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3,3,5-trimethylcyclohexylamine derivs - with hypertensive/hypotensive

机译:3,3,5-三甲基环己胺衍生物-具有高血压/降压药

摘要

Title derivs. of formula (I): (where R1 is H or 1-4C opt. satd. alkyl; and R2 is 1-6C opt. satd. alkyl, cycloalkyl with 5-7 ring C-atoms and opt. substd. by methyl gps., or phenylalkyl in which the alkyl has 1-3 chain atoms and is opt. substd. by 1-3 1-4C atoms and the phenyl is opt. substd. by 1-3 1-4C alkyl or alkoxy gps. or Cl atoms; or NR1R2 is satd. heterocyclyl with 5-7 ring members of which one can be an O- or substd. N-atom) adn their salts with acids have hypertensive activity (at low dosage, duration 10-30 mins.) and hypotensive activity (at high dosage, duration 1-3 mins.). Corresponding quaternary cpds. of formula (II): (where R3 is 1-4C alkyl and Anion is the residue of an inorganic acid) have only hypotensive activity (which activity is not attributable to ganglionic blockade). Processes for preparing (I) and (II) are described and claimed in the specification.
机译:头衔衍生。式(I)的式(I):(其中R 1是H或1-4C,优选饱和的烷基; R 2是1-6C,优选饱和的烷基,具有5-7个环C-原子的环烷基,并且优选被甲基gps取代或苯基烷基,其中烷基具有1-3个链原子且优选被1-3 1-4C原子取代,而苯基优选被1-3 1-4C烷基或烷氧基gps取代原子;或NR1R2是具有5-7个环成员的饱和杂环基,其中一个可以是O原子或N原子;其与酸的盐具有高血压活性(低剂量,持续10-30分钟),并且降压活动(高剂量,持续1-3分钟)。对应的四元cpds。式(II)的通式(II):(其中R 3是1-4C烷基,并且阴离子是无机酸的残基)仅具有降血压活性(该活性不归因于神经节阻滞)。说明书中描述并要求保护制备(I)和(II)的方法。

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