摘要:
The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is alkoxy of 1 to 3 carbon atoms; andR.sub.2 is (aralkylsulfinyl of 7 to 9 carbon atoms)-(alkoxy of 2 to 3 carbon atoms); or (unsubstituted, mono-, di- or trisubstituted phenyl-sulfinyl)-(alkoxy of 2 to 3 carbon atoms), where the substituents are attached to the phenyl moiety and are nitro, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen;their 3H-tautomers; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as hypertensives and cardiotonics.
摘要:
This invention relates to novel indole derivatives of the formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##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, E represents an alkylene group or a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene, or 3-hydroxy-n-butylene group,G represents an alkylene group,R.sub.1 represents a hydrogen, chlorine, or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine, or bromine atom or a hydroxyl, alkoxy, phenylalkoxy, or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen, chlorine, or bromine atom or an alkyl group,R.sub.4 represents a hydrogen atom or an alkyl or phenylalkyl group,R.sub.5 represents a hydrogen, fluorine, chlorine, or bromine atom or an alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.6 represents a hydrogen atom or an alkoxy group, andR.sub.7 represents a hydrogen atom or an alkenyl, alkyl or phenylalkyl group,and the acid additional salts thereof. These compounds, which may be obtained by use of known methods, have valuable pharmacological properties, particularly a heart rate-lowering activity.
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:
This invention related to new aminotetralin derivatives of formula I ##STR1## wherein ##STR2## B is methylene or, when A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO-- or --CH.sub.2 --CO--, B can also be carbonyl or thiocarbonyl;E is a C.sub.2 -C.sub.4 straight-chain alkylene, optionally substituted by a C.sub.1 -C.sub.3 alkyl, or is 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;R.sub.1 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, nitro, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylthio, 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 alkoxy phenyl C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkyl or, together with R.sub.1, can be a C.sub.1 -C.sub.2 alkylenedioxy;R.sub.3 and R.sub.4 are each independently selected from hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, nitro, amino, C.sub.1 -C.sub.3 alkylamino, or C.sub.1 -C.sub.3 dialkylamino, or together can be methylenedioxy; andR.sub.5 is hydrogen, C.sub.3 -C.sub.5 alkenyl, C.sub.1 -C.sub.3 alkyl, or phenyl C.sub.1 -C.sub.3 alkyl, and nontoxic, pharmaceutically acceptable addition salts thereof which have valuable pharmacological properties, particularly a long-lasting heart rate lowering effect and the effect of reducing the O.sub.2 requirement of the heart.
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:
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; trifluoromethyl; alkyl of 1 to 11 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; hydroxyl; alkoxy of 1 to 6 carbon atoms; mercapto; (alkyl of 1 to 6 carbon atoms)-mercapto; phenyl-(alkyl of 1 to 3 carbon atoms); phenyl; or mono-, di- or tri-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, alkyl of 1 to 4 carbon atoms, (alkyl of 1 to 6 carbon atoms)-sulfinyl, hydroxyl, alkoxy of 1 to 6 carbon atoms, mercapto or (alkyl of 1 to 6 carbon atoms)-mercapto;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or phenyl-(alkyl of 1 to 3 carbon atoms); andR.sub.3 is alkyl of 1 to 6 carbon atoms; optically active antipodes thereof; and non-toxic, pharmaceutically acceptable acid addition salts of said compounds or of said optically active antiposed. The compounds are useful as cardiotonics and antithrombotics.
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.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, trifluoromethyl, alkyl of 1 to 5 carbon atoms, mercapto, lower alkyl-mercapto, phenyl, fluoro-phenyl, tolyl, hydroxy-phenyl, methylmercapto-phenyl, methylsulfinyl-phenyl, methylsulfonyl-phenyl, dimethylamino-phenyl, or mono-, di- or tri-methoxy-substituted phenyl;A is hydrogen or, together with B, a double bond,B is hydrogen, alkyl of 1 to 3 carbon atoms or, together with A, a double bond;C is, together with R.sub.2, a double bond, or, together with R.sub.3, oxygen;R.sub.2 is hydrogen, alkyl of 1 to 3 carbon atoms or, together with C, a double bond; andR.sub.3 is chlorine, methylamino, morpholino, 4-methylpiperazino or, when R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, together with C, oxygen;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as hypotensives, antithrombotics and cardiotonics.