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    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof
    13.
    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.

    Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of them to treat certain heart and circulatory diseases
    14.
    发明授权
    Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of them to treat certain heart and circulatory diseases 失效
    吡咯并苯并咪唑，含有它们的药物组合物，以及它们用于治疗某些心脏和循环系统疾病

    公开(公告)号：US4710510A

    公开(公告)日：1987-12-01

    申请号：US807260

    申请日：1985-12-10

    申请人： Alfred Mertens ,  Jens-Peter Holck ,  Wolfgang Kampe ,  Bernd Muller-Beckmann ,  Klaus Strein ,  Wolfgang Schaumann

    发明人： Alfred Mertens ,  Jens-Peter Holck ,  Wolfgang Kampe ,  Bernd Muller-Beckmann ,  Klaus Strein ,  Wolfgang Schaumann

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61P9/00 ,  A61P9/04 ,  C07D209/34 ,  C07D209/42 ,  C07D487/04 ,  A61K31/55

    CPC分类号： C07D487/04 ,  C07D209/34 ,  C07D209/42

    摘要： The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, each represent a hydrogen atom or an alkanesulphonyloxy, trifluoromethanesulphonyloxy, alkanesulphonylamino, trifluoromethanesulphonylamino, N-alkyl-alkanesulphonylamino, N-alkyl-trifluoromethanesulphonylamino, alkylsulphenylmethyl, alkylsulphinylmethyl or alkylsulphonylmethyl radical, a carbonyl group substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino, a sulphonyl group substituted by amino, alkylamino, dialkylamino or cyclic imino, whereby a methylene group in the 4-position can be replaced by a sulphur or oxygen atom, an alkylcarbonylamino, aminocarbonylamino or alkylaminocarbonylamino radical, an alkylthio, alkylsulphinyl or alkylsulphonyl radical, a nitro, halogen, amino, hydroxyl, alkyl, trifluoromethyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, dialkylamino, 1-imidazolyl or cyano group; X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinyl radical; and T is an oxygen or sulphur atom; 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 pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.

    摘要翻译： 本发明提供了以下通式的新的吡咯并苯并咪唑：其中R 1是氢原子或烷基，烯基或环烷基; R2是氢原子，氰基或烷基或烯基或被羟基，烷基，烷氧基，氨基，烷基氨基，二烷基氨基或肼基取代的羰基或与R1一起形成亚环烷基，或者R 1和R 2一起形成亚烷基或亚环烷基 激进; 可以相同或不同的R 3，R 4和R 5各自表示氢原子或烷磺酰氧基，三氟甲磺酰氧基，烷磺酰氨基，三氟甲磺酰氨基，N-烷基 - 烷磺酰氨基，N-烷基 - 三氟甲磺酰氨基，烷基亚磺酰基甲基，烷基亚磺酰基甲基或烷基磺酰基甲基，羰基 被羟基，烷氧基，氨基，烷基氨基或二烷基氨基取代的基团，被氨基，烷基氨基，二烷基氨基或环状亚氨基取代的磺酰基，其中4-位中的亚甲基可以被硫或氧原子，烷基羰基氨基，氨基羰基氨基 或烷基氨基羰基氨基，烷硫基，烷基亚磺酰基或烷基磺酰基，硝基，卤素，氨基，羟基，烷基，三氟甲基，烷氧基，烯氧基，炔氧基，氰基烷氧基，羧基烷氧基，烷氧基羰基烷氧基，二烷基氨基，1-咪唑基或氰基; X是价键，C1-C4亚烷基或乙烯基; 和T是氧或硫原子; 其互变异构体及其与无机和有机酸的生理上可接受的盐。 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用于预防和治疗心脏和循环系统疾病。

    Tricyclic aminoalkyl derivatives
    15.
    发明授权
    Tricyclic aminoalkyl derivatives 失效
    三环氨基烷基衍生物

    公开(公告)号：US4070373A

    公开(公告)日：1978-01-24

    申请号：US291426

    申请日：1972-09-22

    申请人： Werner Winter ,  Max Thiel ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Wolfgang Schaumann ,  Karl Dietmann

    发明人： Werner Winter ,  Max Thiel ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Wolfgang Schaumann ,  Karl Dietmann

    IPC分类号： C07D311/90 ,  C07D313/12 ,  C07D337/12 ,  C07D337/16

    CPC分类号： C07D337/16 ,  C07D311/90 ,  C07D313/12 ,  C07D337/12 ,  C07C2103/18

    摘要： Novel tricyclic aminoalkyl derivatives are disclosed which are characterized by valuable pharmacological activities and namely by cardiac and circulatory activities. The tricyclic aminoalkyl derivatives are compounds of the formula: ##STR1## wherein X is an oxygen or a sulfur atom, a saturated or unsaturated, straight chain or branched alkylene group containing up to 3 carbon atoms, an oxymethylene, thiamethylene or thiaethylene group or a valency bond, R.sub.1 is hydrogen, halogen, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen or hydroxyl, R.sub.3 is hydrogen or together with R.sub.2 represents a further valency bond, R.sub.4 and R.sub.5 which may be the same or different are each hydrogen or lower alkyl, A is alkylene which is substituted by an optionally acylated hydroxyl group, Y is an oxygen or sulfur atom or an optionally alkylated imino group and Z is aryl, aralkyl, cycloalkyl or cycloalkyl-alkyl which may be substituted by halogen, hydroxyl, nitro, amino, alkoxy, aralkoxy, alkyl, trifluoromethyl, alkylamino or alkylsulfonyl group, and the acid addition salts thereof with pharmacologically acceptable acids.

