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    Disubstituted triphenylmethylmidazoles for treating mycotic infections
    1.
    发明授权
    Disubstituted triphenylmethylmidazoles for treating mycotic infections 失效
    用于治疗肌肉感染的三甲基甲酰胺

    公开(公告)号：US4117142A

    公开(公告)日：1978-09-26

    申请号：US726568

    申请日：1976-09-27

    申请人： Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    发明人： Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    IPC分类号： C07D521/00 ,  A61K31/415

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Imidazoles of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof, wherein X is methyl or chloro,Y is methyl or chloro, or, when Z is methyl or chloro, Y is hydrogen, andZ is methyl or chloro, or, when Y is methyl or chloro, Z is hydrogen,Are useful as antimycotics for the treatment of mycotic infections in humans and animals. The imidazoles may be produced by reacting the corresponding triphenylmethylcarbinol with a brominating or chlorinating agent and thereafter reacting the resultant triphenylmethyl halide, either with or without isolation, with imidazole in the presence or absence of an acid-binding agent, or they may be prepared by reacting a triphenylmethyl halide with imidazole, either in the presence or absence of an acid-binding agent.

    N-methyl-imidazole derivatives for treating mycotic infections
    2.
    发明授权
    N-methyl-imidazole derivatives for treating mycotic infections 失效
    用于治疗真菌感染的N-甲基 - 咪唑衍生物

    公开(公告)号：US4062959A

    公开(公告)日：1977-12-13

    申请号：US554009

    申请日：1975-02-28

    申请人： Wilfried Draber ,  Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    发明人： Wilfried Draber ,  Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    IPC分类号： A61K31/495 ,  A61K31/505 ,  C07D241/12 ,  C07D403/06

    CPC分类号： C07D403/06 ,  A61K31/495 ,  A61K31/505 ,  C07D241/12

    摘要： N-methyl-imidazole derivatives of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof, wherein X is an unsubstituted or substituted 6-membered heteroaromatic moiety having two nitro heteroatoms,Y is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety or an unsubstituted or substituted aryl moiety, andZ is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety, an unsubstituted or substituted aryl moiety, an unsubstituted or substituted pyridyl moiety or an alkoxycarbonyl moiety,Are useful as antimycotic agents.

    摘要翻译： 式（I）的N-甲基 - 咪唑衍生物或其药学上可接受的无毒盐，其中X是具有两个硝基杂原子的未取代或取代的6元杂芳族部分，Y是未取代或取代的脂族 未取代或取代的脂环族部分，未取代或取代的芳烷基部分或未取代或取代的芳基部分，Z为未取代或取代的脂族部分，未取代或取代的脂环族部分，未取代或取代的芳烷基部分，未取代或取代的芳烷基部分， 取代的芳基部分，未取代或取代的吡啶基部分或烷氧基羰基部分，可用作抗生药剂。

    N-methyl-imidazole derivatives as anti-mycotic agents
    4.
    发明授权
    N-methyl-imidazole derivatives as anti-mycotic agents 失效
    N-甲基 - 咪唑衍生物作为抗真菌剂

    公开(公告)号：US3934014A

    公开(公告)日：1976-01-20

    申请号：US474873

    申请日：1974-05-31

    申请人： Wilfried Draber ,  Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    发明人： Wilfried Draber ,  Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    IPC分类号： A61K31/495 ,  A61K31/505 ,  C07D241/12 ,  C07D403/06

    CPC分类号： C07D403/06 ,  A61K31/495 ,  A61K31/505 ,  C07D241/12

    摘要： N-methyl-imidazole derivatives of the formula: ##EQU1## or a pharmaceutically acceptable non-toxic salt thereof, wherein X is an unsubstituted or substituted 6-membered heteroaromatic moiety having two nitro heteroatoms,Y is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety or an unsubstituted or substituted aryl moiety, andZ is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety, an unsubstituted or substituted aryl moiety, an unsubstituted or substituted pyridyl moiety or an alkoxycarbonyl moiety,Are useful as antimycotic agents.

