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1. 发明授权

US4814345A 1-phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4814345A
公开(公告)日：1989-03-21
申请号：US123201
申请日：1987-11-20
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuhl , Gerd Buschmann , Stephen J. Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuhl , Gerd Buschmann , Stephen J. Magda
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/42 , A61K31/405
CPC分类号： C07D209/42
摘要： Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.
摘要翻译：公开了具有通式I的新型1-苯基-2-氨基羰基吲哚化合物，其中R 1是脂族或芳族酰基或任选取代的苄基; R2是氢或低级烷基; R3是氢，卤素，低级烷基或低级烷氧基; R4是氢，卤素，低级烷基或低级烷氧基; R5具有给定R3的意义; R6对R4具有重要意义，或R6是硝基或三氟甲基; R7和R8各自表示氢或低级烷基，或与氮原子一起形成杂环基; Z表示任选被羟基或酰氧基取代的亚烷基链。这些化合物具有药理学，特别是抗心律不齐的特性。

2. 发明授权

US4803198A 1-Phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4803198A
公开(公告)日：1989-02-07
申请号：US885684
申请日：1986-07-15
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen J. Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen J. Magda
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/24 , C07D209/42 , A61K31/55 , C07D403/12 , C07D403/14
CPC分类号： C07D209/42
摘要： New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmaceutical properties, in particular antiarrhythmic properties. The compounds may be in the form of the free bases or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them.Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.
摘要翻译：描述了具有通式Ⅰ的新的1-苯基-2-氨基羰基吲哚化合物，其中R 1是氢原子，或低级烷基，烯基，环烷基烷基，R 2是氢原子或低级烷基，R 3 是氢或卤素原子，或低级烷基，羟基或低级烷氧基，R4是氢或卤素原子，或低级烷基，羟基或低级烷氧基，或者如果R3是氢原子，R4可以是硝基或三氟甲基，或R 3和R 4一起表示亚甲二氧基或亚乙二氧基，R 5具有R 3的含义，R 6具有对R 4的定义，R 7是氢原子，或者如果R 5和R 6是低级烷氧基，则R 7 也可以是低级烷氧基，R 8和R 9各自为氢原子或低级烷基，或者与氮原子一起形成杂环基，Z为任选被羟基取代的亚烷基链。这些化合物具有药物性质，特别是抗心律失常性质。化合物可以是游离碱或酸加成盐的形式。含有这些化合物的药物组合物被描述为制备它们的方法。还描述了制备这些化合物的有价值的中间体和制备中间体的方法。

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