摘要:
The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.
摘要:
The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.
摘要:
Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
摘要:
The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen atoms, alkyl or alkoxy groups, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, particularly a heart rate lowering activity.The new compounds may be prepared using methods known per se.
摘要:
The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##STR2## group and B represents a methylene, carbonyl or thiocarbonyl group or A represents a --CO--CO or ##STR3## group and B represents a methylene group, in which the carbon atom marked x is linked to the phenyl nucleus,E represents a straight-chained alkylene group optionally substituted by an alkyl group,G represents a straight-chained alkylene group optionally substituted by an alkyl group,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, an alkenyl group, an alkyl or phenylalkyl group, andHet represents a 5- or 6-membered heteroaromtic ring bonded via a carbon or nitrogen atom, which contains an oxygen, sulphur or nitrogen atom, two nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, and onto which additionally a phenyl ring can be condensed, in which case the bond can also be via the phenyl nucleus, or an imidazo[1,2-a]pyridyl group wherein the carbon structure of the above-mentioned groups can be substituted by a methylenedioxy or ethylenedioxy group or can be mono- or disubstituted by a halogen atom or an alkyl, hydroxy, alkoxy, phenylalkoxy, phenyl, dimethoxyphenyl, nitro, amino, acetylamino, carbamoylamino, N-alkyl-carbamoylamino, hydroxymethyl, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, alkylsulphonylamino, alkoxycarbonylmethoxy, carboxymethoxy or alkoxymethyl group, and at the same time any imino group present in the above-mentioned heteroaromatic groups can be substituted by an alkyl, phenylalkyl or phenyl group, the N-oxides and the acid addition salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly the effect of lowering heart rate and oxygen requirement of the heart. They can be used to treat sinus tachycardia or ischaemic heart disease.
摘要:
Compounds of the formula ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO--, --CH.sub.2 --CO-- or ##STR2## where R.sub.7 is alkyl of 1 to 3 carbon atoms, andB is methylene, carbonyl or thiocarbonyl, orA is --CO--CO--, --N.dbd.CH--, ##STR3## where R.sub.8 is hydrogen or alkyl of 1 to 3 carbon atoms substituted by a phenyl, methoxyphenyl or dimethoxyphenyl, andB is methylene;E is n-alkylene of 2 to 4 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;G is n-alkylene of 1 to 5 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, wherein one methylene group of an n-alkylene of 2 to 5 carbon atoms can be replaced by a carbonyl group, with the proviso that B represents a methylene or carbonyl group, or methylene-n-hydroxy-alkylene of 1 to 4 carbon atoms, where the methylene group is attached to the nitrogen atom; andR.sub.1 to R.sub.5 are simple substituents of various types;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要:
This invention relates to benzazepine derivatives of formula I ##STR1## wherein A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sub.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, acylamino, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy or, together with R.sub.1, can be C.sub.1 -C.sub.3 alkylenedioxy;R.sub.3 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkoxy;R.sub.4 is hydrogen, benzyl, C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.5 alkenyl;R.sub.5 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy or, together with R.sub.5, can be a C.sub.1 -C.sub.2 alkylenedioxy;X is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is oxygen, sulphur, sulphinyl or sulphonyl;Y is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is methylene or carbonyl;m and n are each independently 2, 3 or 4; and nontoxic, pharmaceutically acceptable addition salts thereof. These compounds have valuable pharmacological properties, particularly the effect of lowering heart rate and reducing the O.sub.2 requirement of the heart.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or phenyl,R.sub.2 is hydrogen, chlorine or methoxy,R.sub.3 is hydrogen or methoxy,R.sub.2 and R.sub.3, together with each other, are methylenedioxy or ethylenedioxy,R.sub.4 and R.sub.5 are each hydrogen or lower alkyl,R.sub.6 is hydrogen or lower alkoxy,R.sub.7 is lower alkoxy,R.sub.6 and R.sub.7, together with each other, are methylenedioxy or ethylenedioxy,X is carbonyl or sulfonyl, andn is 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful for slowing the heart rate.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or phenyl,R.sub.2 is hydrogen, chlorine or methoxy,R.sub.3 is hydrogen or methoxy,R.sub.2 and R.sub.3, together with each other, are methylenedioxy or ethylenedioxy,R.sub.4 and R.sub.5 are each hydrogen or lower alkyl,R.sub.6 is hydrogen or lower alkoxy.R.sub.7 is lower alkoxy,R.sub.6 and R.sub.7, together with each other, are methylenedioxy or ethylenedioxy, andn is 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful for slowing the heart rate.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl; phenyl-lower alkyl; cycloalkyl of 3 to 6 carbon atoms; phenyl; mono- or di-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, hydroxyl, methoxy, methylmercapto, methylsulfinyl, methylsulfonyl or benzyloxy; andA is hydrogen or ##STR2## where R.sub.2 is hydrogen or lower alkyl;R.sub.3 is lower alkyl or dimethoxyphenyl-lower alkyl; orR.sub.2 and R.sub.3, together with each other and the nitrogen atom to which they are attached, are piperidino, morpholino or N'-lower alkyl-piperazino; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives, antithrombotics and antiarrhythmics.