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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：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：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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5.发明授权
公开(公告)号：US3969522A
公开(公告)日：1976-07-13
申请号：US557354
申请日：1975-03-11
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。
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公开(公告)号：US4049418A
公开(公告)日：1977-09-20
申请号：US614987
申请日：1975-09-19
IPC分类号： C07D231/56 , C07D521/00 , A01N9/22
CPC分类号： C07D249/08 , C07D231/12 , C07D231/56 , C07D233/56
摘要： Plant growth is regulated, e.g., inhibited or stimulated, by application to the plants or their habitat of effective amounts of at least one 5-azolyl-[a,d]-dibenzocycloheptene compound of the formula ##STR1## WHEREIN X is a --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 -- group,R is alkyl, alkoxycarbonyl or optionally substituted aryl, andAz is an azole radical of the formula ##STR2##
摘要翻译： 通过施用到植物或其栖息地的有效量的式（I）的至少一种5-噻唑基 - [a，d] - 二苯并环庚烯化合物，可以调节植物生长，例如，抑制或刺激。 -CH = CH-或-CH 2 -CH 2 - 基，R是烷基，烷氧基羰基或任选取代的芳基，并且Az是下式的唑基：
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7.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
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.
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公开(公告)号：US4018924A
公开(公告)日：1977-04-19
申请号：US539871
申请日：1975-01-09
IPC分类号： C07D401/06 , C07D403/06 , C07D413/06 , C07D401/02
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06
摘要： Cyclic amides of .alpha.-phenyl-.alpha.-imidazolyl acetic acid which are further substituted by an alkyl group or phenyl group on the .alpha.-carbon atom are antimycotic agents. A typical embodiment is diphenyl imidazolyl acetic acid piperidide.
摘要翻译： 进一步被α-碳原子上的烷基或苯基取代的α-苯基-α-咪唑基乙酸的环酰胺是抗真菌剂。 典型的实例是二苯基咪唑基乙酸哌啶。
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9.发明授权Antimycotic compositions containing an imidazolylacetic acid amide or salt thereof as the active agent and the use thereof in the treatment of mycoses 失效含有咪唑基乙酰胺或其盐作为活性剂的抗真菌组合物及其在治疗真菌病中的应用
公开(公告)号：US4024270A
公开(公告)日：1977-05-17
申请号：US594195
申请日：1975-07-09
IPC分类号： A61K31/415 , C07D417/06
CPC分类号： C07D417/06 , A61K31/415
摘要： Pharmaceutical compositions useful for treating mycotic infections in humans and animals are produced which comprise an antimycotically effective amount of an imidazolylacetic acid amide of the formula: ##STR1## 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: ##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 hydrogen,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 hydrogenWith 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 definedwhich 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.
摘要翻译： 产生用于治疗人和动物中的真菌感染的药物组合物，其包含抗真菌有效量的下式的咪唑基乙酰胺或其药学上可接受的无毒盐，其中R1是未取代或被一个取代的苯基或环烷基 或更多取代基; R2是氢; OR R1和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，X 3和X 4相同或不同，各自为氢或卤素，由A制备。反应式为二氢苯甲酸的酰胺：其中R 1，R 2，X 1，X 2，X 3和X 4为 如上所定义，Hal是氢，具有咪唑; 或B.反应式中的卤代苯甲酸：其中X 1，X 2，X 3和X 4如上所定义，Hal是具有咪唑并氢的氢，以制备式I的咪唑烷：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：
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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
CPC分类号： C07C45/71 , C07C45/004 , C07C45/63 , C07C45/70 , C07D249/08
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。
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