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193 条记录 (耗时 0.016 秒)

    1-Methyl-5-nitro-(2-substituted)-2H-imidazole derivatives, and use as bactericidal and protozoacidal agents
    86.
    发明授权
    1-Methyl-5-nitro-(2-substituted)-2H-imidazole derivatives, and use as bactericidal and protozoacidal agents 失效
    1-甲基-5-硝基 - （2-取代的）-2H-咪唑衍生物，并用作杀菌剂和原生动物剂

    公开(公告)号：US4476138A

    公开(公告)日：1984-10-09

    申请号：US513915

    申请日：1983-07-14

    申请人： Juan B. A. Scalesciani

    发明人： Juan B. A. Scalesciani

    IPC分类号： A61K31/415 ,  A61P31/04 ,  A61P33/02 ,  C07D233/84 ,  C07D233/94 ,  C07D233/22

    CPC分类号： C07D233/94

    摘要： A description is given of new compounds of structural formula: ##STR1## in which R is alkyl and R.sub.1 is H or alkyl; and a process for preparing these compounds starting from 1-methyl-5-nitro-imidazolyl-2-carboxyaldehyde and o-alkyl-phenols.The new compounds are used as drugs for illnesses deriving from protozoa and anaerobic bacteria.

    摘要翻译： 给出了新的结构式化合物：其中R是烷基，R 1是H或烷基;（I）其中R是烷基， 以及从1-甲基-5-硝基 - 咪唑基-2-羧甲醛和邻烷基苯酚开始制备这些化合物的方法。 新化合物被用作来自原生动物和厌氧细菌的疾病的药物。

    Process for the preparation of 2-substituted-alkyl-1-alkyl-nitroimidazoles
    88.
    发明授权
    Process for the preparation of 2-substituted-alkyl-1-alkyl-nitroimidazoles 失效
    2-取代 - 烷基-1-烷基 - 硝基咪唑的制备方法

    公开(公告)号：US4267349A

    公开(公告)日：1981-05-12

    申请号：US119926

    申请日：1980-02-08

    申请人： Helmut Hagen ,  Rolf-Dieter Kohler

    发明人： Helmut Hagen ,  Rolf-Dieter Kohler

    IPC分类号： C07D233/92 ,  C07D233/93 ,  C07D233/94

    CPC分类号： C07D233/92 ,  C07D233/93 ,  C07D233/94

    摘要： Novel 2-substituted 1-alkyl-nitroimidazoles and a process for their preparation by reaction of 2-methyl-nitroimidazoles with oxalic acid diesters, followed by reaction of the resulting nitroimidazol-2-yl-pyruvic acid esters with chlorine, in turn followed, if desired, by reaction of the resulting 2-dihalomethyl-nitroimidazoles with water.Both the novel and the known compounds obtainable by the process of the invention are valuable starting materials for the preparation of dyes, pesticides and drugs.

    摘要翻译： 新的2-取代的1-烷基 - 硝基咪唑及其通过2-甲基 - 硝基咪唑与草酸二酯反应制备的方法，然后将所得的硝基咪唑-2-基 - 丙酮酸酯与氯反应， 如果需要，通过所得2-二卤代甲基 - 硝基咪唑与水的反应。 通过本发明的方法获得的新颖和已知的化合物都是用于制备染料，农药和药物的有价值的起始材料。

    Imidazole ethyl oxyalkoxy derivatives and thio analogues thereof
    89.
    发明授权
    Imidazole ethyl oxyalkoxy derivatives and thio analogues thereof 失效
    咪唑乙氧基烷氧基衍生物及其硫代类似物

    公开(公告)号：US4177350A

    公开(公告)日：1979-12-04

    申请号：US950825

    申请日：1978-10-12

    申请人： Ludwig Zirngibl ,  Kurt Thiele

    发明人： Ludwig Zirngibl ,  Kurt Thiele

    IPC分类号： A61K31/415 ,  A61P31/04 ,  C07D233/60 ,  C07D233/64 ,  C07D233/94 ,  C07D401/12 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07C323/00 ,  C07D233/56 ,  C07D233/94 ,  C07D249/08 ,  Y10S514/962 ,  Y10S514/967 ,  Y10S514/969

