发明授权
- 专利标题: Heterocyclic-substituted indoles and pharmaceutical compositions containing them
- 专利标题(中): 杂环取代的吲哚和含有它们的药物组合物
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申请号: US904092申请日: 1986-09-04
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公开(公告)号: US4851406A公开(公告)日: 1989-07-25
- 发明人: Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
- 申请人: Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
- 申请人地址: DEX Mannheim
- 专利权人: Boehringer Mannheim GmbH
- 当前专利权人: Boehringer Mannheim GmbH
- 当前专利权人地址: DEX Mannheim
- 优先权: DEX3531658 19850905
- 主分类号: C07D409/14
- IPC分类号: C07D409/14 ; A61K31/44 ; A61K31/4427 ; A61K31/4433 ; A61K31/445 ; A61K31/50 ; A61K31/53 ; A61K31/535 ; A61P9/00 ; C07D237/00 ; C07D333/00 ; C07D401/14 ; C07D403/04 ; C07D403/14 ; C07D413/14 ; C07D417/14
摘要:
The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.2 is ##STR2## the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention provides intermediates of the general formula: ##STR3## in which R.sub.1, R.sub.2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
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