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nya heteroaromatiska aminderivat, year foereningar innehaollande laekemedel och foerfarande foer deras framstaellning.

机译:新的杂芳族胺衍生物,含药物的化合物及其制备方法。

摘要

Heteroaromatic amine derivatives of the formula …IMAGE… in which… n denotes the number 0 or 1,… A denotes a methylene, carbonyl or thiocarbonyl group,… B denotes a methylene, carbonyl or thiocarbonyl group, in which only one of the radicals A or B may represent a thiocarbonyl group and in this case the other of the radicals A or B must represent a methylene group,… E denotes a straight-chain alkylene group optionally substituted by an alkyl group,… G denotes a straight-chain alkylene group optionally substituted by an alkyl group,… R1 and R2, which can be identical or different, denote hydrogen atoms, alkyl or alkoxy groups or… R1 and R2 together denote an alkylenedioxy group,… R3 denotes a hydrogen atom, an alkenyl group, an alkyl or phenylalkyl group and… Het denotes a 5- or 6-membered heteroaromatic ring bonded via a carbon or nitrogen atom and which contains an oxygen, sulphur or nitrogen atom, two nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, to which a 1,3-propylene, 1,4-butylene or 1,4-buta-1,3-dienylene group can additionally be bonded via two adjacent carbon atoms, where in this case the bonding can also take place via the carbon ring, and in which the carbon structure of the abovementioned aromatic and heteroaromatic rings can be mono- or disubstituted by a halogen atom, an alkyl, hydroxyl, alkoxy, phenylalkoxy, phenyl, dimethoxyphenyl, nitro, amino, acetylamino, carbamoylamino, N-alkylcarbamoylamino, hydroxymethyl, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, alkylsulphonylamino, alkoxycarbonylmethoxy, carboxymethoxy or alkoxymethyl group or substituted by a methylenedioxy or ethylenedioxy group and at the same time an imino group which may be present in the abovementioned heteroaromatic radicals can be substituted by an alkyl, phenylalkyl or phenyl group, their N-oxides, their enantiomers, their diastereomers and their acid addition salts with inorganic or organic acids, which have useful pharmacological properties, in particular a heart rate-reducing effect and a positive inotropic effect. …??The new compounds can be prepared by processes known per se.
机译:式... ...的杂芳族胺衍生物,其中... n表示数字0或1,... A表示亚甲基,羰基或硫代羰基,... B表示亚甲基,羰基或硫代羰基,其中仅一个基团A或B可以代表硫代羰基,在这种情况下,基团A或B中的另一个必须代表亚甲基,... E表示任选被烷基取代的直链亚烷基,... G表示直链亚烷基任选地被烷基取代,…R1和R2,可以相同或不同,表示氢原子,烷基或烷氧基,或…R1和R2一起表示亚烷基二氧基,…R3表示氢原子,烯基,烷基或苯基烷基,………Het表示通过碳或氮原子键合的5或6元杂芳族环,其包含氧,硫或氮原子,两个氮原子或氮原子以及氧或硫原子,其中1,3-pr可以另外通过两个相邻的碳原子键合1,4-亚丁基,1,4-丁烯基或1,4-丁1,3-二烯基,在这种情况下,键合也可以通过碳环进行,其中碳原子上述芳族和杂芳族环的结构可以被卤素原子,烷基,羟基,烷氧基,苯基烷氧基,苯基,二甲氧基苯基,硝基,氨基,乙酰氨基,氨基甲酰基氨基,N-烷基氨基甲酰基氨基,羟甲基,巯基,烷基巯基单取代或二取代,烷基亚磺酰基,烷基磺酰基,烷基磺酰基氧基,烷基磺酰基氨基,烷氧基羰基甲氧基,羧基甲氧基或烷氧基甲基或被亚甲二氧基或亚乙二氧基取代,并且同时可以存在于上述杂芳族基团中的亚氨基被烷基,苯基烷基或苯基取代,其N-氧化物,其对映异构体,其非对映异构体及其与无机或有机酸的酸加成盐,它们具有有用的药理学意义l特性,特别是心率降低作用和正性肌力作用。 ……可以通过本身已知的方法制备新化合物。

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