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    Antimycotic compositions
    21.
    发明授权
    Antimycotic compositions 失效
    抗真菌组合物

    公开(公告)号：US3968229A

    公开(公告)日：1976-07-06

    申请号：US481660

    申请日：1974-06-21

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

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

    IPC分类号： A61K31/415 ,  A61P31/04 ,  C07D233/60 ,  C07D521/00

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

    摘要： Pharmaceutical compositions are produced which comprise combining an antimycotically effective amount of a compound of the formula ##EQU1## or a pharmaceutically acceptable, nontoxic salt thereof, wherein R.sup.1 is unsubstituted or substituted aryl,R.sup.2 is hydrogen, alkyl or unsubstituted or substituted aryl,R.sup.3 is hydrogen, alkyl, cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl, andR.sup.4 is hydrogen, alkyl, alkenyl, cycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted aralkyl,Provided that R.sup.3 and R.sup.4 are not both hydrogen atoms, in combination with a pharmaceutically-acceptable, nontoxic, inert diluent or carrier.

    摘要翻译： 制备药物组合物，其包括组合抗真菌有效量的式R 2 OH || R1O-CC-R4 | R3化合物或其药学上可接受的无毒盐，其中R 1为未取代或取代的芳基，R 2为氢，烷基或 未取代或取代的芳基，R3为氢，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，R4为氢，烷基，烯基，环烷基，未取代或取代的芳基或未取代或取代的芳烷基，提供R3和R4 不是氢原子，与药学上可接受的，无毒的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
    24.
    发明授权
    Imidazolylacetic acid amides, their production, antimycotic compositions comprising said compounds and their use as antimycotic agents 失效
    咪唑基乙酸酰胺，它们的生产，包含所述化合物的抗真菌组合物及其作为抗真菌剂的用途

    公开(公告)号：US4033964A

    公开(公告)日：1977-07-05

    申请号：US594569

    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 ,  C07D403/12

    CPC分类号： C07D417/06 ,  A61K31/415

    摘要： Imidazolylacetic acid amides of the formula: ##STR1## or pharmaceutically acceptable nontoxic salts thereof WHEREIN EITHERR.sup.1 is phenyl or cycloalkyl, unsubstituted or substituted by one or more substituents; andR.sup.2 is hydrogen;OrR.sup.1 or 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, and 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 andHal is halogen with 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.2 whereinR.sup.1 and R.sup.2 are as above defined.

    摘要翻译： 下式的咪唑基乙酸酰胺或其药学上可接受的无毒盐，其中R1是未被取代或被一个或多个取代基取代的苯基或环烷基; R2是氢; OR R1或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和X 3和X 4相同或不同，各自为氢或卤素，由A制备。反应本发明的二氢苯甲酸酰胺：其中R1，R2，X1，X2，X3和X4 如上所定义，Hal为卤素，咪唑; 或B.反应式中的二卤代苯甲酸：其中X 1，X 2，X 3和X 4如上所定义，Hal是卤素与咪唑，以产生下式的咪唑：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：

    Imidazolylacetic acid amides
    26.
    发明授权
    Imidazolylacetic acid amides 失效
    咪唑乙酸酰胺

    公开(公告)号：US3993647A

    公开(公告)日：1976-11-23

    申请号：US594544

    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 ,  C07D521/00 ,  C07D279/12

    CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D233/56 ,  C07D249/08 ,  C07D417/06

    摘要： Imidazolylacetic acid amides of the formula: ##SPC1##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 antimycotic agents.

    摘要翻译： 咪唑基乙酸酰胺的下式：

    Phenyl-imidazolyl-fatty acid derivatives
    28.
    发明授权
    Phenyl-imidazolyl-fatty acid derivatives 失效
    苯基 - 咪唑基 - 脂肪酸衍生物

    公开(公告)号：US3978069A

    公开(公告)日：1976-08-31

    申请号：US283327

    申请日：1972-08-24

    申请人： Karl Heinz Buchel ,  Werner Meiser ,  Manfred Plempel ,  Carl Metzger

    发明人： Karl Heinz Buchel ,  Werner Meiser ,  Manfred Plempel ,  Carl Metzger

    IPC分类号： C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D401/02

    CPC分类号： C07D401/06 ,  C07D403/06 ,  C07D413/06

    摘要： Phenyl-imidazolyl-fatty acid derivatives of the formula ##EQU1## wherein R.sup.1, R.sup.2, and R.sup.3 are the same or different, and are hydrogen or lower alkyl;R.sup.4 is hydrogen, alkyl, lower alkoxy, alkylmercapto, or an electro negative moiety;R.sup.5 is benzene, benzene substituted by alkyl, lower alkoxy, alkylmercapto or an electro negative moiety, or R.sup.5 is an aliphatic moiety;X is a carboxyl moiety or a grouping of a functional carboxylic acid derivative;m is 0, 1, 2, 3, 4, 5 or 6; andn is 0, 1 or 2,And pharmaceutically acceptable non-toxic salts thereof.These phenyl-imidazolyl-fatty acid derivatives exhibit antimycotic activity.

