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process for the production of new imidazolylaethyl - oxyalkoxy derivatives and thiometon analogue, and their pharmacologically zulaessigen saeureadditionssalze
process for the production of new imidazolylaethyl - oxyalkoxy derivatives and thiometon analogue, and their pharmacologically zulaessigen saeureadditionssalze
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机译:咪唑基甲乙氧基烷氧基衍生物和硫酮类似物的制备方法以及它们的药理学作用
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摘要
Antimycotically and antibacterially effective imidazole derivatives of the formula (1) IMAGE (1) in which R1, R2 and R3 are the same or different and are hydrogen and lower alkyl; R4 is hydrogen, lower alkyl or selected from unsubstituted or substituted cycloalkyl, benzyl and phenyl groups wherein the substituents are selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, phenyl, cyano, nitro and amino, or wherein R4 is an unsubstituted or halosubstituted pyridyl, R5 is nitro or lower alkyl in any unsubstituted position of the imidazole ring, Ar is a phenyl group optionally substituted with at least one substituent which is halogen, lower alkyl, lower alkoxy or a C4-C8 cycloalkyl, or wherein Ar is a benzyl group optionally substituted with a substituent of the type set forth for R4, X and Y are independently selected from oxygen (-O-) or sulfur (-S), n is an integer of from 1 to 5 inclusive and p is Zero or an integer of from 1 to 3 inclusive, and the addition salts of formula (1) compounds with pharmaceutically acceptable organic or inorganic acids; the formula (1) compounds and their addition salts as specified have a relatively low oral toxicity or/and an improved solubility and are suitable for use in human and veterinary medicine and for chemo-agricultural fungus control purposes. Suitable pharmaceutical compositions including the novel derivatives or/and their addition salts with acceptable acids as well as methods for producing such novel derivatives are disclosed.
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机译:式(1)(1)的抗真菌和抗菌有效的咪唑衍生物,其中R1,R2和R3相同或不同,并且为氢和低级烷基; R 4是氢,低级烷基或选自未取代或取代的环烷基,苄基和苯基,其中取代基选自卤素,低级烷基,低级烷氧基,低级烷硫基,苯基,氰基,硝基和氨基,或其中R 4是未取代的或卤代的吡啶基,R5为在咪唑环的任何未取代位置上的硝基或低级烷基,Ar为任选地被至少一个取代基取代的苯基,所述取代基为卤素,低级烷基,低级烷氧基或C4-C8环烷基,或其中Ar为任选地被R 4所示类型的取代基取代的苄基,X和Y独立地选自氧(-O-)或硫(-S),n是1至5的整数,包括5和p式(1)化合物与药学上可接受的有机或无机酸的加成盐;或1至3的整数,包括1和3。所述的式(1)化合物及其加成盐具有较低的口服毒性或/和改善的溶解度,并且适用于人和兽药以及化学农业真菌防治目的。公开了包括新衍生物或/和它们与可接受的酸的加成盐的合适的药物组合物,以及生产这种新衍生物的方法。
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