发明名称 N-Alkylated aminoalcohols and their pharmaceutical compositions useful for the treatment of cardiac insufficiency
摘要 The invention relates to novel N-alkylated aminoalcohols of the formula <IMAGE> (I) 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.
申请公布号 US4460580(A) 申请公布日期 1984.07.17
申请号 US19820391814 申请日期 1982.06.24
申请人 CIBA-GEIGY CORPORATION 发明人 OSTERMAYER, FRANZ;ZIMMERMANN, MARKUS
分类号 A61K31/165;A61P9/04;A61P25/02;C07C67/00;C07C229/38;C07C231/00;C07C231/12;C07C231/14;C07C235/46;C07C237/30;C07D213/38;C07D265/22;C07D307/52;C07D333/20;(IPC1-7):C07D213/56;A61K31/44 主分类号 A61K31/165
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