Abstract: Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl; are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

Abstract: 1-Substituted pyrazole-5-ones of the formula ##STR1## and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen or amino;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky;X is(a) ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom;(b) propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; or(c) methylene;provided that when X is methylene, R.sup.1 is not hydrogen if R is amino;R.sup.

Abstract: Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

Abstract: Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl; are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

Abstract: Pyrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein R is hydrogen, trifluoromethyl or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is mono- or di-substituted aryl, naphthyl, or pyridyl;R.sup.4 is R.sup.5 CO wherein R.sup.5 is alkyl unsubstituted or substituted by 1, 2 or 3 halogen moieties, by alkoxy, or by mono- or dialkylamino; lower alkoxy; dialkylamino; thiophene; phenyl unsubstituted or substituted by 1 or 2 alkyl, trifluoromethyl, alkoxy, nitro or halogen moieties; or a 5- to 7-membered heterocycle unsubstituted or substituted by 1 or 2 halogen, alkyl or nitro moieties; orR.sup.4 is Z--SO.sub.2 wherein Z is alkyl, phenyl or phenyl substituted by 1 or 2 alkyl, halogen, nitro, trifluoromethyl or trifluoromethylsulphonyl moieties; or dichloroquinoxalinyl.The pyrazole derivatives and their salts are useful as diuretics, saluretics and antihypertensives.

Abstract: 1-Substituted pyrazol-5-ones of the formula ##STR1## and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen, amino, alkyl, alkenyl, phenyl or trifluoromethyl;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl;R.sup.2 is alkyl; andR.sup.3 is pyridyl, aryl or substituted by:A. 1 or 2 of the same or different substitutents selected from the group consisting of halogen, trifluoromethyl, lower alkyl, lower alkenyl and lower alkoxy;B. cycloalkyl of 5, 6 or 7 carbon atoms or cycloalkenyl of 5, 6 or 7 carbon atoms;C. mono(lower alkyl)amino, di(lower alkyl)amino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, di(lower alkyl)carbamoyl, sulphamyl, lower alkylsulphamyl, di(lower alkyl)sulphamyl, or --SO.sub.n lower alkyl wherein n is 0, 1 or 2;D.

Abstract: 1-Substituted-3-amino-pyrazol-5-ones of the formula ##STR1## or a pharmaceutically acceptable non-toxic salt thereof wherein R is a substituted phenyl or naphthyl group or unsubstituted .beta.-naphthyl, anthryl or phenanthryl which exhibit strong diuretic, saluretic and anti-hypertensive effects.

Abstract: Pyrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable nontoxic salts thereof WHEREINR is hydrogen, trifluoromethyl or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is aryl substituted by:A. one or two of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl, alkenyl and alkoxy;B. one substituent selected from the group consisting of alkylamino, dialkylamino wherein the alkyl moieties may form a heterocyclic ring with the nitrogen atom to which they are attached, cycloalkyl, cycloalkenyl, trifluoromethoxy, nitro, cyano, carbonamido unsubstituted or substituted by 1 or 2 alkyl moieties, sulphonamido unsubstituted or substituted by 1 or 2 alkyl moieties, and SO.sub.n -alkyl wherein n is 0, 1 or 2;C.

Abstract: 1-Substituted-3-amino-pyrazol-5-ones of the formula ##STR1## or a pharmaceutically acceptable non-toxic salt thereof wherein R is A. PHENYL SUBSTITUTED BY ONE OR TWO IDENTICAL OR DIFFERENT SUBSTITUENTS SELECTED FROM THE GROUP CONSISTING OF ALKYL, PHENYL, TRIFLUOROMETHYL, TRIFLUOROMETHOXY, NITRO, CYANO, FLUORO, BROMO, IODO, LOWER ALKYLAMINO, A CARBONAMIDO MOIETY OF THE FORMULA ##STR2## and a sulphonamido moiety of the formula ##STR3## wherein R.sub.1 and R.sub.2 are each hydrogen or straight or branched chain alkyl of 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached may be linked together to form a 5-, 6- or 7-membered heterocyclic ring wherein the nitrogen atom is the only heteroatom or wherein oxygen is also present as a ring member;B.

Abstract: 1-Substituted pyrazole-5-ones of the formula ##STR1## and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen or amino;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky;X isA. ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom;B. propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; orC. methylene;Provided that when X is methylene, R.sup.1 is not hydrogen if R is amino;R.sup.2 is aryl unsubstituted or substituted by:A.

Abstract: 1-[2-(.beta.-Naphthyloxy)ethyl]-3-methylpyrazolone-(5) and its salts are useful in the treatment and prophylaxis of thrombotic conditions. The compound is prepared through the reaction of 2-(.beta.-naphthyloxy)ethylhydrazine with either an acetoacetate or an ester of tetrolic acid, or through the condensation of 3-methylpyrazolinone-(5) with a derivative of 2-(.beta.-naphthyloxy)ethane, optionally with subsequent salt formation.

