Ludwig Heumann & Co. Gmbh

Heumann Pharma Gmbh & Co.

Kurt H Ahrens

Helmut Schickaneder

Peter Morsdorf

Istvan Szelenyi

Rolf Herter

Heidrun Engler

Stefan Postius

Walter Schunack

Ingomar Grafe

Volker Pfahlert

Kay Brune

Armin Buschauer

Istvan Szeleny

Hartmut Vergin

Kurt Wegner

Walter Otto Liebenow

Sigurd Elz

Gert Baumann

Edgar Fritschi

Manfred Haake

Herbert Hansen

Reinhold Weidner

Peter W Jungblut

Volker Pfanhlert

Geidrun Engler

Reinhold Pothmann

Lothar Kisielowski

Peter Mosdorf

Klaus Hoxer

Irene Kramer

New benzimidazoles correponding to the general formula I ##STR1## are described, in which the pyridazinone ring is attached in the 5- or 6- position of the benzimidazole ring and R.sup.1 denotes a hydrogen atom or a straight chained or branched C.sub.1 to C.sub.4 alkyl group, R.sup.2 denotes a hydrogen atom, a straight chained or branched C.sub.1 to C.sub.4 alkyl group, a C.sub.1 to C.sub.4 alkoxy group, a hydroxy group, a halogen atom, an amino group or a nitro group, A denotes a hydrogen atom, a group of the formula ##STR2## wherein R.sup.3 denotes a hydrogen atom, an optionally substituted C.sub.1 to C.sub.4 alkyl group or a C.sub.1 to C.sub.4 alkoxy group and B denotes a cyano group, a benzoyl group or a phenylsulphonyl group, or A denotes a group of the formula ##STR3## in which m has the value 2 or 3 and n represents an integer from 1 to 6, and the physiologically acceptable salts thereof as well as processes for their preparation and pharmaceutical preparations. containing these compounds These compounds are new, effective, positive inotropic substances which do not act by the mechanism of phosphodiesterase inhibition.

Benzimidazoles and pharmaceutical preparations containing these compounds

The invention relates to pyrimidine-thioalkyl pyridine derivatives corresponding to the following general formula ##STR1## in which R.sub.1 to R.sub.4, independently of one another, represent hydrogen, lower alkyl, halogen, amino or hydroxy groups, R.sub.5 represents a free electron pair or a lower alkyl group, a halogen atom, m has the value 0 or 1, the pyrimidine-thioalkyl group being bonded in the 2-, 3- or 4-position of the pyridine ring, and to therapeutically compatible acid addition salts thereof. The invention also relates to a process for producing the new pyrimidine-thioalkyl pyridine derivatives and to medicaments containing these compounds.

Pyrimidine-thioalkyl pyridine derivatives, medicaments containing these

New imidazolylalkyl-guanidine derivatives are described, which by virtue of their agonistic action on histamine-H.sub.2 receptors and in part also due to their additional H.sub.1 -antagonistic receptor activity can be used in the treatment of cardiac diseases, certain forms of hypertension and diseases of arterial occlusion. These imidazolylalkyl-guanidine derivatives correspond to the general formula I: ##STR1##

Imidazolyl alkyl guanidine derivatives, processes for their preparation

A new process for the preparation of 2,6-dichlorodiphenylamine derivatives is described, which process provides the desired active compound in a high yield and with a very high degree of purity by a technically simple and realizable procedure.

Process for the preparation of 2,6-dichlorodiphenylaminoacetic acid

This invention relates to new stereochemically pure and stable adducts of Z-1-(p-.beta.-dimethylaminoethoxyphenyl)-1-(p-hydroxyphenyl)-2-phenyl-but- 1-ene and certain solvents which by virtue of their marked antioestrogenic activities may be used for the therapeutic treatment of benign breast diseases and hormone-dependent mammary tumors, in particularly by percutaneous application.

Stable solvent adducts of

New 6-oxo-pyridazine derivatives corresponding to the general formula I ##STR1## which represent new, positive inotropic compounds having a higher and more selective inotropy-increasing activity are described. A process of preparation and the medical use of these substances or of a medicament containing these substances are also described.

6-oxo-pyridazine derivatives, a process for their preparation and

A new process for the preparation of the nitroethane derivatives, ranitidine and nizatidine, is described which takes place via intermediate products and enables the said compounds to be prepared with a higher degree of purity. Another advantage is that in contrast to the known processes, it is not accompanied by the liberation of the highly toxic and malodorous compound, methylmercaptan.

Process for the preparation of nitroethene derivatives

New benzimidazoles corresponding to the general formula I ##STR1## are described, in which the pyridazinone ring is attached in the 5- or 6- position of the benzimidazole ring and R.sup.1 denotes a hydrogen atom or a straight chained or branched C.sub.1 to C.sub.4 alkyl group, R.sup.2 denotes a hydrogen atom, a straight chained or branched C.sub.1 to C.sub.4 alkyl group, a C.sub.1 to C.sub.4 alkoxy group, a hydroxy group, a halogen atom, an amino group or a nitro group, A denotes a hydrogen atom, a group of the formula ##STR2## wherein R.sup.3 denotes a hydrogen atom, an optionally substituted C.sub.1 to C.sub.4 alkyl group or a C.sub.1 to C.sub.4 alkoxy group and B denotes a cyano group, a benzoyl group or a phenylsulphonyl group, or A denotes a group of the formula ##STR3## in which m has the value of 2 or 3 and n represents an integer from 1 to 6, and the physiologically acceptable salts thereof as well as processes for their preparation and pharmaceutical preparations containing these compounds. These compounds are new, effective, positive inotropic substances which do not act by the mechanism of phosphodiesterase inhibition.

Benzimidazoles, and pharmaceutical preparations containing these

New dihydropryidazinone derivatives corresponding to the following formula ##STR1## and a process for their preparation and pharmaceutical preparations containing these compounds are described. These compounds are effective positively inotropic substances with an improved therapeutic profile.

Dihydropyridazinone derivatives, a process for their preparation and

The invention relates to new 1,4-piperazine compounds corresponding to the following general formula ##STR1## which show improved antimycotic activity in relation to the known compounds miconazol and ketoconazol.

4-[4-[[2-(halophenyl)-2-[1H-tr:azol(or

A new anhydrous crystalline form of prazosine hydrochloride characterized by the following bands in the infra-red spectrum in potassium bromide is described:

Crystalline, anhydrous sigma-form of

New compounds which act on the cardiac circulation and correspond to the general formula ##STR1## and may be used for the treatment of cardiac diseases, in certain forms of hypertension and in diseases of arterial occlusion are described. Methods of preparation for these compounds and medicaments containing these compounds are also described.

1,4-dihydropyridine derivatives

1,3,4-Thiadiazole derivatives corresponding to the general formula I ##STR1## which constitute highly effective inhibitors for histamine-H.sub.2 receptors are described. These compounds in addition have a cytoprotective action.

1,3,4-Thiadiazole derivatives and pharmaceutical preparations useful as

Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group or R.sup.6 and R.sup.7 represent the group ##STR6## wherein R.sup.14 denotes a linear C.sub.1 -C.sub.3 -alkyl group, as well as the physiologically acceptable salts thereof, a process for the preparation of these compounds, and a pharmaceutical preparation containing them, are described.

Benzothiazole derivatives, processes for their preparation and

3,4-Diazole derivatives corresponding to the general formula I ##STR1## which exert a highly selective action on histamine-H.sub.2 receptors are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.

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Nuremberg, Germany

Kurt H Ahrens