    摘要翻译： 其中X是具有两个硝基杂原子的未取代或取代的6元杂芳族部分，Y是一个 未取代或取代的脂族部分，未取代或取代的脂环族部分，未取代或取代的芳烷基部分或未取代或取代的芳基部分，Z为未取代或取代的脂族部分，未取代或取代的脂环族部分，未取代或取代的芳烷基部分 ，未取代或取代的芳基部分，未取代或取代的吡啶基部分或烷氧基羰基部分，可用作抗生药剂。

    Disubstituted triphenylmethylimidazoles
    5.
    发明授权
    Disubstituted triphenylmethylimidazoles 失效
    分离的三苯基甲基咪唑

    公开(公告)号：US4052409A

    公开(公告)日：1977-10-04

    申请号：US339430

    申请日：1973-03-08

    申请人： Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    发明人： Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    IPC分类号： C07D233/62 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Imidazoles of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof, wherein X is methyl or chloro,Y is methyl or chloro, or, when Z is methyl or chloro, Y is hydrogen, andZ is methyl or chloro, or, when Y is methyl or chloro, Z is hydrogen,Are useful as antimycotics for the treatment of mycotic infections in humans and animals. The imidazoles may be produced by reacting the corresponding triphenylmethylcarbinol with a brominating or chlorinating agent and thereafter reacting the resultant triphenylmethyl halide, either with or without isolation, with imidazole in the presence or absence of an acid-binding agent, or they may be prepared by reacting a triphenylmethyl halide with imidazole, either in the presence or absence of an acid-binding agent.

    N-Methyl-imidazole derivatives for treating mycotic infections
    7.
    发明授权
    N-Methyl-imidazole derivatives for treating mycotic infections 失效
    用于治疗真菌感染的N-甲基 - 咪唑衍生物

    公开(公告)号：US3980780A

    公开(公告)日：1976-09-14

    申请号：US554203

    申请日：1975-02-28

    申请人： Wilfried Draber ,  Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    发明人： Wilfried Draber ,  Karl Heinz Buchel ,  Erik Regel ,  Manfred Plempel

    IPC分类号： A61K31/495 ,  A61K31/505 ,  C07D241/12 ,  C07D403/06

    CPC分类号： C07D403/06 ,  A61K31/495 ,  A61K31/505 ,  C07D241/12

    摘要： N-methyl-imidazole derivatives of the formula: ##EQU1## or a pharmaceutically acceptable non-toxic salt thereof, wherein X is an unsubstituted or substituted 6-membered heteroaromatic moiety having two nitro heteroatoms,Y is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety or an unsubstituted or substituted aryl moiety, andZ is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety, an unsubstituted or substituted aryl moiety, an unsubstituted or substituted pyridyl moiety or an alkoxycarbonyl moiety,Are useful as antimycotic agents.

    摘要翻译： 其中X是具有两个硝基杂原子的未取代或取代的6元杂芳族部分，Y是未取代的或未取代的或未取代的 取代的脂族部分，未取代或取代的脂环族部分，未取代或取代的芳烷基部分或未取代或取代的芳基部分，Z是未取代或取代的脂族部分，未取代或取代的脂环族部分，未取代或取代的芳烷基部分， 未取代或取代的芳基部分，未取代或取代的吡啶基部分或烷氧基羰基部分，作为抗菌剂有用。

    Imidazolylacetic acid amides, their production, antimycotic compositions comprising said compounds and their use as antimycotic agents
    8.
    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

    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 ,  A61K31/54

    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.

    1-Propyl-triazolyl antimycotic compositions and methods of treating mycoses
    10.
    发明授权
    1-Propyl-triazolyl antimycotic compositions and methods of treating mycoses 失效
    1-丙基 - 三唑基抗真菌组合物和治疗真菌病的方法

    公开(公告)号：US4079142A

    公开(公告)日：1978-03-14

    申请号：US638754

    申请日：1975-12-08

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

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

    IPC分类号： C07D249/08 ,  A61K31/41

    CPC分类号： C07D249/08

    摘要： Pharmaceutical compositions are produced which comprise an antimycotically effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable non-toxic salt thereof wherein R.sup.1 is an unsubstituted or substituted aryl moiety,R.sup.2 is hydrogen, alkyl, alkenyl, cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl, andR.sup.3 is hydrogen, alkyl or cycloalkyl,Provided that when R.sup.3 is hydrogen, R.sup.2 cannot be hydrogen, in combination with a pharmaceutically acceptable non-toxic inert diluent or carrier.

    摘要翻译： 制备药物组合物，其包含抗真菌有效量的下式化合物或其药学上可接受的无毒盐，其中R 1是未取代或取代的芳基部分，R 2是氢，烷基，烯基，环烷基，未取代的或未取代的 取代的芳基或未取代或取代的芳烷基，并且R 3是氢，烷基或环烷基，当R3是氢时，R2不能是氢，与药学上可接受的无毒惰性稀释剂或载体组合。