Antimycotic imidazolyl-9,10-dihydro-anthracene derivatives
    82.
    发明授权
    Antimycotic imidazolyl-9,10-dihydro-anthracene derivatives 失效
    抗真菌咪唑基-9,10-二氢 - 蒽衍生物

    公开(公告)号:US4183940A

    公开(公告)日:1980-01-15

    申请号:US840461

    申请日:1977-10-07

    摘要: The invention provides new azolyl-9,10-dihydroanthracene derivatives of the formula ##STR1## in which A represents a CH group or a nitrogen atom,B represents a CO group or a group of the formula: ##STR2## X, Y and Z are identical or different and represent halogen, alkyl, halogenoalkyl, alkoxy, or alkylthio and n represents 0 or an integer of from 1 to 4,and their salts.Also included in the invention are methods for the preparation of said compounds, compositions containing said compounds and methods for their use. The compounds of the invention have antimycotic activity.

    摘要翻译: 本发明提供了式(I)的新的唑基-9,10-二氢蒽衍生物,其中A表示CH基团或氮原子,B表示CO基团或下式的基团:X, Y和Z相同或不同,表示卤素,烷基,卤代烷基,烷氧基或烷硫基,n表示0或1-4的整数,及其盐。 本发明还包括制备所述化合物的方法,含有所述化合物的组合物及其使用方法。 本发明的化合物具有抗真菌活性。

    Disubstituted triphenylmethylimidazoles
    84.
    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

    IPC分类号: C07D233/62 C07D521/00

    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.

    Imidazolylacetic acid amides, their production, antimycotic compositions
comprising said compounds and their use as antimycotic agents
    85.
    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

    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
    87.
    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

    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:

    N-Methyl-imidazole derivatives for treating mycotic infections
    90.
    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

    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。