    摘要： Antimycotically and antibacterially effective imidazole derivatives of the formula (1) ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen and lower alkyl; R.sup.4 is hydrogen, lower alkyl or selected from unsubstituted or substituted cycloalkyl, benzyl and phenyl groups wherein the substituents are selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, phenyl, cyano, nitro and amino, or wherein R.sup.4 is an unsubstituted or halosubstituted pyridyl, R.sup.5 is nitro or lower alkyl in any unsubstituted position of the imidazole ring, Ar is a phenyl group optionally substituted with at least one substituent which is halogen, lower alkyl, lower alkoxy or a C.sub.4 -C.sub.8 cycloalkyl, or wherein Ar is a benzyl group optionally substituted with a substituent of the type set forth for R.sup.4, X and Y are independently selected from oxygen (--O--) or sulfur (--S), n is an integer of from 1 to 5 inclusive and p is Zero or an integer of from 1 to 3 inclusive, and the addition salts of formula (1) compounds with pharmaceutically acceptable organic or inorganic acids; the formula (1) compounds and their addition salts as specified have a relatively low oral toxicity or/and an improved solubility and are suitable for use in human and veterinary medicine and for chemo-agricultural fungus control purposes. Suitable pharmaceutical compositions including the novel derivatives or/and their addition salts with acceptable acids as well as methods for producing such novel derivatives are disclosed.

    摘要翻译： 式（1）的抗真菌和抗菌有效的咪唑衍生物其中R 1，R 2和R 3相同或不同，为氢和低级烷基; R4是氢，低级烷基或选自未取代或取代的环烷基，苄基和苯基，其中取代基选自卤素，低级烷基，低级烷氧基，低级烷硫基，苯基，氰基，硝基和氨基，或其中R4是未取代或未取代的 卤素取代的吡啶基，R5是咪唑环的任何未取代的位置的硝基或低级烷基，Ar是任选被至少一个取代基取代的苯基，该取代基是卤素，低级烷基，低级烷氧基或C 4 -C 8环烷基，或其中Ar是 任选被R4，X和Y所示类型的取代基取代的苄基独立地选自氧（-O-）或硫（-S），n为1至5的整数，p为零 或1〜3的整数，式（1）化合物与药学上可接受的有机酸或无机酸的加成盐; 式（1）化合物及其加成盐具有相对较低的口服毒性或/和改善的溶解性，适用于人兽药和化学农药真菌控制目的。 公开了包括新型衍生物和/或其与可接受的酸的加成盐的合适的药物组合物以及用于制备这些新型衍生物的方法。

    Nitroimidazoles
    90.
    发明授权
    Nitroimidazoles 失效
    硝基咪唑

    公开(公告)号：US4080340A

    公开(公告)日：1978-03-21

    申请号：US723414

    申请日：1976-09-15

    申请人： Peter Kulsa ,  Clarence S. Rooney

    发明人： Peter Kulsa ,  Clarence S. Rooney

    IPC分类号： C07D233/94 ,  C07D233/95 ,  C07D413/14

    CPC分类号： C07D233/95 ,  C07D233/94

    摘要： Novel substituted nitroimidazoles are provided, for example, 2-(4,5-substituted-isoxazol-3-yl)-1-substituted-5-nitroimidazole; 2-(4,5-disubstituted-.DELTA..sup.2 -isoxazolin-3-yl)-1-substituted-5-nitroimidazole; or 2-(4,5-disubstituted-2-loweralkyl-isoxazolidin-3-yl)-1-substituted-5-nitroimidazole. These compounds have antibacterial and antiprotozoal activity especially against human and animal trypanosomiasis and trichomoniasis.

    摘要翻译： 提供新的取代的硝基咪唑，例如2-（4,5-取代的 - 异恶唑-3-基）-1-取代-5-硝基咪唑; 2-（4,5-二取代的-TATA 2-异恶唑啉-3-基）-1-取代-5-硝基咪唑; 或2-（4,5-二取代-2-低级烷基 - 异恶唑烷-3-基）-1-取代-5-硝基咪唑。 这些化合物具有抗菌和抗原虫活性，特别是针对人和动物锥虫病和毛滴虫病。