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    1-Phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them
    1.
    发明授权
    1-Phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
    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。

    1-phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them
    2.
    发明授权
    1-phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
    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：US4924004A

    公开(公告)日：1990-05-08

    申请号：US264049

    申请日：1988-10-28

    申请人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuehl ,  Gerd Buschmann ,  Stephen Magda

    发明人： Heinrich-Wilhelm Ohlendorf ,  Wilhelm Kaupmann ,  Ulrich Kuehl ,  Gerd Buschmann ,  Stephen Magda

    IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/06 ,  C07D209/24 ,  C07D209/42

    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, cycloalkyl or 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 a alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmacological properties, in particular antiarrhythmic properties. The compounds may be in the form of the free base 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.

    N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine derivatives and medical compositions thereof
    3.
    发明授权
    N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine derivatives and medical compositions thereof 失效
    N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺衍生物及其医药组合物

    公开(公告)号：US4714709A

    公开(公告)日：1987-12-22

    申请号：US653707

    申请日：1984-09-24

    申请人： Peter W. Thies ,  Samuel David ,  Ulrich Kuehl ,  Gerd Buschmann ,  Peter Flecker

    发明人： Peter W. Thies ,  Samuel David ,  Ulrich Kuehl ,  Gerd Buschmann ,  Peter Flecker

    IPC分类号： A61K31/35 ,  A61K31/357 ,  A61P9/12 ,  C07D319/00 ,  C07D493/08 ,  A61K31/40 ,  C07D405/12

    CPC分类号： C07D493/08

    摘要： N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.

    摘要翻译： 对应于具有降血压效果的式“IMAGE”I的N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺化合物， 制备这样的化合物和掺入这种化合物的药物组合物，其中R 1是氢，苄基或低级烷基; R2是低级烷基或低级烷酰基; R3是氢或低级烷基; R4是氢，苄氧基，羟基或低级烷氧基; R5是氢，苄氧基，羟基或低级烷氧基; 并且A和B既可以是氢，也可以一起表示它们各自的碳之间的键。

    3,7-Diazabicyclo(3,3,1)nonane compounds and their use in treating heart disease
    8.
    发明授权
    3,7-Diazabicyclo(3,3,1)nonane compounds and their use in treating heart disease 失效
    3,7-二氮杂双环（3,3,1）壬烷化合物及其在治疗心脏病中的应用

    公开(公告)号：US4550112A

    公开(公告)日：1985-10-29

    申请号：US532762

    申请日：1983-09-16

    申请人： Uwe Schoen ,  Bernd Hachmeister ,  Wolfgang Kehrbach ,  Ulrich Kuehl ,  Gerd Buschmann

    发明人： Uwe Schoen ,  Bernd Hachmeister ,  Wolfgang Kehrbach ,  Ulrich Kuehl ,  Gerd Buschmann

    IPC分类号： A61K31/435 ,  A61P9/06 ,  A61P9/10 ,  C07D471/08 ,  C07D471/10 ,  A61K31/445

    CPC分类号： C07D471/08 ,  C07D471/10

    摘要： Novel 3,7-diaza bicyclo-(3,3,1)-nonane compounds are described which are represented by the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 each denotes hydrogen,R.sub.1 and R.sub.2 each denotes (A) a substituent which contains up to 12 carbon atoms and which is selected from the group consisting of alkyl, alkenyl, and alkinyl, or (B) a cycloalkyl group containing 3 to 6 carbon atoms which is attached to the nitrogen atom directly or by an alkylene group containing 1 to 3 carbon atoms, andR.sub.3 and R.sub.4 each denotes an alkyl group with up to 7 carbon atoms, or both together form an alkylene chain represented by the formula --(CH.sub.2).sub.n --, wherein n is an integer ranging between about 3 and 6, such that the substituents R.sub.1, R.sub.2, R.sub.3, and R.sub.4 together contain at least 5 carbon atoms. Also described are processes of producing said compounds, pharmaceutical compositions containing compounds of Formula I, and methods of preparing and using said compositions.

    摘要翻译： 描述了由下式表示的新颖的3,7-二氮杂双环（3,3,1） - 壬烷化合物：其中Z1和Z2各自表示氢，R1和R2各自表示（A）含有 至多12个碳原子，并且其选自烷基，烯基和炔基，或（B）含有3至6个碳原子的环烷基，其直接连接到氮原子上或通过含有1至 3个碳原子，并且R 3和R 4各自表示具有至多7个碳原子的烷基，或两者一起形成由式 - （CH 2）n - 表示的亚烷基链，其中n为约3至6的整数， 使得取代基R 1，R 2，R 3和R 4一起含有至少5个碳原子。 还描述了生产所述化合物的方法，含有式I化合物的药物组合物，以及制备和使用所述组合物的方法。