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Imidazolylmethyl substituted phenylacetic-acid amides, process for their preparation and their pharmaceutical application

机译:咪唑基甲基取代的苯基乙酸酰胺,其制备方法及其药物应用

摘要

Substituted phenylacetic acid derivatives of the general formula IMAGE in which A represents straight-chain or branched alkyl or alkenyl, each of which has up to 8 carbon atoms, or represents cycloalkyl having 3 to 8 carbon atoms, B represents hydrogen, halogen or perfluoroalkyl having up to 5 carbon atoms, C represents a group of the formula -CH2OR3, -CO-R4, -CO-NR5R6, IMAGE or IMAGE, E represents hydrogen, halogen, nitro, hydroxyl, trifluoromethyl, trifluoromethoxy, straight-chain or branched alkyl, alkoxy or alkoxycarbonyl, each of which has up to 6 carbon atoms, cyano or carboxyl, L represents straight-chain or branched alkyl having up to 8 carbon atoms which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or phenyl, or represents cycloalkyl having 3 to 12 carbon atoms which is optionally substituted by straight-chain or branched alkyl having up to 6 carbon atoms, R1 represents hydrogen or straight-chain or branched alkyl having up to 8 carbon atoms, R2 represents, with the exception of tetrazolyl, a 5- to 7-membered saturated or unsaturated heterocycle or a benzo-fused heterocycle which is bonded via phenyl and has up to 3 hetero atoms from the series comprising S, N or O, optionally up to trisubstituted identical or different substituents from the series comprising nitro, cyano, halogen, hydroxyl, trifluoromethyl, carboxyl, straight-chain or branched alkoxy or alkoxycarbonyl, each of which has up to 6 carbon atoms, phenoxy, benzyloxy, phenoxycarbonyl or benzyloxycarbonyl, or represents a radical of the formula IMAGE R1 and R2 together with the nitrogen atom form a 5- to 7-membered saturated or unsaturated heterocycle having up to two further hetero atoms from the series comprising S, N or O, and salts thereof. The compounds are angiotensin-II antagonists and can be used in pharmaceuticals for the treatment of hypertension and atherosclerosis.
机译:通式的取代的苯乙酸衍生物,其中A代表直链或支链烷基或烯基,每个碳原子数至多为8,或代表具有3至8个碳原子的环烷基,B表示氢,卤素或具有至多5个碳原子的全氟烷基,C代表下式的基团-CH2OR 3,-CO-R 4,-CO-NR 5 R 6,,E代表氢,卤素,硝基,羟基,三氟甲基,三氟甲氧基,直链或支链烷基,烷氧基或烷氧羰基,每个碳原子数最多为6个,氰基或羧基,L表示具有最多8个碳原子的直链或支链烷基任选被具有3至8个碳原子的环烷基或苯基取代的碳原子,或代表具有3至12个碳原子的环烷基,其任选被具有至多6个碳原子的直链或支链烷基取代,R 1代表氢或碳数不超过8的直链或支链烷基除了四唑基以外,R 2代表5至7元的饱和或不饱和杂环或苯并稠合的杂环,其通过苯基键合并具有多达3个包含S,N的杂原子或O,选自由硝基,氰基,卤素,羟基,三氟甲基,羧基,直链或支链烷氧基或烷氧基羰基组成的系列中的至多三取代的相同或不同取代基,每个取代基具有至多6个碳原子,苯氧基,苄氧基,苯氧基羰基或苄氧基羰基,或代表式的基团R 1和R 2与氮原子一起形成5至7元饱和或不饱和杂环,该杂环还具有最多两个该系列的杂原子包含S,N或O及其盐。该化合物是血管紧张素II拮抗剂,可用于治疗高血压和动脉粥样硬化的药物。

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