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    (2H)-3-benzazepin-2-ones, their pharmaceutical compositions and their pharmaceutical uses
    4.
    发明授权
    (2H)-3-benzazepin-2-ones, their pharmaceutical compositions and their pharmaceutical uses 失效

    公开(公告)号：US4737495A

    公开(公告)日：1988-04-12

    申请号：US868986

    申请日：1986-05-30

    申请人： Andreas Bomhard ,  Manfred Psiorz ,  Joachim Heider ,  Norbert Hauel ,  Klaus Noll ,  Berthold Narr ,  Walter Kobinger ,  Christian Lillie

    发明人： Andreas Bomhard ,  Manfred Psiorz ,  Joachim Heider ,  Norbert Hauel ,  Klaus Noll ,  Berthold Narr ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04 ,  C07D521/00 ,  A61K31/445 ,  A61K31/47 ,  A61K31/55 ,  C07D233/16

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04

    摘要： The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##STR2## group and B represents a methylene, carbonyl or thiocarbonyl group or A represents a --CO--CO or ##STR3## group and B represents a methylene group, in which the carbon atom marked x is linked to the phenyl nucleus,E represents a straight-chained alkylene group optionally substituted by an alkyl group,G represents a straight-chained alkylene group optionally substituted by an alkyl group,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, an alkenyl group, an alkyl or phenylalkyl group, andHet represents a 5- or 6-membered heteroaromtic ring bonded via a carbon or nitrogen atom, which contains an oxygen, sulphur or nitrogen atom, two nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, and onto which additionally a phenyl ring can be condensed, in which case the bond can also be via the phenyl nucleus, or an imidazo[1,2-a]pyridyl group wherein the carbon structure of the above-mentioned groups can be substituted by a methylenedioxy or ethylenedioxy group or can be mono- or disubstituted by a halogen atom or an alkyl, hydroxy, alkoxy, phenylalkoxy, phenyl, dimethoxyphenyl, nitro, amino, acetylamino, carbamoylamino, N-alkyl-carbamoylamino, hydroxymethyl, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, alkylsulphonylamino, alkoxycarbonylmethoxy, carboxymethoxy or alkoxymethyl group, and at the same time any imino group present in the above-mentioned heteroaromatic groups can be substituted by an alkyl, phenylalkyl or phenyl group, the N-oxides and the acid addition salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly the effect of lowering heart rate and oxygen requirement of the heart. They can be used to treat sinus tachycardia or ischaemic heart disease.

    Benzazepine derivatives
    6.
    发明授权
    Benzazepine derivatives 失效
    苯扎西平衍生物

    公开(公告)号：US4604389A

    公开(公告)日：1986-08-05

    申请号：US732204

    申请日：1985-05-08

    申请人： Manfred Reiffen ,  Klaus Noll ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    发明人： Manfred Reiffen ,  Klaus Noll ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/55 ,  A61P9/06 ,  C07C59/64 ,  C07D223/16 ,  C07D233/16 ,  C07D243/04 ,  C07D405/12 ,  C07D491/04 ,  C07D491/056 ,  C07D521/00

    CPC分类号： C07D223/16 ,  C07C59/64 ,  C07D243/04 ,  C07D405/12 ,  C07D491/04

    摘要： This invention relates to benzazepine derivatives of formula I ##STR1## wherein A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sub.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, acylamino, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy or, together with R.sub.1, can be C.sub.1 -C.sub.3 alkylenedioxy;R.sub.3 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkoxy;R.sub.4 is hydrogen, benzyl, C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.5 alkenyl;R.sub.5 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy or, together with R.sub.5, can be a C.sub.1 -C.sub.2 alkylenedioxy;X is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is oxygen, sulphur, sulphinyl or sulphonyl;Y is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is methylene or carbonyl;m and n are each independently 2, 3 or 4; and nontoxic, pharmaceutically acceptable addition salts thereof. These compounds have valuable pharmacological properties, particularly the effect of lowering heart rate and reducing the O.sub.2 requirement of the heart.

