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    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof
    3.
    发明授权
    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof 失效

    公开(公告)号：US4642309A

    公开(公告)日：1987-02-10

    申请号：US780704

    申请日：1985-09-26

    申请人： Helmut Michel ,  Klaus Marzenell ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Wolfgang Schaumann

    发明人： Helmut Michel ,  Klaus Marzenell ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Wolfgang Schaumann

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P9/08 ,  A61P25/02 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06

    摘要： The present invention provides indolin-2-one derivatives of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl radical or a radical of the general formula: ##STR2## in which A is a straight-chained or branched C.sub.2 -C.sub.4 alkylene radical and Z is an oxygen or sulphur atom, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, C.sub.2 -C.sub.6 alkanoyl radicals, C.sub.2 -C.sub.4 alkenyl radicals, C.sub.2 -C.sub.4 alkynyl radicals, C.sub.1 -C.sub.6 alkyl radicals, C.sub.1 -C.sub.6 alkoxy radicals, C.sub.2 -C.sub.4 alkenyloxy radicals, C.sub.2 -C.sub.4 alkynyloxy radicals, C.sub.1 -C.sub.6 alkylthio radicals, C.sub.2 -C.sub.6 alkanoylamido radicals or radicals of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 alkyl radicals or C.sub.3 -C.sub.10 cycloalkyl radicals or R.sub.4 and R.sub.5 together represent a C.sub.2 -C.sub.8 alkylene radical optionally interrupted by an oxygen or sulphur atom or by an >N-R.sub.6 group, in which R.sub.6 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical, X is a hydrogen atom, Y is a hydrogen atom or a group of the general formula ##STR4## in which Q is a hydrogen atom or, together with X, can also represent a bond and R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxyl or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by halogen, hydroxyl, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulphinyl, C.sub.1 14 C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, methylenedioxy, nitro, cyano or amino, with the proviso that R.sub.1 cannot be a C.sub.1 -C.sub.6 alkyl radical when X and Y are both hydrogen atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides intermediates of the general formula: ##STR5## in which R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxy or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by hydroxyl, halogen, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 14 C.sub.6 alkylsulphinyl, cyano C.sub.1 -C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, nitro amino or methylenedioxy.Furthermore, the invention provides processes for the preparation of the above indolin-2-one derivatives and the above intermediates, as well as pharmaceutical compositions containing the above indolin-2-one derivatives.

    3-Cyano indoles as intermediates for cardioselective compounds
    5.
    发明授权
    3-Cyano indoles as intermediates for cardioselective compounds 失效
    3-氰基吲哚作为心脏选择性化合物的中间体

    公开(公告)号：US4442295A

    公开(公告)日：1984-04-10

    申请号：US288077

    申请日：1981-07-29

    申请人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch

    发明人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42 ,  C07D209/43 ,  C07D405/12 ,  C07D209/04

    CPC分类号： C07D405/12 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42

    摘要： The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, an aralkyl radical or a radical of the general formula: ##STR2## in which B is a reactive group or, together with R.sub.5, represents a valency bond, and R.sub.5 is a hydrogen atom or an aliphatic or aromatic acyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen atom, a methyl radical or a --CH.sub.2 --O--R.sub.5 radical, R.sub.5 having the same meaning as above, and R.sub.4 is an aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, with the proviso that R.sub.1 is not an aralkyl radical when R.sub.4 is a formyl radical. The present invention also provides processes for the preparation of these compounds. Furthermore, the present invention is concerned with the use of these compounds for the preparation of compounds with a heart and circulatory activity.

    摘要翻译： 本发明提供以下通式的吲哚衍生物：其中R 1是氢原子，芳烷基或具有以下通式的基团：其中B是反应性基团，或与R 5一起 表示价键，R5表示氢原子或脂肪族或芳香族酰基，R2表示氢原子或低级烷基，R3表示氢原子，甲基或-CH2-O-R5基， R5具有与上述相同的含义，R4是氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基，条件是当R 4是甲酰基时，R 1不是芳烷基。 本发明还提供了这些化合物的制备方法。 此外，本发明涉及这些化合物用于制备具有心脏和循环活性的化合物的用途。

    3-Cyano-indoles as cardioselective agents
    6.
    发明授权
    3-Cyano-indoles as cardioselective agents 失效
    3-氰基 - 吲哚作为心脏选择剂

    公开(公告)号：US4468520A

    公开(公告)日：1984-08-28

    申请号：US288075

    申请日：1981-07-29

    申请人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch ,  Karl Dietmann ,  Gisbert Sponer

    发明人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch ,  Karl Dietmann ,  Gisbert Sponer

    IPC分类号： C07D209/12 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  C07D209/08 ,  C07D209/42 ,  C07D209/43 ,  C07D209/04

    CPC分类号： C07D209/08

    摘要： The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for the prophylaxis and treatment of heart and circulatory diseases.