    摘要翻译： 式R 3 -C C的苯基 - 咪唑基 - 脂肪酸衍生物 - N并行对映R1-CC-R2 ANGLE N | -C-（CH2）mX | R5其中R1，R2和R3相同或不同，以及 是氢或低级烷基; R4是氢，烷基，低级烷氧基，烷基巯基或电负性部分; R5是苯，被烷基，低级烷氧基，烷基巯基或电负性部分取代的苯，或R5是脂族部分; X是羧基部分或官能羧酸衍生物的一组; M IS 0,1,2,3,4,5 OR 6; 和N是0，1或2，以及药物可接受的非毒性销售。

    Diaryl-pyridyl-imidazole methanes for treating mycotic infections
    29.
    发明授权
    Diaryl-pyridyl-imidazole methanes for treating mycotic infections 失效
    用于治疗真菌感染的二芳基 - 吡啶基 - 咪唑甲烷

    公开(公告)号：US3969522A

    公开(公告)日：1976-07-13

    申请号：US557354

    申请日：1975-03-11

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

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

    IPC分类号： A61K31/44

    CPC分类号： A61K31/44

    摘要： Diaryl-pyridyl-imidazolyl methanes of the formula ##SPC1##And pharmaceutically acceptable non-toxic salts thereof, wherein R.sup.1 and R.sup.2 are the same or different alkyl of 1 to 4 carbon atoms, are produced either byA. reacting a (dialkylphenyl-phenyl-pyridyl)-methanol of the formula ##SPC2##Wherein R.sup.1 and R.sup.2 are as above defined, with thionyl-bis-imidazole in the presence of an inert organic diluent at a temperature of from -20.degree. C to about 150.degree. C; orB. reacting a (dialkylphenyl-phenyl-pyridyl)-methyl halide of the formula ##SPC3##Wherein R.sup.1 and R.sup.2 are as above defined and Hal is chlorine or bromine, with imidazole in the presence of an acid binding agent at a temperature of from 20.degree. C to about 180.degree.C. The diaryl-pyridyl-imidazole methanes of the present invention are useful for their antimycotic activity.

    摘要翻译： 式II的二芳基 - 吡啶基 - 咪唑基甲烷及其药学上可接受的非毒性盐，其中R 1和R 2是相同或不同的1至4个碳原子的烷基，由A.产生A（对二苯基苯基 - 吡啶基） 在惰性有机稀释剂存在下，在-20℃至约150℃的温度下，在亚甲基 - 双 - 咪唑存在的情况下，R1和R2如上所定义。 或B.反应式（R 1和R 2如上所定义），并且Hal是氯或溴，在酸性粘合剂存在下，在20℃的温度下，将式（1）中的（对二苯基苯基） - 吡啶基 - 本发明的二芳基 - 吡啶基 - 咪唑甲烷可用于其抗真菌活性。

    Imidazolylacetic acid amides
    30.
    发明授权
    Imidazolylacetic acid amides 失效
    咪唑啉酸

    公开(公告)号：US3950354A

    公开(公告)日：1976-04-13

    申请号：US400263

    申请日：1973-09-24

    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： C07D233/61 ,  A61K31/415 ,  A61K31/495 ,  A61K31/54 ,  A61P31/04 ,  C07D233/56 ,  C07D233/60 ,  C07D417/06 ,  C07D521/00

    CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D233/56 ,  C07D249/08 ,  C07D417/06

    摘要： Imidazolylacetic acid amides of the formula: ##SPC1##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: ##SPC2##WhereinR.sup.1, r.sup.2, x.sup.1, x.sup.2, x.sup.3 and X.sup.4 are as above defined, andHal is halogen,With imidazole; orB. reacting a halodiphenylacetic acid halide of the formula: ##SPC3##WhereinX.sup.1, x.sup.2, x.sup.3 and X.sup.4 are as above defined andHal is halogenWith imidazole to produce an imidazolide of the formula: ##SPC4##WhereinX.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.2wherein R.sup.1 and R.sup.2 are as above defined.