摘要:
Compounds of formula ##STR1## (the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are explained in the specification) may be prepared by conventional methods.Owing to their favorable activity profile the compounds may advantageously be used to treat certain heart and circulatory disorders.
摘要:
The invention relates to a compound of the formula ##STR1## wherein R.sub.1 is a linear or branched alkyl of 4 to 20 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or a bivalent radical --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5, inclusive, and the free bonds of said bivalent radical are attached to adjacent carbon atoms of the phenyl ring; andR.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is alkyl of 1 to 3 carbon atoms; orR.sub.3 and R.sub.4, together with each other, are --(CH.sub.2).sub.p --, where p is an integer from 4 to 6, inclusive,or a non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds of formula I are useful for treatment and prophylaxis of diseases of the coronaries, for the treatment of hypertension, and for treatment of cardiac arrhythmia, particularly tachycardia.
摘要:
Compounds of the formula ##STR1## wherein X, Y and Z are each independently hydrogen, halogen, lower alkyl, halo(lower alkyl), lower alkoxy, halo(lower alkoxy), (lower alkyl)thio or halo(lower alkyl)thio, orY and Z, together with each other, are lower alkylenedioxy;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as analgesics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen; alkyl of 1 to 5 carbon atoms; or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
摘要:
Pharmaceutical compositions containing as an active ingredient a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, hydroxy-lower alkyl, chloro-hydroxy-propyl, 2,3-epoxy-propyl, alkoxyalkyl, aminoalkyl, N-substituted aminoalkyl, benzyl or phenethyl,R.sub.3 is hydrogen or halogen, andR.sub.4 is halogen or methyl, or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as bradycardiacs.
摘要:
Compounds of the formula ##STR1## wherein R is 2-bromo-4,5-dihydroxy-phenyl; 3-chloro-4-hydroxy-phenyl; 4-bromo-2,5-dihydroxy-phenyl; 3,5-dihydroxy-phenyl; 5-chloro-2,4-dihydroxy-phenyl; 3-hydroxy-4-methyl-phenyl; 2,6-dibromo-4-hydroxymethyl-phenyl; 3,5-dibromo-4-amino-phenyl; 3-methylmercapto-phenyl; 3,4,5-trihydroxy-phenyl; or 3-bromo-4-fluoro-phenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen, alkyl of 1 to 5 carbon atoms, or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
摘要:
Pharmaceutical dosage unit compositions containing as an active ingredient a 1-aryloxy-2-hydroxy-3-alkynylamino-propane selected from the group consisting of racemic or optically active compounds of the formula ##STR1## wherein R.sub.1 is a member selected from the group consisting of hydrogen; halogen; nitro; alkyl having from 1 to 5 carbon atoms; alkoxy having from 1 to 4 carbon atoms; alkenyl having from 2 to 5 carbon atoms; alkynyl having from 2 to 5 carbon atoms; alkylamino having from 1 to 5 carbon atoms; dialkylamino having from 1 to 5 carbon atoms in each alkyl; alkoxyalkyl having from 2 to 6 carbon atoms; alkylaminoalkyl having from 2 to 6 carbon atoms; dialkylaminoalkyl having from 3 to 12 carbon atoms; --(CH.sub.2).sub.x -NH.sub.2 or --(CH.sub.2).sub.x -OH, where x is an integer from 0 to 3; alkynyloxy having from 3 to 6 carbon atoms; alkenyloxy having from 3 to 6 carbon atoms; --CO-R.sub.9, where R.sub.9 is a member selected from the group consisting of alkyl having 1 to 6 carbon atoms, phenylalkyl having 7 to 10 carbon atoms and phenyl; cycloalkyl having from 3 to 7 carbon atoms; phenyl; phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro; phenoxy; and phenoxy substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro;R.sub.2 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms, alkanoyl having from 2 to 4 carbon atoms, alkenyl having from 2 to 4 carbon atoms, amino and nitro;R.sub.3 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms and, together with R.sub.2 in the ortho-position, --CH.dbd.CH-CH.dbd.CH- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5;R.sub.4 is a member selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms; andR.sub.5 is a member selected from the group consisting of alkyl having from 1 to 3 carbon atoms, and, together with R.sub.4, --(CH.sub.2).sub.p --, where p is an integer from 4 to 6;And physiologically compatible acid addition salts thereof; and a method of using the same as adrenolytics and hypotensives.
摘要:
Pharmaceutical compositions containing as an active ingredient a racemic or optically active compound of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms, andR.sub.2 is straight or branched hydroxyalkyl of 3 to 6 carbon atoms,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as .beta.-adrenergic receptor blocking agents and hypotensives.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, methyl, ethyl, methoxy or trifluoromethyl, andR.sub.4 and R.sub.5 are each hydrogen or propargyl, but other than both hydrogen or both propargyl at the same time,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as analgesics and hypotensives.