摘要:
Novel tricyclic aminoalkyl derivatives are disclosed which are characterized by valuable pharmacological activities and namely by cardiac and circulatory activities. The tricyclic aminoalkyl derivatives are compounds of the formula: ##STR1## wherein X is an oxygen or a sulfur atom, a saturated or unsaturated, straight chain or branched alkylene group containing up to 3 carbon atoms, an oxymethylene, thiamethylene or thiaethylene group or a valency bond, R.sub.1 is hydrogen, halogen, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen or hydroxyl, R.sub.3 is hydrogen or together with R.sub.2 represents a further valency bond, R.sub.4 and R.sub.5 which may be the same or different are each hydrogen or lower alkyl, A is alkylene which is substituted by an optionally acylated hydroxyl group, Y is an oxygen or sulfur atom or an optionally alkylated imino group and Z is aryl, aralkyl, cycloalkyl or cycloalkyl-alkyl which may be substituted by halogen, hydroxyl, nitro, amino, alkoxy, aralkoxy, alkyl, trifluoromethyl, alkylamino or alkylsulfonyl group, and the acid addition salts thereof with pharmacologically acceptable acids.
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:
Benzopyrones of the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or a hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl radical,R.sub.2, r.sub.3, r.sub.4 and R.sub.5 each independently is hydrogen, a halogen atom, a hydroxyl radical, a lower alkyl or lower alkoxy radical, or a lower alkyl or lower alkoxy radical substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring,A is a lower alkylene radical, andn is 0, 1 or 2,And salts thereof exhibit anti-allergic activity.
摘要:
4-Phenoxymethyl-piperidines of the formula ##STR1## wherein R is hydrogen, halogen, nitro, lower alkyl or lower alkoxy, in the form of the free base or an acid addition salt, are provided and they are useful as intermediates in the production of anti-hypertensive agents through condensation with (a) propyl chloride and then with an adenine, or (b) a propyl indole.
摘要:
9-[3-(4-Phenoxymethylpiperidino)-propyl]-adenines of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom, a ower alkyl radical optionally substituted by hydroxyl, or a cycloalkyl radical, orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a heterocyclic ring, andR.sub.3 is a hydrogen atom, a halogen atom, a lower alkyl radical or a lower alkoxy radical,In the form of the free base or a salt thereof, exhibit anti-allergic, anti-inflammatory, anti-oedematous and anti-hypertensive activity.
摘要:
New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO--NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof, are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.
摘要:
An L-3-(3,4-dihydroxyphenyl)-2-methyl-alanine peptide of the formula ##STR1## wherein A is an alkylene radical which can be substituted by a hydroxyl group or by a phenyl radical which optionally carries at least one hydroxyl group, andR is a hydrogen atom or a lower alkyl radical or a glycyl or alanyl radical,Or a pharmacologically compatible salt thereof. These compounds are outstanding in lowering blood pressure.
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:
A N.sup.6 -substituted-9-[3-(4-phenyl-piperazino)-propyl]-adenine of the formula ##STR1## wherein R.sub.1 is hydrogen or a lower alkyl radical, andR.sub.2 is a lower alkyl radical, a lower alkyl radical substituted by at least one of phenyl and hydroxyl, a lower alkenyl radical, a cycloalkyl radical or an aryl radical, orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a piperidine, pyrrolidine or morpholine ring, andR.sub.3 is hydrogen, halogen, a lower alkyl radical or a lower alkoxy radical,Or a salt thereof with a pharmacologically compatible acid, which compounds are characterized by marked anti-edematous activity as well as by activity in reducing capillary permeability.