Beiersdorf Ag

Erich Cohnen

Ben Armah

Wolfgang Stenzel

Eva Hofferber

Wolfgang Fleck

Thomas Beuttler

Petra Jacobitz

New substituted phenoxyalkanolamines and phenoxyalkanol-cycloalkylamines of the general formula I ##STR1## in which R.sup.1 and R.sup.2, which can be identical or different, denote alkyl groups with in each case 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 together denote the group --(CH.sub.2).sub.n --, wherein n is the number 4 or 5, R.sup.3 denotes hydrogen, or an alkyl group or an acyl group with in each case 1 to 6 carbon atoms, R.sub.4 denotes an alkyl group with 1 to 4 carbon atoms or the cyclopropylmethyl group and R.sup.5 denotes hydrogen halogen or alkyl, and acid addiition salts thereof, have a cardioselective .beta..sub.1 -adrenolytic and hypotensive action. They can be used as medicaments for the treatment of angina pectoris, hypertension and arrhythmias.

Substituted phenoxyalkanolamies and phenoxyalkanol-cycloalkylamines in

New substituted phenoxyalkanolamines and phenoxyalkanol-cycloalkylamines of the general formula I ##STR1## in which R.sup.1 and R.sup.2, which can be identical or different, denote alkyl groups with in each case 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 together denote the group --(CH.sub.2).sub.n --, wherein n is the number 4 or 5, R.sup.3 denotes hydrogen, or an alkyl group or an acyl group with in each case 1 to 6 carbon atoms, R.sub.4 denotes an alkyl group with 1 to 4 carbon atoms or the cyclopropylmethyl group and R.sup.5 denotes hydrogen halogen or alkyl, and acid addition salts thereof, have a cardioselective .beta..sub.1 -adrenolytic and hypotensive action. They can be used as medicaments for the treatment of angina pectoris, hypertension and arrhythmias.

Substituted phenoxyalkanolamines and phenoxyalkanol-cycloalkylamines,

Bicyclic lactams of the general formula I ##STR1## in which R.sup.1 and R.sup.2, which can be identical or different, denote a hydrogen atom or an alkyl group with 1 to 3 carbon atoms, R.sup.3 denotes an unsubstituted phenyl group or a phenyl group which is substituted by a halogen atom, one or two alkoxy groups, a methylenedioxo group or one or several hydroxyl groups, or denotes a pyridyl group, an indolyl group, a 1,2-benzisoxazolyl group which is optionally substituted by a halogen atom or the benzimidazol-2-one or 1,4-benzodioxane radical, R.sup.4 denotes a hydrogen atom or an alkyl group with 1 to 6 carbon atoms or a carbalkoxymethylen group, Z denotes a straight-chain, saturated or unsaturated alkylene group with 2 or 3 carbon atoms, which is optionally alkylated, X denotes an oxygen atom or a single bond and n denotes the number 1, 2 or 3, and their tautomeric forms and their salts and acid addition salts, block both the alpha and the beta receptors of the adrenergic system and are therefore suitable for the treatment of hypertension, circulatory disturbances, angina pectoris and coronary insufficiency.

Bicyclic lactams, processes for their use, and formulations containing

Pyrido[1,8]naphthyridinones of the general formula I ##STR1## in which R.sup.1 denotes hydrogen, a straight-chain or branched alkyl group having 1 to 6 carbon atoms, the phenyl group or a substituted phenyl group, a cycloalkyl group, a carboxyl group, an alkoxycarbonyl group, a carboxamide group or a cyano group,

Pyrido(1,8)naphthyridinones, and their use as pharmaceuticals

Substituted 4-fluoro-isoindolines of the general formula I ##STR1## in which R denotes hydrogen or an acyl group, and their tautomeric forms and their acid addition salts have an alpha.sub.2 -antagonistic action.

Alpha-2-antagonistic substituted 4-fluoro-isoindolines

Substituted 5-phenylthio-6-aminopyrimidinones of the general formula I ##STR1## in which R denotes an amino or hydroxyl group, and their tautomeric forms and acid addition salts thereof, have diuretic, saluretic and uricosuric actions. They can be used as medicaments for the treatment of hypertension, hyperuricemia and edemas.

