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    Nitropyrazole compounds and anti-microbial compositions
    1.
    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。

    3-Nitropyrazole compounds and anti-microbial compositions
    2.
    发明授权
    3-Nitropyrazole compounds and anti-microbial compositions 失效
    3-硝基吡唑化合物和抗微生物组合物

    公开(公告)号：US4172136A

    公开(公告)日：1979-10-23

    申请号：US889594

    申请日：1978-03-23

    申请人： Herbert Berger ,  Rudi Gall ,  Kurt Stach, deceased ,  Max Thiel ,  Wolfgang Vomel

    发明人： Herbert Berger ,  Rudi Gall ,  Kurt Stach, deceased ,  Max Thiel ,  Wolfgang Vomel

    IPC分类号： C07D231/16 ,  C07D401/02 ,  C07D403/02

    CPC分类号： C07D231/16

    摘要： New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO-NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.

    摘要翻译： 新的具有下式的3-硝基吡唑化合物：其中R 1是低级烷基; R2是氢或低级烷基; R3是氰基，羧基或低级烷氧基羰基或基团-CO-NR4R5，其中R4是氢或羟基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，硫代氨基甲酰基，脲基，硫脲基，羟基苯基，吡啶甲基或是低级烷基，烯基或环烷基取代 如果需要，通过氰基，羟基，吡咯烷子基，哌啶子基，氨基，低级烷基氨基，低级二烷基氨基或低级酰基氨基取代基，R 5是氢原子或低级烷基，或者R 4和R 5一起代表低级亚烷基桥; 并且其药理学兼容的药物作为抗微生物药剂，特别是在系统性和在尿道感染中是非常有效的。

    3-Nitropyrazole compounds and anti-microbial compositions
    3.
    发明授权
    3-Nitropyrazole compounds and anti-microbial compositions 失效
    3-硝基吡唑化合物和抗微生物组合物

    公开(公告)号：US4105772A

    公开(公告)日：1978-08-08

    申请号：US744215

    申请日：1976-11-22

    申请人： Herbert Berger ,  Rudi Gall ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Max Thiel ,  Wolfgang Vomel

    发明人： Herbert Berger ,  Rudi Gall ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Max Thiel ,  Wolfgang Vomel

    IPC分类号： C07D231/16 ,  A61K31/41 ,  C07D231/10

    CPC分类号： C07D231/16

    摘要： New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO--NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof, are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.

    摘要翻译： 新的具有下式的3-硝基吡唑化合物：其中R 1是低级烷基; R2是氢或低级烷基; R3是氰基，羧基或低级烷氧基羰基或基团-CO-NR4R5，其中R4是氢或羟基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，硫代氨基甲酰基，脲基，硫脲基，羟基苯基，吡啶甲基或是低级烷基，烯基或环烷基取代 如果需要，通过氰基，羟基，吡咯烷子基，哌啶子基，氨基，低级烷基氨基，低级二烷基氨基或低级酰基氨基取代基，R 5是氢原子或低级烷基，或者R 4和R 5一起代表低级亚烷基桥; 并且其药理学兼容的药物作为抗微生物剂，特别是在系统性和全球性的治疗中是非常有效的。

    Tricyclic aminoalkyl derivatives
    9.
    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。