1,2,4-Triazole antimycotic compositions and use thereof
    3.
    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

    IPC分类号: C07D249/08 A61K31/41

    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。

    1,2,4-Triazole antimycotic compositions and use thereof
    6.
    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:US4036967A

    公开(公告)日:1977-07-19

    申请号:US645946

    申请日:1976-01-02

    IPC分类号: C07D249/08 A61K31/41

    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 or 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是酮基或酮基的官能衍生物,与药学上可接受的无毒惰性稀释剂或载体组合。

    Imidazolylacetic acid amides, their production, antimycotic compositions
comprising said compounds and their use as antimycotic agents
    9.
    发明授权
    Imidazolylacetic acid amides, their production, antimycotic compositions comprising said compounds and their use as antimycotic agents 失效
    咪唑啉酸,它们的生产,含有化合物的抗微生物组合物及其作为抗菌剂的用途

    公开(公告)号:US4032636A

    公开(公告)日:1977-06-28

    申请号:US651419

    申请日:1976-01-22

    CPC分类号: C07D417/06 A61K31/415

    摘要: Imidazolylacetic acid amides of the formula: ##STR1## or pharmaceutically acceptable nontoxic salts thereof wherein either R.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 halogen,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 halogenWith 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 defined which 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.