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:
Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.
摘要:
New aminopropanol compounds of the formula ##STR1## wherein A is alkylene;B is sulfur or a valency bond;R is a straight-chained or branched lower alkyl; and the pharmacologically compatible salts thereof; are outstandingly effective adrenergic .beta.-receptor inhibitors and useful in the treatment or prophylaxis of circulatory diseases.
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:
New N-substituted 1-amino-3-phenoxy-propan-2-ol compounds of the formula: ##EQU1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or, taken together, represent a sulfur linkage, an ethylene radical or a valency bond;B is straight or branched chain alkylene or hydroxyalkylene of from 2 to 5 carbon atoms; andR.sub.3 is hydrogen or alkyl of up to 3 carbon atoms;And the physiologically compatible salts thereof; possess valuable cardiac and circulatory activity.
摘要:
Novel 9-[3-(4-amino-piperidino)-propyl]-adenine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R.sub.1 and the nitrogen atom to which they are attached form a heterocyclic ring, andR.sub.3 is a hydrogen atom or an acyl radical,or salts thereof with pharmacologically acceptable acids, characterized by anti-allergic, anti-inflammatory and anti-oedematous activity.
摘要:
New N-substituted 1-amino-3-phenoxy-propan-2-ol compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or, taken together, represent a sulfur linkage, an ethylene radical or a valency bond;B is straight or branched chain alkylene or hydroxyalkylene of from 2 to 5 carbon atoms; andR.sub.3 is hydrogen or alkyl of up to 3 carbon atoms;And the physiologically compatible salts thereof; possess valuable cardiac and circulatory activity.
摘要:
New amine derivatives of azidophenols having the formula: ##EQU1## wherein R is straight-chained or branched alkyl;And the pharmacologically compatible salts thereof;Inhibit adrenogenic .beta.-receptors and are suitable for the treatment and prophylaxis of cardiac and circulatory diseases.
摘要:
New nitropyrazole compounds of the formula ##STR1## wherein R.sub.1 is alkyl or hydroxyalkylR.sub.2 and R.sub.3, which may be the same or different, are alkyl orR.sub.2 and R.sub.3 together represent a 4- or 5-membered alkylene bridge which is optionally interrupted by an oxygen atom or by the grouping >N-R, in which R is an alkyl or hydroxyalkyl radical;And the pharmacologically compatible salts thereof, possess excellent anti-microbial action not only in vitro but also in vivo, especially systemically.
摘要:
An N-phenoxyalkylpiperidine derivative of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, an acyl radical or an optionally substituted aryl radical, R.sub.2 is a hydroxymethyl radical, a cyano group, an amidino group, an amidino group substituted by hydroxyl, a 1H tetrazol-5-yl radical or a --CO--R.sub.3 radical, R.sub.3 is a hydroxyl group, a lower alkoxy radical, an amino group, or an amino group substituted by a 1H-tetrazol-5-yl radical, X is an imino group or an oxymethyl radical, A is an alkylene radical containing 2 to 4 carbon atoms, and B is a valency bond or a 4-hydroxypyrimidin-2,5-diyl radical; or a pharmacologically acceptable salt thereof. The compounds exhibit anti-histaminic, anti-oedematous and anti-phlogistic activity.