Bayer Aktiengesellschaft

Gunter Thomas

Matthias Schramm

Rainer Gross

Siegfried Goldmann

Gerhard Franckowiak

Jurgen Stoltefuss

Horst Boshagen

Horst Meyer

Michael Kayser

Friedrich Bossert

Martin Bechem

Ulrich Rosentreter

Fred R Heiker

Andreas Knorr

Stanislav Kazda

Bodo Junge

Robertson Towart

Rudiger Sitt

Bernward Garthoff

Karl-Heinz Schlemmer

Elisabeth Perzborn

Thomas Schenke

Egbert Wehinger

Erwin Bischoff

Rolf Grosser

Friedel Seuter

Walter Puls

Helmut Haning

Lutz Muller

Ulrich Niew&ouml;hner

J&ouml;rg Keldenich

Hans P Krause

Bernd Pelster

Benward Garthoff

Rosentreter Ulrich

Ulrich Bartke

Klaus Gorlitzer

Helmuth Sch{umlaut Over (u)}tz

The 1,5-dihydro-pyrazolo&lsqb;3,4-d&rsqb;-pyrimidinone derivatives are prepared by fusing the pyrimidone heterocycle with the suitably substituted pyrazoles. The compounds are suitable as active compounds in medicaments, in particular in medicaments for the treatment of cardiovascular and cerebrovascular diseases, diseases of the peripheral blood vessels and diseases of the urogenital tract.

1,5-dihydro-pyrazolo&lsqb;34-D&rsqb;-pyrimidinone derivatives

A composition effective for treating circulation disorders comprises a mixture of ##STR1## wherein the variables can have varied meetings. I are inotropic and II are vasodilating but, whereas the ingredients in the combination would be expected to be antagonistic, they are reinforcing.

Mixture of different dihydropyridines

Circulatory system-active novel dihydropyrimidines of the formula ##STR1## in which R.sup.1 and R.sup.6 are diverse organic radicals, and pharmacologically acceptable addition salts thereof.

Circulation-active 4-phenyl-6-substituted dihydropyrimidines

5-Aryl-1,4-dihydropyridines of the formula ##STR1## in which R

Circulation active novel 5-aryldihydropyridines

Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,

Circulation-active 1,4-dihydropyridines

Novel cardioactive compounds of the formula ##STR1## in which R.sup.1 is alkyl, aryl or heterocyclic, preferably substituted phenyl,

Circulation-active 3-amino-dihydropyridines

Pure enantiomers of 5-nitrodihydropyridine of the formula ##STR1## are mixed, wherein one of the enantiomers has a high vasodilative action and a low negative inotropic activity on heart muscle, the other enantiomer has a low vasoconstrictive action and a high positive inotropic activity on heart muscle, the mixture being high in vasodilative activity and in positive inotropic activity on heart muscle.

Mixtures of optically active nitrodihydropyridines active on the

1-Oxo-1,3,4,7-tetrahydrobenzofuranes of the formula ##STR1## in which X is O or S,

1-oxo-1,3,4,7-tetrahydrobenzo[C]furans

Novel compounds of the formula ##STR1## in which R.sup.2 is hydrogen or a substituent, and

Circulation active pyrimidinyl-dihydropyridines

1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.

Circulation active dihydropyridine-3-carboxamides

Hydroxytetrahydropyridinelactones of the formula ##STR1## in which R represents a phenyl, naphthyl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, quinolyl, isoquinolyl, indolyl, benzimidazolyl, quinazolyl, quinoxalyl, thionaphthenyl, isothionaphthenyl, chromonyl, thiochromonyl, chromenyl, thiochromenyl, benzoxadiazolyl or benzthiadiazolyl radical, and the stated radicals may carry 1 to 3 identical or different substituents from the group comprising C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkinyl, C.sub.1 -C.sub.20 -alkoxy, fluorine, chlorine, bromine, iodine, trifluoromethyl, monofluoro-C.sub.1 -C.sub.10 -alkoxy, polyfluoro-C.sub.1 -C.sub.10 -alkoxy, hydroxyl, amino, mono-C.sub.1 -C.sub.10 -alkylamino, di-C.sub.1 -C.sub.10 -alkylamino, nitro, cyano, azido, carboxyl, carb-C.sub.1 -C.sub.10 -alkoxy, carboxamido, sulphonamido, SO.sub.m -alkyl (m=0 to 2, 1 to 20 C atoms), phenyl, benzyl, benzyloxy or benzylthio, it being possible for the 4 last-mentioned substituents to carry 1 to 3 radicals from the group comprising C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -alkylthio, fluorine, chlorine, bromine, iodine, cyano, nitro, azido, hydroxyl, trifluoromethyl, amino, C.sub.1 -C.sub.6 -alkylamino or di-C.sub.1 -C.sub.6 -alkylamino,

Circulation-active hydroxy-tetra-hydropyridinelactones

Novel 3-nitro-dihydropyridine derivatives of the formula ##STR1## in which R.sub.1 and R.sub.2 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkylmercapto, ##STR2## Z is oxygen or sulphur, R.sub.4 and R.sub.5 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkoxy or nitro, or

Positive inotropic 3-nitro-5-substituted ester and

Tetrahydrothienopyridines of the formula ##STR1## in which R is optionally substituted aryl or heterocyclyl,

Circulation-active tetrahydrothienopyridines

Novel chromone-8-aldehydes and thiochromone-8-aldehydes, useful in making pharmaceutically active dihydropyridines, of the formula ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1 -C.sub.10 aliphatic hydrocarbon radical, a C.sub.1 -C.sub.10 alkyl carboxylate, or an aromatic or heteroaromatic ring which optionally has 1-5 identical or different halogen, C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulphinyl, cyano, hydroxyl, nitro, C.sub.1 -C.sub.5 -monofluoroalkyl or polyfluoroalkyl, C.sub.1 -C.sub.5 monofluoroalkoxy or polyfluoroalkoxy, C.sub.1 -C.sub.6 monofluoroalkylthio or polyfluoroalkylthio, amino, C.sub.1 -C.sub.5 -monoalkylamino or C.sub.1 -C.sub.5 dialkylamino substituents,

Intermediate 8-carboxaldehyde-(-chromone and -thiochromone) derivatives

4-(Nitrophenyl)-1,2,3,4-tetrahydropyridines of the formula ##STR1## in which R.sub.1 and R.sub.2 are identical or different and each represent hydrogen, phenyl or a straight-chain or branched alkyl radical which is optionally substituted by halogen or alkoxy,

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Wuppertal, Germany

Gunter Thomas