHUS H., M. |
发明人 |
DEN HARTOG, JACOBUS A., J.;VISSER, GERBEN, M.;VAN STEEN, BARTHOLOMEUS, J.;TULP, MARTINUS, T., M.;RONKEN, ERIC;KRUSE, CORNELIS, G.;LANGE, JOSEPHUS H., M. |
分类号 |
A61K31/445;A61K31/454;A61K31/55;A61P25/00;A61P25/16;A61P25/22;A61P25/24;A61P25/28;A61P43/00;C07D413/14 |
主分类号 |
A61K31/445 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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