Abstract: Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##STR1## or a pharmaceutically acceptable nontoxic salt thereof wherein R is hydrogen, lower alkyl or amino;X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl;Y is a direct bond, oxygen or sulphur, provided that when X is methylene wherein 1 hydrogen atom is substituted by alkyl of 1 to 4 carbon atoms, Y is a direct bond; Z is aryl of 6 to 10 carbon atoms unsubstituted or substituted by:A.

Abstract: 1,4-Dihydropyridines characterized by a carbo(arylalkoxy) group in the 5-position, an aryl group in the 4-position and a alkanoyl or carbalkoxy group in the 3-position and further optionally substituted in the 1,2 and 6-positions are coronary dilating, spasmolytic and hypotensive agents. The compounds, of which 2,6-dimethyl-3-carbomethoxy-4-(2-nitrophenyl)-5-carbobenzoxy-1,4-dihydropy ridine is a representative embodiment, are prepared through the reaction of an ylidene-.beta.-dicarbonyl compound, which may be generated in situ from the corresponding .beta.-dicarbonyl compound and an aldehyde, and an enaminocarboxylic acid ester, which may also be generated in situ from a .beta.-dicarbonyl compound and an amine.

Abstract: Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##STR1## or a pharmaceutically acceptable nontoxic salt thereof wherein R is hydrogen, lower alkyl or amino;R.sup.1 is lower alkyl, alkenyl of 2 to 4 carbon atoms, monoaryl or monoaralkyl unsubstituted or substituted in the aryl moiety by 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, halogen, nitro, cyano and trifluoromethyl;X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl;Y is a direct bond, oxygen or sulphur, provided that when X is methylene, Y is a direct bond; andZ is aryl unsubstituted or nuclear substituted by:A. 3 halogens;B.

Abstract: A new class of 1,4-dihydropyridines which are characterized by the presence of ester substitutes at positions 3 and 5 of the nucleus and by the presence of an alkoxyalkyl have particular application as coronary dilators, antifibrillators, anti-hypertensives, and as muscular and vascular spasmolytics.

Abstract: Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereofWhereinR is hydrogen, lower alkyl or amino;X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl;Y is a direct bond, oxygen or sulphur, provided that when X is methylene wherein 1 hydrogen atom is substituted by alkyl of 1 to 4 carbon atoms, Y is a direct bond;Z is aryl of 6 to 10 carbon atoms unsubstituted or substituted by:A. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkenyl or 2 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, and alkenoxy of 2 to 4 carbon atoms;B.

Abstract: 1-Substituted pyrazol-5-ones of the formula ##STR1## and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen, amino, alkyl, alkenyl, phenyl or trifluoromethyl;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl;R.sup.2 is alkyl; andR.sup.3 is pyridyl, or aryl substituted by:A. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, lower alkyl, lower alkenyl and lower alkoxy;B. cycloalkyl of 5, 6 or 7 carbon atoms or cycloalkenyl of 5, 6 or 7 carbon atoms;C. mono(lower alkyl)amino, di(lower alkyl)amino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, di(lower alkyl)carbamoyl, sulphamyl, lower alkylsulphamyl, di(lower alkyl)sulphamyl, or --SO.sub.n lower alkyl wherein n is 0, 1 or 2;D.

Abstract: Pyrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable nontoxic salts thereof WHEREINR is hydrogen, trifluoromethyl or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is aryl substituted by:A. one or two of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl, alkenyl and alkoxy;B. one substituent selected from the group consisting of alkylamino, dialkylamino wherein the alkyl moieties may form a heterocyclic ring with the nitrogen atom to which they are attached, cycloalkyl, cycloalkenyl, trifluoromethoxy, nitro, cyano, carbonamido unsubstituted or substituted by 1 or 2 alkyl moieties, sulphonamido unsubstituted or substituted by 1 or 2 alkyl moieties, and SO.sub.n -alkyl wherein n is 0, 1 or 2;C.

Abstract: 1-Substituted pyrazole-5-ones of the formula ##STR1## and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen or amino;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky;X isA. ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom;B. propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; orC. methylene;Provided that when X is methylene, R.sup.1 is not hydrogen if R is amino;R.sup.2 is aryl unsubstituted or substituted by:A.

Abstract: 1-Substituted pyrazole-5-ones of the formula ##SPC1##And pharmaceutically acceptable, nontoxic salts thereof, whereinR is hydrogen or amino;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky;X isA. ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom;B. propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; orC. methylene;Provided that when X is methylene, R.sup.1 is not hydrogen if R is amino;R.sup.2 is aryl unsubstituted or substituted by:A.