    摘要翻译： 本发明涉及式I的苯并氮杂衍生物，其中A是-CH 2 CH 2 - 或-CH = CH-; R1是氢，氯，溴，C1-C3烷基，氨基，C1-C3烷基氨基，C1-C3二烷基氨基，酰氨基，羟基，C1-C3烷氧基或苯基C1-C3烷氧基; R2是氢，氯，溴，羟基，C1-C3烷基，C1-C3烷氧基或苯基C1-C3烷氧基，或与R1一起可以是C1-C3亚烷基二氧基; R3是氢，氯，溴或C1-C3烷氧基; R4是氢，苄基，C1-C3烷基或C3-C5烯基; R5是氢，卤素，C1-C3烷基或C1-C3烷氧基; R 6是氢，C 1 -C 3烷基或C 1 -C 3烷氧基，或与R 5一起可以是C 1 -C 2亚烷基二氧基; X是任选被苄基或C 1 -C 3烷基取代的亚氨基，或是氧，硫，亚磺酰基或磺酰基; Y是任选被苄基或C 1 -C 3烷基取代的亚氨基，或亚甲基或羰基; m和n各自独立地为2,3或4; 和无毒的药学上可接受的加成盐。 这些化合物具有有价值的药理学特性，特别是降低心率并降低心脏O2需求的作用。

    Benzazepine derivatives, their pharmaceutical compositions and method of use
    7.
    发明授权
    Benzazepine derivatives, their pharmaceutical compositions and method of use 失效
    苯扎西平衍生物，其药物组合物和使用方法

    公开(公告)号：US4490369A

    公开(公告)日：1984-12-25

    申请号：US547940

    申请日：1983-11-02

    申请人： Manfred Reiffen ,  Joachim Heider ,  Norbert Hauel ,  Volkhard Austel ,  Wolfgang Eberlein ,  Walter Kobinger ,  Christian Lillie ,  Klaus Noll ,  Helmut Pieper ,  Gerd Kruger ,  Johannes Keck

    发明人： Manfred Reiffen ,  Joachim Heider ,  Norbert Hauel ,  Volkhard Austel ,  Wolfgang Eberlein ,  Walter Kobinger ,  Christian Lillie ,  Klaus Noll ,  Helmut Pieper ,  Gerd Kruger ,  Johannes Keck

    IPC分类号： C07C59/64 ,  C07D205/04 ,  C07D223/16 ,  C07D243/02 ,  C07D243/04 ,  C07D491/04 ,  A61K31/55 ,  C07D521/00

    CPC分类号： C07D223/16 ,  C07C59/64 ,  C07D205/04 ,  C07D243/02 ,  C07D243/04 ,  C07D491/04

    摘要： Compounds of the formula ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO--, --CH.sub.2 --CO-- or ##STR2## where R.sub.7 is alkyl of 1 to 3 carbon atoms, andB is methylene, carbonyl or thiocarbonyl, orA is --CO--CO--, --N.dbd.CH--, ##STR3## where R.sub.8 is hydrogen or alkyl of 1 to 3 carbon atoms substituted by a phenyl, methoxyphenyl or dimethoxyphenyl, andB is methylene;E is n-alkylene of 2 to 4 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;G is n-alkylene of 1 to 5 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, wherein one methylene group of an n-alkylene of 2 to 5 carbon atoms can be replaced by a carbonyl group, with the proviso that B represents a methylene or carbonyl group, or methylene-n-hydroxy-alkylene of 1 to 4 carbon atoms, where the methylene group is attached to the nitrogen atom; andR.sub.1 to R.sub.5 are simple substituents of various types;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

    摘要翻译： 其中A是-CH 2 -CH 2 - ， - CH = CH - ， - NH-CO-， - CH 2 -CO-或者其中R 7是1至3个碳原子的烷基，和B 是亚甲基，羰基或硫代羰基，或A是-CO-CO-，-N = CH-，其中R 8是氢或被苯基，甲氧基苯基或二甲氧基苯基取代的1至3个碳原子的烷基，和 B是亚甲基; E是任选被1至3个碳原子的烷基取代的2至4个碳原子的正亚烷基，2-羟基 - 正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯; G是任选被1至3个碳原子的烷基取代的1至5个碳原子的正亚烷基，其中2至5个碳原子的正亚烷基的一个亚甲基可被羰基取代，条件是 B表示亚甲基或羰基，或亚甲基与氮原子连接的1至4个碳原子的亚甲基 - 正 - 羟基 - 亚烷基; 而R1至R5是各种简单的取代基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作心动过缓。

    Aminotetralin derivatives
    8.
    发明授权
    Aminotetralin derivatives 失效
    氨基四氢萘衍生物

