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公开(公告)号：US3978069A
公开(公告)日：1976-08-31
申请号：US283327
申请日：1972-08-24
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。
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92.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：US3950354A
公开(公告)日：1976-04-13
申请号：US400263
申请日：1973-09-24
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.
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