摘要:
The present invention relates to the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing such compounds and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
摘要:
The present invention relates to new amino alcohol derivatives, process for the production thereof and medicaments and reagents containing these compounds.
摘要:
The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要:
The present invention provides N.sup.6 -disubstituted purine derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.4 are the same or different and each represents a hydrogen or halogen atom or an --NR.sub.6 R.sub.7 group, R.sub.2 and R.sub.3 are the same or different and each represents a C.sub.1 -C.sub.6 alkyl radical, a C.sub.2 -C.sub.6 alkenyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, a phenalkyl radical containing up to 4 carbon atoms in the alkyl moiety, which can be straight-chained or branched, the phenyl moiety of which can be substituted one or more times by halogen, hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or trifluoromethyl; a furylmethyl or furylethyl radical, a thiophenemethyl or thiopheneethyl radical, a pyridylmethyl or pyridylethyl radical optionally substituted by a C.sub.1 -C.sub.4 alkyl radical, an indanyl radical or a tetrahydronaphthyl radical, R.sub.5 is a hydrogen atom, a tetrahydrofuranyl or tetrahydropyranyl radical or a C.sub.1 -C.sub.10 radical which is optionally substituted one or more times by hydroxyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 carboxyalkanoyloxy, C.sub.2 -C.sub.6 hydroxyalkoxy, C.sub.3 -c.sub.6 dihydroxyalkoxy, carboxyl, cyano or 1H-tetrazol-5-yl radical, R.sub.6 and R.sub.7 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical or together represent a C.sub.2 -C.sub.5 alkylene radical optionally interrupted by oxygen, sulphur or an NR.sub.8 group and R.sub.8 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical; as well as the pharmacologically acceptable salts thereof.
摘要:
The present invention provides aminoalcohols of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be same or different, are hydrogen atoms, hydroxyl groups, C.sub.1 -C.sub.4 -alkoxy, benzyloxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkanesulphonylamino, C.sub.1 -C.sub.4 -alkanesulphinyl or C.sub.1 -C.sub.4 -alkanesulphonyl radicals, m is 2, 3 or 4, X and Y, which can be the same or different, are hydrogen atoms or benzyl radicals and R.sub.3 is a phenyl radical substituted twice by C.sub.1 -C.sub.6 -alkyl radicals, a nitrophenyl radical, an aminophenyl radical, a 1,3,5-tri-C.sub.1 -C.sub.6 -alkyl-2,4-dioxo-1H,3H-pyrimidin-6-yl radical, an indolyl radical, an indazolyl radical, a benzimidazolyl radical, a 1,4-di-C.sub.1 -C.sub.6 -alkylpyrazol-5-yl radical or a radical of the general formula: ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different, are C.sub.1 -C.sub.4 -alkyl radicals and R.sub.6 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, phenyl or benzyl radical; and the pharmacologically acceptable salts there, as well as methods for making and using these compounds and compositions containing them. There are useful as cardiovascular medicaments.
摘要:
An aryl ether derivative of the formula ##STR1## in which A is an oxygen atom or an >N--R.sub.1 grouping,R.sub.1 is a hydrogen atom or a lower alkyl radical,B is an alkylene radical containing 2 to 4 carbon atoms,R.sub.2 and R.sub.3 each independently is a hydrogen or halogen atom, hydroxyl group or lower alkyl, lower alkoxy or lower alkanoyl radical,R.sub.4 is a hydrogen atom or an acyl radical, andn is an integer from 1 to 5,or a pharmacologically acceptable salt thereof, which possesses anti-allergic activity.
摘要:
Compounds of formula I ##STR1## in which Q denotes hydrogen, a hydroxy group or a C.sub.1 to C.sub.8 alkoxy group which can be substituted if desired, by carboxyl or C.sub.1 to C.sub.6 alkoxycarbonyl and either Y and Z together form a group ##STR2## and X represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.2 to C.sub.6 alkenyl or Y and X together form a group ##STR3## or an alkylene residue of 2-4 carbon atoms and Z represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkanoyl, where R denotes hydrogen or a C.sub.1 to C.sub.6 alkyl residue as well as physiologically tolerated salts thereof, processes for their production and pharmaceutical agents containing these compounds for the treatment of inflammatory diseases and allergic diseases.
摘要:
Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.
摘要:
The present invention provides new aminopropanol derivatives of the general formula: ##STR1## wherein A is a direct bond, a straight-chained or branched alkylene chain containing up to 3 carbon atoms or a --CO--CH.sub.2 -- group; X is a direct bond or a carbonyl group; B is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, in which one or two --CH.sub.2 -- groups can also be replaced by a saturated or unsaturated alkylene ring containing 3 to 7 carbon atoms and/or by an oxygen or sulphur atom or an --S(.dbd.O)-- or --S(.dbd.O).sub.2 -- group, n is 1, 2 or 3; R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical containing up to 6 carbon atoms or a --B--(ONO.sub.2).sub.n group, in which B and n have the same meanings as above, or when A is a --CO--CH.sub.2 -- group and X is a direct bond, R.sub.1 together with the nitrogen atom and a carbon atom of chain B can represent a heteroaliphatic ring containing 2 to 7 carbon atoms; R.sub.2 is a hydrogen or halogen atom or a cyano, hydroxyl, amino, nitro, carboxyl, carbamoyl, ureido or sulphamoyl group or an alkyl, alkoxy, alkylamino, alkylthio, hydroxyalkyl, aminoalkyl, alkoxycarbonyl, alkylcarbonyl, alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonylamino or alkylaminocarbonylamino radical; and R.sub.3 is an alkyl or nitroxyalkyl radical containing 3 to 8 carbon atoms; and the physiologically acceptable salts thereof.The present invention also provides processes for the preparation of these aminopropanol derivatives and pharmaceutical compositions containing them, as well as intermediates for the preparation of the new aminopropanol derivatives.
摘要:
The present invention provides bicyclic phenol ethers of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom or an acyl radical,X is an oxygen or sulphur atom or an --NH-- group;Y is a --CO--CHR.sub.3 -- group or a ##STR2## group; R.sub.3 is a hydrogen atom, a lower alkyl radical which can be optionally substituted by an aryl radical, or a cycloalkyl radical containing 3 to 7 carbon atoms; andR.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, lower alkyl radicals, lower alkyl radicals, alkenyl radicals containing 2 to 16 carbon atoms, which can be optionally substituted by an aryl radical, or an aryl radical; orR.sub.4 and R.sub.5, together with the carbon atom to which they are attached, form a cycloalkyl ring containing 3 to 7 carbon atoms; and thesalts thereof with pharmacologically acceptable acids.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.