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公开(公告)号：US4062959A
公开(公告)日：1977-12-13
申请号：US554009
申请日：1975-02-28
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。
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公开(公告)号：US4118487A
公开(公告)日：1978-10-03
申请号：US638274
申请日：1975-12-05
IPC分类号： C07D233/54 , A61K31/41 , A61P31/04 , A61P31/10 , C07C29/143 , C07D231/10 , C07D231/12 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/64 , C07D249/08 , C07D521/00 , C08K5/3445 , C08K5/3472
CPC分类号： C07D231/12 , C07C29/143 , C07D233/56 , C07D249/08
摘要： Azol-1-ylmethanes substituted on the methane carbon atom by (a) phenyl or lower alkyl and (b) by a biphenyl-4-yl, 4-phenoxyphenyl, 4-phenylthiophenyl, 4-phenylsulfinylphenyl or 4-phenylsulfonylphenyl group are antimycotic and antibacterial agents. The compounds, of which (biphenyl-4-yl)phenyl-imidazol-1-ylmethane is a typical example, are prepared from the correspondingly substituted carbinol through treatment with thionyl-bis-azole or from the correspondingly substituted methyl halide with the azole or a derivative thereof.
摘要翻译： （a）苯基或低级烷基和（b）联苯-4-基，4-苯氧基苯基，4-苯硫基苯基，4-苯基亚磺酰基苯基或4-苯基磺酰基苯基在甲烷碳原子上取代的偶氮-1-基甲烷是防霉的， 抗菌剂。 其中（联苯-4-基）苯基 - 咪唑-1-基甲烷是典型的实例，其化合物是由相应取代的甲醇通过用亚硫酰基 - 双 - 唑或相应地取代的甲基卤与唑或 其衍生物。
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公开(公告)号：US3934014A
公开(公告)日：1976-01-20
申请号：US474873
申请日：1974-05-31
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。
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公开(公告)号：US3980780A
公开(公告)日：1976-09-14
申请号：US554203
申请日：1975-02-28
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。
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公开(公告)号：US3941800A
公开(公告)日：1976-03-02
申请号：US405969
申请日：1973-10-12
IPC分类号： C07D249/08 , C07D261/08 , C07D521/00
CPC分类号： C07D233/56 , C07D231/12 , C07D249/08 , C07D261/08
摘要： Novel N-benzyltriazoles of the formula ##SPC1##In whichTriazolyl is 1,2,4 or 1,2,3 triazolyl which may be substituted;X is halogen, trifluoromethyl, lower alkyl, lower alkoxy, lower alkylthio, aryl, nitro, cyano or (alkylated) amino;m is 0, 1 or 2;A is optionally substituted phenyl, pyridyl, alkyl or cycloalkyl; andB is a 5-membered heterocyclic ring, e.g., N-heterocycle;And their salts are outstandingly effective in regulating plant growth, e.g., inhibiting, stimulating or altering plant growth.
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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.
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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.
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公开(公告)号：US3985766A
公开(公告)日：1976-10-12
申请号：US873098
申请日：1969-10-31
申请人： Erik Regel , Karl Heinz Buchel , Manfred Plempel
发明人： Erik Regel , Karl Heinz Buchel , Manfred Plempel
IPC分类号： C07D233/54 , C07D233/62 , C07D235/06 , C07D235/18 , C07D521/00 , C07D233/56
CPC分类号： C07D231/12 , C07D233/56 , C07D235/06 , C07D235/18 , C07D249/08
摘要： Bis-imidazolyl-bisphenylmethane derivatives and pharmaceutically acceptable non-toxic salts thereof are useful as antimycotics especially against dermatomycosis caused by Trichophyton and Microsporium species and also against yeast infections of the skin and internal organs.
摘要翻译： 双咪唑基 - 双苯基甲烷衍生物及其药学上可接受的无毒盐可用作抗霉菌剂，特别是针对由毛癣菌和微孢子菌引起的皮肤真菌病，并且还可用于皮肤和内脏器官的酵母菌感染。
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公开(公告)号：US4141981A
公开(公告)日：1979-02-27
申请号：US813055
申请日：1977-07-05
申请人： Wilfried Draber , Manfred Plempel , Karl H. Buchel , Erik Regel
发明人： Wilfried Draber , Manfred Plempel , Karl H. Buchel , Erik Regel
IPC分类号： C07D401/06 , A61K31/44 , A61K31/4427 , A61P17/00 , A61P31/04 , C07D213/30 , C07D521/00
CPC分类号： C07D213/30 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Antimycotic compositions in topical or vaginal administration form are prepared wherein the active agent is imidazol-1-yl-(4-phenoxyphenyl)-(pyridin-2-yl)phenylmethane in combination with a pharmaceutically acceptable carrier suitable for topical application to the skin of a human or suitable for vaginal administration to humans. Such compositions are useful for treating mycoses in humans.
摘要翻译： 制备局部或阴道给药形式的抗真菌组合物，其中活性剂是咪唑-1-基 - （4-苯氧基苯基） - （吡啶-2-基）苯基甲烷与适用于局部施用于皮肤的药学上可接受的载体的组合 人类或适合于对人类进行阴道给药。 这样的组合物可用于治疗人类的真菌病。
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10.发明授权.alpha.-(4-Biphenylyl)-benzyl-azolium salts and their use for combating micro-organisms 失效α-（4-联苯基） - 苄基 - 唑烷鎓盐及其用于抗微生物的用途
公开(公告)号：US4243670A
公开(公告)日：1981-01-06
申请号：US14783
申请日：1979-02-23
申请人： Erik Regel , Wilfried Draber , Karl H. Buchel , Manfred Plempel
发明人： Erik Regel , Wilfried Draber , Karl H. Buchel , Manfred Plempel
IPC分类号： C08G69/48 , A61K31/41 , A61K31/415 , A61P31/04 , A61P31/10 , C07D233/56 , C07D233/58 , C07D233/60 , C07D249/08 , C07D521/00 , C08G69/00 , A01N43/26 , A01N43/28
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention relates to novel .alpha.-(4-biphenylyl)-benzyl-azolium salts of the general formula ##STR1## in which A represents the CH group or a N atomR.sup.1 and R.sup.2 are identical or different and each represents hydrogen, alkyl or optionally substituted phenyl,R.sup.3 represents hydrogen, alkyl, or an optionally substituted phenyl, phenylalkyl, phenylcarbonyl or phenylcarbonylalkyl group,X represents halogen, alkyl, halogenoalkyl, alkoxy, alkylthio, nitro or cyano,Y represents X or optionally substituted phenyl,m and n each represents 0 or an integer from1 to 5 andZ represents the anion of an inorganic or organic acid.The invention also includes processes for the preparation of the compounds and, in addition includes compositions containing the compounds and methods for their use. The compounds of the invention exhibit antimicrobial activity and sporicidal activity.
摘要翻译： 本发明涉及其中A表示CH基团或N原子R1和R2相同或不同并且各自表示氢的通式为“IMA”（I）的新型α-（4-联苯基） - 苄基 - ，烷基或任选取代的苯基，R 3表示氢，烷基或任选取代的苯基，苯基烷基，苯基羰基或苯基羰基烷基，X表示卤素，烷基，卤代烷基，烷氧基，烷硫基，硝基或氰基，Y表示X或任选取代的苯基， m和n各自表示0或1至5的整数，Z表示无机或有机酸的阴离子。 本发明还包括制备化合物的方法，并且还包括含有这些化合物的组合物及其使用方法。 本发明的化合物显示出抗微生物活性和杀孢子活性。
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