Cassella Aktiengesellschaft

Hoechst Roussel Pharmaceuticals

Cassella Aktiengellschaft

Aventis Pharma Deutschland, Gmbh

Karl Schonafinger

Helmut Bohn

Rudi Beyerle

Melitta Just

Piero A Martorana

Rolf-Eberhard Nitz

Ursula Schindler

Helen H Ong

Volker Fiedler

Joachim Brendel

Bernd Jablonka

Eckhard Schraven

Eckard Kujath

Jorg Ostrowski

Jeffery Troke

Anton Mogilev

Hartmut Strobel

Christian Baumgartner

Helen Hu Ong

Dieter Voegele

The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: ##STR1## in which X, R.sup.1, R.sup.1a, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate 'cGMP' and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula 1, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.

Pyrazole derivatives, their preparation and their use in pharmaceuticals

The invention relates to the use of 2-(N-(2-aminoethyl)amino)acetic acid derivatives of the formula I ##STR1## in which R denotes, for example, phenyl or thienyl, and their pharmacologically acceptable acid addition salts as pharmacological active compounds.

Use of 2- (N-(2-aminoethyl)amino) acetic acid derivatives

2-(N-(2-aminomethyl)amino)acetic acid derivatives to inhibit advanced

The present invention relates to hydroxymethylfurazancarboxylic acid derivatives of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents hydroxymethyl and the other represents ##STR2## where X represents NR.sup.3 R.sup.4, OH or OR.sup.7, and R.sup.3, R.sup.4 and R.sup.7 are defined as indicated in claim 1, to processes for their preparation and to their use.

Hydroxymethylfurazancarboxylic acid derivatives

The present invention relates to phenyl-1,2,5-oxadiazolecarboxamide-2-oxides of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents ##STR2## and the other represents ##STR3## and R.sup.3 and R.sup.4 are defined as indicated in claim 1, to processes for their preparation and to their use for the treatment of disorders of the cardiovascular system, including angina pectoris and erectile dysfunctions.

Phenyl-1,2,5-oxadiazolecarboxamide-2-oxides, their preparation and their

The present invention relates to 3-(cis-2,6-dimethylpiperidino)sydnone imine salts of the general formula I ##STR1## in which X denotes H.sub.2 PO.sub.4 or ##STR2## processes for their preparation and their use.

Salts of 3-(cis-2,6-dimethylpiperidino) sydnone imine

The present invention relates to phenylfuroxans of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents phenyl and the other represents ##STR2## where R.sup.3, R.sup.4 and n are defined as indicated in claim 1, processes for their preparation and their use.

Phenylfuroxans

The present invention relates to pyrimidofuroxans of the general formula I ##STR1## in which A denotes ##STR2## where in each case the nitrogen atom is bonded via the C-4 and the carbon atom via the C-3 of the furoxan ring and the R radicals are defined as indicated in Claim 1, processes for their preparation and their use for the control and prevention of disorders of the cardiovascular system, in particular for the control and prevention of angina pectoris, and for the treatment of erectile dysfunctions.

Pyrimidofuroxans, their preparation and their use

The present invention relates to pyridyl-1,2,5-oxadiazolcarboxamide-2-oxides of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents pyridyl and the other represents ##STR2## and R.sup.3 and R.sup.4 are defined as indicated in claim 1, processes for their preparation and their use.

Pyridyl-1,2,5-oxadiazolecarboxamide-2-oxides

The present invention relates to fused 1,2,5-oxadiazole-2-oxides of the general formula I ##STR1## in which A denotes ##STR2## and X, Y, Z as well as R.sup.1, R.sup.2, R.sup.3 and n are defined as indicated in Claim 1, to processes for their preparation and to their use for the control and prevention of disorders of the cardiovascular system, in particular for the control and prevention of angina pectoris, and for the treatment of erectile dysfunctions.

Fused 1,2,5-oxadiazole-2-oxides and their use

Substituted 3-aminosydnonimines of the formula I ##STR1## and pharmacologically acceptable acid addition salts thereof, in which R.sup.1 denotes hydrogen or the radical --COR.sup.4,

Substituted 3-aminosydnonimines

The invention relates to pharmacologically active substituted 3-aminosydnone imines of the general formula I ##STR1## in which n denotes 0 or 1, and their pharmacologically acceptable salts and acid addition salts, and to a process for the preparation of the compounds according to the invention and their use.

Substituted 3-aminosydnone imines and salts thereof

There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.

Dihydro-4(hydroxyalkyeneamino)quinolines

Substituted 3-aminosydnone imines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sup.1 denotes e.g. hydrogen;

Substituted 3-aminosydnone imines

The present invention relates to pharmacologically active substituted 3-dicyclohexylaminosydnone imines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sup.1 denotes hydrogen or the radical --COR.sup.2 and R.sup.2 denotes (C.sub.1 to C.sub.4)-alkyl, (C.sub.1 to C.sub.4)alkoxy-(C.sub.1 to C.sub.4)alkyl, (C.sub.1 to C.sub.4) alkoxy, (C.sub.1 to C.sub.4)alkoxy-(C.sub.1 to C.sub.4 )alkoxy, (C.sub.5 to C.sub.7)cycloalkyl, phenyl, a phenyl radical which is mono-, di- or trisubstituted by 1 to 3 halogen atoms and/or 1 to 3 alkyl radicals having 1 to 4 C atoms and/or 1 to 3 alkoxy radicals having 1 to 4 C atoms, a nicotinoyl radical or an allylmercaptoacetyl radical, and to a process for the preparation of the compounds according to the invention and their use.

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Alzenau, Germany

Karl Schonafinger