    摘要翻译： 本发明提供以下通式的氨基丙醇衍生物：其中R1是氢原子或低级烷酰基或芳酰基，R2是低级烷基或通式如下的基团：其中 X是价键，亚甲基或氧或硫原子，Ar是单环，碳或杂环芳基，R6和R7可以相同或不同，是氢原子或低级烷基，R8和 R9可相同或不同，为氢或卤原子，羟基，低级烷酰基，烯基，炔基，烷基，低级烷氧基，芳烷氧基，烯氧基，炔氧基，低级烷硫基，氨基羰基 自由基，氨基磺酰基或酰氨基; 或R 2为1,4-苯并二恶烷-2-基甲基，R'2为氢原子或苄基，R 3为羧基或低级烷氧基羰基，氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基 R4是氢原子或低级烷基或-CH2-O-R1基，R1具有与上述相同的含义，R 5是氢原子或低级烷基; 其任选活性形式和外消旋物及其药理学上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。 此外，本发明涉及这些化合物用于预防和治疗心脏和循环系统疾病的用途。

    Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof
    9.
    发明授权
    Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof 失效
    含有硝基烷基胺，新型硝基烷基胺的药物组合物及其制备方法

    公开(公告)号：US5037849A

    公开(公告)日：1991-08-06

    申请号：US424452

    申请日：1989-10-20

    申请人： Herbert Simon ,  Helmut Michel ,  Michael Schultz ,  Wolfgang Bartsch

    发明人： Herbert Simon ,  Helmut Michel ,  Michael Schultz ,  Wolfgang Bartsch

    IPC分类号： A61K31/21 ,  A61K31/395 ,  A61K31/40 ,  A61K31/445 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07C235/10 ,  C07C235/26 ,  C07C235/40 ,  C07C237/08 ,  C07C237/18 ,  C07C275/10 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07D211/06 ,  C07D295/13 ,  C07D295/14 ,  C07D295/215

    CPC分类号： C07D295/215 ,  A61K31/21 ,  C07C235/10 ,  C07C235/26 ,  C07C235/40 ,  C07C237/08 ,  C07C275/10 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07D295/13 ,  C07C2101/14

    摘要： The present invention provides pharmaceutical compositions effective against angina-like heart and circulatory diseases containing at least one nitroxyalkylamine derivative of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower-alkyl radical, a C.sub.3 -C.sub.8 -cycloalkyl or C.sub.3 -C.sub.8 -cycloalkenyl radical, an aminocarbonyl, C.sub.1 -C.sub.6 -mono- or di-alkylaminocarbonyl radical, R.sup.2 is a hydrogen atom, a lower-alkyl radical or a C.sub.3 -C.sub.8 -cycloalkyl or cycloalkenyl radical or R.sup.2, together with R.sup.1 and the nitrogen atom to which they are attached, form a heteroaliphatic ring containing up to 6 carbon atoms, A is a valency bond or a straight-chained or branched lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical, B is a lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical and X is an --NR.sup.3 --CO-- or --CO--NR.sup.3 -- radical, in which R.sup.3 is a hydrogen atom or a lower-alkyl radical, when X is an --NR.sup.3 --CO-- radical, R.sup.3, together with the nitrogen atom and a carbon atom of the group A, bridge a heterocyclic ring containing 4 to 6 carbon atoms or R.sup.3, together with R.sup.2, A and the two nitrogen atoms, bridge a heterocyclic ring containing 3 to 5 carbon atoms; and the optically-active forms and physiologically acceptable salts thereof.

    摘要翻译： 本发明提供了有效抗心绞痛的心脏和循环系统疾病的药物组合物，其含有至少一种以下通式的硝基烷基胺衍生物：其中R 1是氢原子，低级烷基，C 3 -C 8 - 环烷基或C 3 -C 8 - 环烯基，氨基羰基，C 1 -C 6 - 单 - 或二 - 烷基氨基羰基，R 2是氢原子，低级烷基或C 3 -C 8 - 环烷基或环烯基或R 2，连同 R1和它们所连接的氮原子形成含有至多6个碳原子的杂脂族环，A是价键或直链或支链的低级亚烷基，其中-CH 2 - 基团可以被 亚环烷基，B是低级亚烷基，其中-CH 2 - 基团可被亚环烷基代替，X是-NR 3 -CO-或-CO-NR 3 - 基，其中R 3是氢原子 或低级烷基，当X是-NR 3 -CO-基时，R 3与硝基一起形成 原子和A基团的碳原子，桥接含有4至6个碳原子的杂环或R3与R2，A和两个氮原子一起桥接含有3至5个碳原子的杂环; 和其光学活性形式和生理上可接受的盐。