摘要:
Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.
摘要:
A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.
摘要:
The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, which may be the same or different, are mono- or divalent substituents selected from hydrogen, halogen, notro, hydraxylamino, amino, lower acylamino, lower alkylamino, di-(lower alkyl)-amino, hydroxyethylamino, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acylaminomethyl, halomethyl, aminomethyl, lower acylaminomethyl, di(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acyaminomethyl, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-hydroxyethyl, phenyl lower alkyl and phenyl, the phenyl radicals being optionally substituted with 1 or 2 hydroxyl or methoxy radicals, or from oxygen or sulphur; the optically-active forms and the racemic mixtures thereof, and the pharmacologically compatible salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. These compounds are useful for the prophylaxis and combatting of cardiac and circulatory diseases.
摘要:
The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamido, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, which may be the same or different, are mono- or divalent substituents selected from hydrogen, halogen, nitro, hydroxylamino, amino, lower acylamino, lower alkylamino, di-(lower alkyl)-amino, hydroxyethylamino, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acylaminomethyl, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-(lower alkoxycarbonyl)-ethyl, 2-carboxyethyl, 2-hydroxyethyl, phenyl lower alkyl and phenyl, the phenyl radicals being optionally substituted with 1 or 2 hydroxyl or methoxy radicals, or from oxygen or sulphur; the optically-active forms and the racemic mixtures thereof, and the pharmacologically compatible salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要:
New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译:新的式(I)的氨基丙醇化合物其中R是低级烷基,环烷基或烷硫基烷基,R1是氢或低级烷基,羟烷基,新戊酰氧基烷基,烷氧基烷基,烷氧基羰基,羧基或-CONR3R4,其中R3和R4可以是 R 2为低级烷基,羟基烷基,烷氧基烷基或新戊酰氧基烷基,或当R为烷硫基烷基或R 1为新戊酰氧基烷基时,R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏和循环系统疾病方面非常有效。
摘要:
New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen andThe pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要:
New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof;Are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译:新的式(I)的氨基丙醇化合物其中R是低级烷基,环烷基或烷硫基烷基,R1是氢或低级烷基,羟烷基,新戊酰氧基烷基,烷氧基烷基,烷氧基羰基,羧基或-CONR3R4,其中R3和R4可以是 R 2为低级烷基,羟基烷基,烷氧基烷基或新戊酰氧基烷基,或当R为烷硫基烷基或R 1为新戊酰氧基烷基时,R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。
摘要:
New indazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; andR.sub.2 is straight-chain or branched lower alkyl which can be substituted by lower alkylthio;And the pharmacologically compatible salts thereof; are outstandingly effective adrenergic .beta.-receptor inhibitors and useful in the treatment or prevention of a recurrence of cardiac and circulatory diseases.
摘要:
An aminopropanol compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from hydrogen and lower alkyl; orR.sub.1 and R.sub.2 together represent an alkylene radical;R.sub.3 is hydrogen or acyl;A is one of the following structures ##STR2## wherein R.sub.4 is hydrogen or lower alkyl optionally substituted by hydroxyl halogen and lower alkylthio; andR.sub.5 and R.sub.6 are individually selected from lower alkyl;B is alkylamino which optionally carries a phenyl and a phenoxy radical optionally substituted by at at least one of halogen, hydroxyl or lower alkyl, lower acyl, lower alkylthio, acylamino, aminocarbonyl, lower alkoxy, lower alkenyloxy, phenoxy, lower alkenyl, lower alkylsulphonyl, lower alkylsulphinyl or haloalkyl; orB is an aryl- or heteroaryloxymethylpiperidine radical optionally substituted by at least one of halogen hydroxyl or lower alkyl, hydroxyl alkyl or carboxamido alkyl, or by lower alkoxy, lower acyl, amino, carboxamido, lower alkylcarbonylamido or lower alkylsulphonylamino;and the pharmacologically acceptable salts thereof, are outstandingly effective beta blockers and blood-pressure depressants.
摘要:
The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for the prophylaxis and treatment of heart and circulatory diseases.