摘要:
The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要:
The new pyrrolobenzimidazoles according to the present invention are compounds of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom, an alkyl or alkenyl radical or a cyano group or a carbonyl group substituted by a hydroxyl or hydrazino group or by an alkyl, alkoxy, amino, alkylamino or dialkylamino group or together with R.sub.1 represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical, X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinylene radical, T is an oxygen or sulphur atom and Py is a 2-, 3- or 4-pyridyl radical which optionally carries an oxygen atom on the ring heteroatom and/or can be substituted one or more times by alkyl, alkoxy, hydroxyl, cyano or nitro, as well as by halogen; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.
摘要:
The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 -R.sub.5, X and T are as defined in the specification. The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
摘要:
The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, each represent a hydrogen atom or an alkanesulphonyloxy, trifluoromethanesulphonyloxy, alkanesulphonylamino, trifluoromethanesulphonylamino, N-alkyl-alkanesulphonylamino, N-alkyl-trifluoromethanesulphonylamino, alkylsulphenylmethyl, alkylsulphinylmethyl or alkylsulphonylmethyl radical, a carbonyl group substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino, a sulphonyl group substituted by amino, alkylamino, dialkylamino or cyclic imino, whereby a methylene group in the 4-position can be replaced by a sulphur or oxygen atom, an alkylcarbonylamino, aminocarbonylamino or alkylaminocarbonylamino radical, an alkylthio, alkylsulphinyl or alkylsulphonyl radical, a nitro, halogen, amino, hydroxyl, alkyl, trifluoromethyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, dialkylamino, 1-imidazolyl or cyano group; X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinyl radical; and T is an oxygen or sulphur atom; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
摘要:
Pyrrolobenzimidazoles, processes for the preparation thereof and pharmaceutical compositions thereof for the treatment of coronary insufficiencies, cardiac failure, blood circulatory disturbances and occlusive diseases. The new pyrrolobenzimidazoles are of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkenyl or cycloalkyl, R.sub.2 is hydrogen, alkyl, alkenyl, cyano or a substituted carbonyl or R.sub.1 and R.sub.2 together represent cycloalkylene or form alkylidene or cycloalkylidene, X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene, T is oxygen or sulphur and Py is pyridyl or substituted pyridyl and including the tautomers thereof and the physiologically acceptable salts thereof.
摘要:
The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要:
The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.
摘要翻译:本发明涉及以下通式的化合物的用途:其中A是任选取代的苯基或杂芳族基团,R 6和R 7是氢或低级烷基,X是含有至多6个亚烷基的亚烷基链 碳原子,Y是价键或> C = O基团,B是任选取代的苯基或杂芳族基团,以及它们的药理学上可接受的盐用于治疗血流紊乱。 本发明还提供含有这些化合物的药物组合物。
摘要:
The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.
摘要翻译:本发明涉及以下通式的化合物的用途:其中A是任选取代的苯基或杂芳族基团,R 6和R 7是氢或低级烷基,X是含有至多6个亚烷基的亚烷基链 碳原子,Y是价键或> C = O基团,B是任选取代的苯基或杂芳族基团,以及它们的药理学上可接受的盐用于治疗血流紊乱。 本发明还提供含有这些化合物的药物组合物。
摘要:
The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.