Substituted 5-phenylthio-6-amino-pyrimidinones, a process for their

New substituted tetrahydro-1H-pyrazolo[5,1-a]isoindoles of the formula I ##STR1## in which R.sup.1 denotes a hydrogen or halogen atom or an alkoxy group having 1 to 4 carbon atoms, R.sup.2, R.sup.3 and R.sup.4, which can be identical or different, denote a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R.sup.2 and R.sup.3 together denote the ethylene group, and X denotes a nitrogen atom or a methine group, and their acid addition salts have a long-lasting hypertensive effect and can be used as anti-hypotensives.

Antihypotensive tetrahydro-1H-pyrazolo[5,1-a]isoindoles

New isoindolin-2-yl-guanidines and isoindolin-2-yl-aminoimidazolines of the general formula ##STR1## in which R.sup.1 and R.sup.2 can be identical or different and either hydrogen or a halogen, alkyl, or alkoxy, each with 1 to 4 carbon atoms,

Hypertensive isoindolin-2-yl-aminoimidazolines and

Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl, R.sup.2 is halogen or alkyl, R.sup.3 is hydrogen, acyl, or saturated or unsaturated alkyl, R.sup.4 and R.sup.5 are individually hydrogen, or alkyl, wherein all alkyl and acyl groups are branched or straight-chain and each contains 1 to 4 carbon atoms, X is oxygen, nitrogen, or sulfur, Y is oxygen or nitrogen, and --X--Y-- is --O--N--, --N--O--, or --S--N--, or salts of the above, with certain exceptions. Methods of preparation of the compounds, as well as their use as anti-hypertensives are also disclosed.

Substituted oxadiazoles and thiadiazoles, and methods of preparation and

Substituted aryloxyamino propanols and pharmaceutically acceptable acid addition salts thereof according to the following formula ##STR1## wherein X is selected from oxygen and NH, R.sup.1 is selected from hydrogen, amino and acylamino having 1 to 8 carbon atoms, R.sup.2 is selected from isopropyl, tertiarybutyl, and 2-(3,4-dimethoxyphenethyl), are disclosed which are useful as anti-hypertensive and .beta.-adrenolytic agents. Also, substituted aryl azoles selected from 3-aryl pyrazoles and 5-aryl oxazoles having the formula ##STR2## wherein X and R.sup.1 are the same, and R.sup.3 is selected from hydrogen, the radical ##STR3## are disclosed which are useful in the preparation of the substituted aryloxyamino propanols of Formula I. Compositions containing the aryloxyamino propanols, and methods of preparation are also disclosed.

Substituted aryloxyamino propanols, and process for their use

A compound of the formula ##STR1## wherein R is a straight or branched chain alkyl group having 1 to 17 carbon atoms or a cycloalkyl group having 3 to 6 carbon atoms; as well as the physiologically acceptable acid addition salts thereof. A method of production of the compounds, pharmaceutical compositions containing them, and methods of use are also disclosed. The compounds of the present invention are useful in the treatment of angina pectoris, hypertension, and certain forms of arrhythmia.

Substituted oxadiazoles, method for the production thereof, compositions

There is disclosed substituted alkenones of Formula I ##STR1## wherein R.sup.1 is alkyl or acylamino each having 1 to 4 carbon atoms, hydrogen, or halogen,

Substituted 3-aryl-2-cycloalken-1-one and method of preparation thereof

The present invention is directed to certain aminopyrimidines of the general formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are hydrogen, halogen, alkoxy, alkylthio, or alkyl having 1 to 4 carbon atoms, or cycloalkyl having 3 to 5 carbon atoms and R.sup.4 is hydrogen or an aliphatic or aromatic acyl group, as well as physiologically compatible acid addition salts thereof. Compounds of the present invention are useful as blood pressure lowering agents and in the treatment of glaucoma.

Growing community of inventors

Hamburg, Germany

Erich Cohnen