利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

93 条记录 (耗时 0.027 秒)

    Antimycotic compositions containing an imidazolylacetic acid amide or salt thereof as the active agent and the use thereof in the treatment of mycoses
    68.
    发明授权
    Antimycotic compositions containing an imidazolylacetic acid amide or salt thereof as the active agent and the use thereof in the treatment of mycoses 失效
    含有咪唑基乙酰胺或其盐作为活性剂的抗真菌组合物及其在治疗真菌病中的应用

    公开(公告)号：US4024270A

    公开(公告)日：1977-05-17

    申请号：US594195

    申请日：1975-07-09

    申请人： Jurgen Wenzelburger ,  Karl Heinz Buchel ,  Manfred Plempel ,  Werner Meiser

    发明人： Jurgen Wenzelburger ,  Karl Heinz Buchel ,  Manfred Plempel ,  Werner Meiser

    IPC分类号： A61K31/415 ,  C07D417/06

    CPC分类号： C07D417/06 ,  A61K31/415

    摘要： Pharmaceutical compositions useful for treating mycotic infections in humans and animals are produced which comprise an antimycotically effective amount of an imidazolylacetic acid amide of the formula: ##STR1## or pharmaceutically acceptable nontoxic salts thereof WHEREINEitherR.sup.1 is phenyl or cycloalkyl, unsubstituted or substituted by one or more substituents; andR.sup.2 is hydrogen;OrR.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, form a saturated 5 to 7-membered heterocyclic ring which ring may contain an --SO.sub.2 -- or --NY-- moiety wherein Y is alkoxycarbonyl, dialkylaminocarbonyl, or phenyl or diphenylmethyl, unsubstituted or substituted by one or more substituents and wherein said 5 to 7-membered heterocyclic ring itself is otherwise unsubstituted or substituted by one or more substituents; andX.sup.1, x.sup.2, x.sup.3 and X.sup.4 are the same or different and are each hydrogen or halogen,Are produced byA. reacting a halodiphenylacetic acid amide of the formula: ##STR2## wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined, and Hal is hydrogen,With imidazole; orB. reacting a halodiphenylacetic acid halide of the formula: ##STR3## WHEREIN X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined and Hal is hydrogenWith imidazole to produce an imidazolide of the formula: ##STR4## wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above definedwhich in turn is transaminated by reaction with an amine of the formula:NHR.sup.1 R.sup.2whereinR.sup.1 and R.sup.2 are as above defined.

    摘要翻译： 产生用于治疗人和动物中的真菌感染的药物组合物，其包含抗真菌有效量的下式的咪唑基乙酰胺或其药学上可接受的无毒盐，其中R1是未取代或被一个取代的苯基或环烷基 或更多取代基; R2是氢; OR R1和R2与它们连接的氮原子一起形成饱和的5至7元杂环，该环可以含有-SO 2 - 或-NY-部分，其中Y是烷氧基羰基，二烷基氨基羰基或苯基或二苯基甲基 未取代或被一个或多个取代基取代，并且其中所述5至7元杂环本身是未取代的或被一个或多个取代基取代; 并且X 1，X 2，X 3和X 4相同或不同，各自为氢或卤素，由A制备。反应式为二氢苯甲酸的酰胺：其中R 1，R 2，X 1，X 2，X 3和X 4为 如上所定义，Hal是氢，具有咪唑; 或B.反应式中的卤代苯甲酸：其中X 1，X 2，X 3和X 4如上所定义，Hal是具有咪唑并氢的氢，以制备式I的咪唑烷：其中X1，X2，X3 和X 4如上所定义，其又通过与下式的胺反应进行转氨：

    1,2,4-Triazole antimycotic compositions and use thereof
    69.
    发明授权
    1,2,4-Triazole antimycotic compositions and use thereof 失效
    1,2,4-三唑抗真菌组合物及其用途

    公开(公告)号：US4002763A

    公开(公告)日：1977-01-11

    申请号：US532191

    申请日：1974-12-12

    申请人： Werner Meiser ,  Wolfgang Kramer ,  Karl Heinz Buchel ,  Manfred Plempel

    发明人： Werner Meiser ,  Wolfgang Kramer ,  Karl Heinz Buchel ,  Manfred Plempel

    IPC分类号： C07D249/08 ,  A61K31/41

    CPC分类号： C07C45/71 ,  C07C45/004 ,  C07C45/63 ,  C07C45/70 ,  C07D249/08

    摘要： Antimycotic compositions are produced which comprise an antimycotically effective amount of a 1,2,4-triazole of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof wherein X.sup.1 is hydrogen or alkyl;X.sup.2 is hydrogen or alkyl;R.sup.1 is alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl;R.sup.2 is hydrogen, alkyl or unsubstituted or substituted aryl;R.sup.3 is alkyl, cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl; andY is a keto group of a functional derivative of a keto group, in combination with a pharmaceutically acceptable non-toxic, inert diluent or carrier.

    摘要翻译： 产生抗真菌组合物，其包含抗真菌有效量的下式的1,2,4-三唑或其药学上可接受的无毒盐，其中X 1是氢或烷基; X2是氢或烷基; R1是烷基，未取代或取代的芳基或未取代或取代的芳烷基; R2是氢，烷基或未取代或取代的芳基; R3是烷基，环烷基，未取代或取代的芳基或未取代或取代的芳烷基; 和Y是酮基的功能性衍生物的酮基，其与药学上可接受的无毒惰性稀释剂或载体的组合。