Ciba-geigy Corporation

Ciba-geigy Ag

Markus Zimmermann

Franz Ostermayer

Walter Fuhrer

Hans Kuhnis

Compounds of the formula ##STR1## in which R represents a carbocyclic or heterocyclic aryl radical,

3,5-Diacyl-4-aryl-1,4 dihydropyridine derivatives, their uses and

The invention relates to novel 1,4-dihydropyridine-3-carboxylic acid phenoxyaliphatylphenyleneoxyalkyl esters of the formula ##STR1## in which Ac represents an acyl group, X represents oxy or optionally substituted imino, A represents a divalent aliphatic hydrocarbon radical interrupted by a group --X.sub.1 --Ph--X.sub.2 -- in which at least one of the radicals X.sub.1 and X.sub.2 represents oxy and a radical X.sub.1 or X.sub.2 that is other than oxy represents a direct bond, and Ph represents an optionally substituted phenylene radical, and R represents an optionally substituted phenyl, pyridyl or 1-oxidopyridyl, (1,3-dioxa)indanyl or benzofurazanyl radical, R.sub.1 represents an optionally substituted phenyl or indolyl radical, R.sub.2 represents an aliphatic hydrocarbon radical and R.sub.3 represents an aliphatic radical, cyano or amino, and acid addition salts thereof.

Novel phenoxyaliphatylphenyleneoxyalkyl esters and amides

Derivatives of 3-aminopropane-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,

Derivatives of 3-aminopropane-1,2-diol

Derivatives of 3-aminopropan-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,

The invention relates to novel substituted phenyl ethers of the formula ##STR1## in which Ar represents a mono- or bi-cyclic carbocyclic aryl radical, or a mono- or bi-cyclic heterocyclic aryl radical bonded to a phenylene radical by way of a ring carbon atom,

Certain antihypertensive 1-[2-[3-carbamoyl-4-hydroxy phenoxy]alkylene

The present invention relates to novel N-oxide compounds that have cardiovascular properties, especially antihypertensive activity, and that correspond to the formula ##STR1## in which Py represents an unsubstituted or substituted N-oxidopyridyl radical, R.sub.1 represents hydrogen or unsubstituted or substituted lower alkyl, one of the radicals R.sub.2 and R.sub.3 represents lower alkyl and the other represents hydrogen; lower alkyl; lower alkyl containing free, etherified or esterified hydroxy, oxo, functionally modified carboxy or free or substituted amino or imino; functionally modified carboxy; or free or substituted amino, it being possible for an amino group R.sub.2 or R.sub.3 to be bonded to a lower alkyl radical R.sub.1 or, if R.sub.2 or R.sub.3 represents, for example, hydroxy-lower alkyl, for this hydroxy-lower alkyl, together with the adjacent acyl radical Ac.sub.1 or Ac.sub.2, to form a 2-oxa-1-oxo-lower alkylene radical, the carbonyl group of which is bonded to the 3- or 5-ring carbon atom of the 1,4-dihydropyridine ring, and each of the groups Ac.sub.1 and Ac.sub.2 represents, independently of the other, the acyl radical of an acid, and salts of compounds of the formula I having salt-forming groups, processes for the manufacture of these compounds, the use of these compounds and their salts, and pharmaceutical preparations which contain these compounds and salts, as antihypertensive agents and coronary dilators for the treatment of cardiovascular conditions, such as hypertonia, vascular constrictions, Angina pectoris and cardiac insufficiency.

N-Oxide compounds useful in the treatment of cardiovascular ailments

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.

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Riehen, Switzerland

Markus Zimmermann