发明授权
US4728649A 3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity
失效
具有抗癌剂活性的3-氧代 - 哌嗪-1-基 - 麦角酰胺
- 专利标题: 3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity
- 专利标题(中): 具有抗癌剂活性的3-氧代 - 哌嗪-1-基 - 麦角酰胺
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申请号: US817135申请日: 1986-01-08
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公开(公告)号: US4728649A公开(公告)日: 1988-03-01
- 发明人: Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi , Lorenzo Pegrassi
- 申请人: Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi , Lorenzo Pegrassi
- 申请人地址: ITX Milan
- 专利权人: Farmitalia Carlo Erba
- 当前专利权人: Farmitalia Carlo Erba
- 当前专利权人地址: ITX Milan
- 优先权: GBX8501078 19850116
- 主分类号: A61K31/48
- IPC分类号: A61K31/48 ; A61P9/12 ; A61P25/00 ; A61P25/20 ; C07D457/02 ; C07D457/12 ; A61K31/445
摘要:
The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.
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