    摘要翻译： 公开了新颖的三环氨基烷基衍生物，其特征在于有价值的药理活性，即通过心脏和循环活性。 三环氨基烷基衍生物是下式的化合物：其中X是氧或硫原子，含有至多3个碳原子的饱和或不饱和的直链或支链亚烷基，亚甲基，亚亚甲基或亚硫代亚乙基或 化合键，R 1是氢，卤素，烷基，烷氧基或三氟甲基，R 2是氢或羟基，R 3是氢或与R 2一起代表另外的价键，可以相同或不同的R 4和R 5各自是氢或低级烷基 A是被任意酰化的羟基取代的亚烷基，Y是氧或硫原子或任选烷基化的亚氨基，Z是可以被卤素，羟基，硝基取代的芳基，芳烷基，环烷基或环烷基 - 烷基， 氨基，烷氧基，芳烷氧基，烷基，三氟甲基，烷基氨基或烷基磺酰基，及其与药理学上可接受的酸的酸加成盐。

    Nitropyrazole compounds and anti-microbial compositions
    16.
    发明授权
    Nitropyrazole compounds and anti-microbial compositions 失效
    硝基吡唑化合物和抗微生物组合物

    公开(公告)号：US4069330A

    公开(公告)日：1978-01-17

    申请号：US678588

    申请日：1976-04-20

    申请人： Herbert Berger ,  Rudi Gall ,  Max Thiel ,  Wolfgang Schaumann ,  Wolfgang Vomel

    发明人： Herbert Berger ,  Rudi Gall ,  Max Thiel ,  Wolfgang Schaumann ,  Wolfgang Vomel

    IPC分类号： G09F7/02 ,  C07D231/16 ,  G09F3/20 ,  H01B7/36 ,  H01R13/46 ,  A61K31/415

    CPC分类号： H01B7/368 ,  C07D231/16

    摘要： New nitropyrazole compounds of the formula ##STR1## wherein R.sub.1 is alkyl or hydroxyalkylR.sub.2 and R.sub.3, which may be the same or different, are alkyl orR.sub.2 and R.sub.3 together represent a 4- or 5-membered alkylene bridge which is optionally interrupted by an oxygen atom or by the grouping >N-R, in which R is an alkyl or hydroxyalkyl radical;And the pharmacologically compatible salts thereof, possess excellent anti-microbial action not only in vitro but also in vivo, especially systemically.

    摘要翻译： 其中R 1是烷基或羟基烷基的新的硝基吡唑化合物，其可以相同或不同，R 2和R 3可以是烷基或R 2和R 3一起代表4-或5-元亚烷基桥，其任选地被 氧原子或通过NR> NR，其中R是烷基或羟烷基; 和药物相容性好的药物，不仅仅是体内，而且在体内非常有效地进行非常有效的抗微生物作用。

    "> Ketals of 3'
    19.
    发明授权
    Ketals of 3'"-dehydrocardenolide tridigitoxosides 失效
    3“ - 脱氢伐内酰氯沙多昔多糖的水分

    公开(公告)号：US4436735A

    公开(公告)日：1984-03-13

    申请号：US439653

    申请日：1982-11-05

    申请人： Wolfgang Schaumann ,  Fritz Kaiser ,  Wolfgang Voigtlander ,  Edgar Hoyer ,  Peter Neubert

    发明人： Wolfgang Schaumann ,  Fritz Kaiser ,  Wolfgang Voigtlander ,  Edgar Hoyer ,  Peter Neubert

    IPC分类号： A61K31/704 ,  A61P9/00 ,  C07J19/00 ,  A61K31/585

    CPC分类号： C07J19/005

    摘要： The present invention provides ketals of 3'"-dehydrocardenolide tridigitoxosides of the general formula: ##STR1## in which R.sub.1 and R.sub.2 are identical alkyl radicals containing up to 3 carbon atoms or together represent a cyclic ketal containing 2 to 6 carbon atoms, R.sub.3 represents two hydrogen atoms, the group ##STR2## or the radical ##STR3## wherein R.sub.1 and R.sub.2 have the above-given meaning, and R.sub.4 is a hydrogen atom or a lower acyl or alkyl radical.The present invention also provides processes for the preparation of these ketals, as well as pharmaceutical compositions containing them, which are useful for the treatment of cardiac insufficiency.

    摘要翻译： 本发明提供了通式为：其中R 1和R 2是含有至多3个碳原子的相同烷基或一起代表含有2至6个碳原子的环状缩酮的3“ - 脱氢伐尼洛德三唑一硫酮的缩酮 原子，R 3表示两个氢原子，基团或基团，其中R 1和R 2具有上述含义，并且R 4是氢原子或低级酰基或烷基。 本发明还提供了制备这些缩酮的方法以及含有它们的药物组合物，其可用于治疗心功能不全。