    公开(公告)号：US4584293A

    公开(公告)日：1986-04-22

    申请号：US732199

    申请日：1985-05-08

    申请人： Manfred Reiffen ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    发明人： Manfred Reiffen ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/55 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C45/00 ,  C07C45/51 ,  C07C49/755 ,  C07C57/58 ,  C07C59/64 ,  C07C205/56 ,  C07D223/16 ,  C07D243/04 ,  C07D491/056 ,  C07D521/00

    CPC分类号： C07D223/16 ,  C07C205/56 ,  C07C45/00 ,  C07C45/513 ,  C07C49/755 ,  C07C57/58 ,  C07C59/64 ,  C07D231/12 ,  C07D233/56 ,  C07D243/04 ,  C07D249/08

    摘要： This invention related to new aminotetralin derivatives of formula I ##STR1## wherein ##STR2## B is methylene or, when A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO-- or --CH.sub.2 --CO--, B can also be carbonyl or thiocarbonyl;E is a C.sub.2 -C.sub.4 straight-chain alkylene, optionally substituted by a C.sub.1 -C.sub.3 alkyl, or is 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;R.sub.1 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, nitro, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylthio, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkoxy phenyl C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkyl or, together with R.sub.1, can be a C.sub.1 -C.sub.2 alkylenedioxy;R.sub.3 and R.sub.4 are each independently selected from hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, nitro, amino, C.sub.1 -C.sub.3 alkylamino, or C.sub.1 -C.sub.3 dialkylamino, or together can be methylenedioxy; andR.sub.5 is hydrogen, C.sub.3 -C.sub.5 alkenyl, C.sub.1 -C.sub.3 alkyl, or phenyl C.sub.1 -C.sub.3 alkyl, and nontoxic, pharmaceutically acceptable addition salts thereof which have valuable pharmacological properties, particularly a long-lasting heart rate lowering effect and the effect of reducing the O.sub.2 requirement of the heart.

    摘要翻译： 本发明涉及新的式I的氨基蝶呤衍生物，其中B是亚甲基，或当A是-CH 2 -CH 2 - 时，-CH = CH-，-NH-CO-或-CH 2 -CO-，B也可以是羰基或硫代羰基; E是任选被C 1 -C 3烷基取代的C 2 -C 4直链亚烷基，或是2-羟基 - 正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯; R1是氢，氟，氯，溴，三氟甲基，硝基，氨基，C1-C3烷基氨基，C1-C3二烷基氨基，C1-C3烷基，C1-C3烷硫基，羟基，C1-C3烷氧基或苯基C1-C3烷氧基; R2是氢，氯，溴，羟基，C1-C3烷氧基苯基C1-C3烷氧基或C1-C3烷基，或与R1一起可以是C1-C2亚烷基二氧基; R 3和R 4各自独立地选自氢，氟，氯，溴，C 1 -C 3烷基，羟基，C 1 -C 3烷氧基，硝基，氨基，C 1 -C 3烷基氨基或C 1 -C 3二烷基氨基，或一起可以是亚甲二氧基; 并且R 5是氢，C 3 -C 5烯基，C 1 -C 3烷基或苯基C 1 -C 3烷基，以及其无毒的药学上可接受的加成盐，其具有有价值的药理学性质，特别是持久的心率降低效果和降低 心脏的O2要求。

    Novel indole derivatives and pharmaceutical compositions containing same
    9.
    发明授权
    Novel indole derivatives and pharmaceutical compositions containing same 失效
    新型吲哚衍生物和含有它们的药物组合物

    公开(公告)号：US4616011A

    公开(公告)日：1986-10-07

    申请号：US675084

    申请日：1984-11-26

    申请人： Manfred Reiffen ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    发明人： Manfred Reiffen ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/55 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P25/02 ,  C07C59/64 ,  C07D209/14 ,  C07D209/16 ,  C07D209/18 ,  C07D223/16 ,  C07D403/12 ,  C07D405/14

    CPC分类号： C07D223/16 ,  C07C59/64 ,  C07D209/16 ,  C07D209/18 ,  C07D403/12

    摘要： This invention relates to novel indole derivatives of the formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## group and B represents a methylene, carbonyl, or thiocarbonyl group or A represents a --CO--CO-- or ##STR3## group and B represents a methylene group, E represents an alkylene group or a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene, or 3-hydroxy-n-butylene group,G represents an alkylene group,R.sub.1 represents a hydrogen, chlorine, or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine, or bromine atom or a hydroxyl, alkoxy, phenylalkoxy, or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen, chlorine, or bromine atom or an alkyl group,R.sub.4 represents a hydrogen atom or an alkyl or phenylalkyl group,R.sub.5 represents a hydrogen, fluorine, chlorine, or bromine atom or an alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.6 represents a hydrogen atom or an alkoxy group, andR.sub.7 represents a hydrogen atom or an alkenyl, alkyl or phenylalkyl group,and the acid additional salts thereof. These compounds, which may be obtained by use of known methods, have valuable pharmacological properties, particularly a heart rate-lowering activity.

