申请人:Ciba-Geigy Corporation
公开号:US04460580A1
公开(公告)日:1984-07-17
The invention relates to novel N-alkylated aminoalcohols of the formula ##STR1## in which Ar is a radical of aromatic character which is unsubstituted or substituted by hydroxyl, n has the values nought or 1 and Alk is an alkylene radical having 2 to 5 carbon atoms and the nitrogen atom and the oxygen atom or, if n is nought, the salicylamide radical are separated from one another by at least two carbon atoms in the straight-chain, and their salts. The main action of the novel compounds consists in a stimulation of cardiac .beta.-receptors; the compounds also effect a blockage of adrenergic .alpha.-receptors and a lowering in the blood pressure. They can therefore be used as .beta.-stimulators, especially as agents having a positively inotropic action for the treatment of cardiac insufficiency. Compounds of the formula I in which Ar is phenyl, unsubstituted or substituted by 1 or 2 hydroxyl groups, Alk is an alkylene radical having 2 to 4 carbon atoms, n has the value 1, and the nitrogen atom and the oxygen atom are separated from one another by at least 2 carbon atoms in the straight-chain, or salts thereof, exhibit effects on the central nervous system, which are reflected for example in the suppression of the symptoms of impaired sympathetic functions and in the suppression of lack of initiative. Such compounds of the formula I therefore can be used for the treatment of reactive or endogenic states of depression of varying degrees of severity, and also for the treatment of neurotic or other psychic disturbances involving loss of initiative and depressive disorders. Such compounds can also be used for the short-term treatment of post-partum or postoperative depression, or of depression of different origin. Such compounds of the formula I can be used on their own or in combination with other antidepressants.
本发明涉及新型N-烷基氨基醇,其化学式为##STR1##其中,Ar是具有芳香性质的基团,可以是未取代或取代的羟基;n的值为零或1;Alk是具有2至5个碳原子的烷基基团,且直链中氮原子和氧原子或者如果n为零,则水杨酰胺基团之间至少相隔两个碳原子;以及它们的盐。新型化合物的主要作用是刺激心脏β-受体;这些化合物还能够阻断肾上腺素α-受体和降低血压。因此,它们可以用作β-刺激剂,特别是具有正性肌力作用的药物,用于治疗心力衰竭。化合物I的Ar为苯基,在直链中氮原子和氧原子之间至少相隔2个碳原子,Alk为具有2至4个碳原子的烷基基团,n的值为1,或其盐,表现出对中枢神经系统的作用,例如抑制交感功能障碍的症状和抑制缺乏主动性的症状。因此,化合物I可用于治疗不同程度的反应性或内源性抑郁状态,以及神经症或其他精神障碍,包括缺乏主动性和抑郁症。这些化合物还可用于短期治疗产后或手术后抑郁症,或不同起源的抑郁症。这些化合物可以单独使用或与其他抗抑郁药物联合使用。