    摘要翻译： 本发明涉及式（I）的新的吲哚衍生物，其中A代表-CH2-CH2-，-CH = CH-，IMA组，B代表亚甲基，羰基或硫代羰基，或A代表 -CO-CO-或基，B表示亚甲基，E表示亚烷基或2-羟基正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯基 ，G表示亚烷基，R 1表示氢，氯或溴原子或三氟甲基，硝基，氨基，烷基氨基，二烷基氨基，烷基，羟基，烷氧基或苯基烷氧基，R 2表示氢，氯或溴原子或 羟基，烷氧基，苯基烷氧基或烷基，或者R 1和R 2一起表示亚烷基二氧基，R 3表示氢，氯或溴原子或烷基，R 4表示氢原子或烷基或苯基烷基，R 5表示 氢，氟，氯或溴原子或烷基，羟基，烷氧基或苯基烷氧基，R6代表 氢原子或烷氧基，R7表示氢原子或烯基，烷基或苯基烷基，及其酸加成盐。 可以通过使用已知方法获得的这些化合物具有有价值的药理学性质，特别是心率降低活性。

    (Aminoalkoxy-aryl)-substituted isoquinolinones and naphthydrinones and salts thereof, and hypotensive compositions and methods employing them
    10.
    发明授权
    (Aminoalkoxy-aryl)-substituted isoquinolinones and naphthydrinones and salts thereof, and hypotensive compositions and methods employing them 失效
    （氨基烷氧基 - 芳基） - 取代的异喹啉酮和萘啶酮及其盐，以及使用它们的低血压组合物和方法

    公开(公告)号：US4154837A

    公开(公告)日：1979-05-15

    申请号：US867308

    申请日：1978-01-06

    申请人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Jurgen Dammgen ,  Walter Kobinger ,  Christian Lillie

    发明人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Jurgen Dammgen ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/444 ,  A61K31/47 ,  A61K31/472 ,  A61P9/00 ,  A61P9/12 ,  C07D217/24 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D217/24

    摘要： Compounds of the formula ##STR1## wherein A is benzo, mono-, di- or tri-substituted benzo, the substituents being selected from the group consisting of lower alkoxy, amino and nitro, or pyrido;R.sub.1 is hydrogen or lower alkyl;R.sub.2 is alkyl of 1 to 6 carbon atoms or --X--R.sub.6, where X is straight alkylene of 1 to 4 carbon atoms or hydroxy-substituted straight alkylene of 1 to 4 carbon atoms; andR.sub.6 is amino; carbalkoxy of 2 to 6 carbon atoms; phenyl; mono-, di- or tri-substituted phenyl, the substituents being selected from the group consisting of lower alkyl and lower alkoxy; phenoxy; or mono-, di- or tri-substituted phenoxy, the substituents being selected from the group consisting of lower alkyl and lower alkoxy;R.sub.3 is hydrogen or hydroxyl;R.sub.4 is hydrogen, lower alkyl or lower alkoxy;R.sub.5 is hydrogen or lower alkyl; andN is 0, 1 or 2;And non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as antiarrhythmics, .beta.-adrenergic-receptor blockers and anti-anginous agents.

    摘要翻译： 其中A是苯并，一或二取代或三取代的苯并，其取代基选自低级烷氧基，氨基和硝基，或吡啶并。 R1是氢或低级烷基; R2是1至6个碳原子的烷基或-X-R6，其中X是1至4个碳原子的直链亚烷基或1至4个碳原子的羟基取代的直链亚烷基; R6为氨基; 2至6个碳原子的烷氧基; 苯基; 单取代，二取代或三取代的苯基，所述取代基选自低级烷基和低级烷氧基; 苯氧基 或单 - ，二 - 或三 - 取代的苯氧基，所述取代基选自低级烷基和低级烷氧基; R3是氢或羟基; R4是氢，低级烷基或低级烷氧基; R5是氢或低级烷基; 和N IS 0，1或2; 和非毒性，药理学上可接受的酸添加量。 化合物和盐可用作抗心律失常药，β-肾上腺素能受体阻断剂和抗麻痹剂。