Bayer Aktiengesellschaft

Friedrich Hoffmeister

Stanislav Kazda

Mithat Mardin

Otto Behner

Wolf-Dieter Busse

Karl Heinrich Mayer

Elisabeth Perzborn

Friedel Seuter

Arend Heise

Klaus Schlossmann

Volker Fiedler

Dieter Mayer

Siegismund Schutz

Wolfgang Wuttke

Rudolf Hiltmann

Erich Klauke

Horst Meyer

Friedrich Bossert

Wulf Vater

Harald Horstmann

Siegfried Raddatz

Hartmund Wollweber

Rudolf Sundermann

Helmut Heitzer

Ulrich Horlein

Siegfried Petersen

Hans Werner Schubert

Helmut Kramer

A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of nafazatrom.

Nafazatrom as a lipoxygenase inhibitor

The invention relates to pyrazolooxazines, pyrazolothiazines and pyrazoloquinolines defined herein by Formula I. The invention also includes compositions containing said Formula I compounds and methods for the use of said compounds and compositions for their lipoxygenase-inhibiting properties. Also included in the invention are methods for the manufacture of said compounds of Formula I.

Pyrazolooxazines, pyrazolothiazines, and pryazoloquinolines and their

The invention provides pharmaceutical compositions and medicaments, useful for the treatment of cerebral disorders, wherein the active compound is 1,4-dihydro-2,6-dimethyl-4-(3'-nitrophenyl)-pyridine-3-(.beta.-methoxyethy l ester)-5-(isopropyl ester). Also included in the invention are methods for the use of said compositions and medicaments.

Cerebral therapeutic agent and its use

The invention covers compounds of the formula ##STR1## in which R.sup.1 and R.sup.5 each represents 0, 1, 2, 3 or 4 of the following substituents: alkyl, hydroxyl, acyloxy, alkoxy, nitro, amino, alkylamino, dialkylamino, acylamino, acylalkylamino, alkoxycarbonylamino, halogen, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminoamino, R.sup.2 is hydrogen, optionally substituted alkyl, aralkyl or aryl or heterocyclo-alkyl, acyl or alkoxycarbonyl, and R.sup.3 and R.sup.4 are each hydrogen, or optionally substituted alkyl, aralkyl, aryl or hetero-aryl, are useful as medicaments which have an action on the central nervous system, in particular as, for example, tranquilizers and/or antiamnesics. Also included in the invention are methods for preparing said compounds, compositions containing them and methods for the use of said compounds and compositions.

Benzodiazepine-diones, a process for their production and their use as

N-Diphenylmethyl and o-biphenylenemethyl derivatives of 1-(disubstituted phenoxy)-3-amino-2-hydroxypropane and their salts are useful for combatting cerebrovascular insufficiency and producing psychostimulation in humans and other animals. The compounds, of which 1-(2-methoxy-4-allylphenoxy)-2-hydroxy-3-diphenylmethylamino-propane is a typical embodiment, can be prepared by a number of synthetic routes.

Derivatives of 1-(disubstituted phenoxy)-3-amino-2-hydroxypropanes

Enteral pharmaceutical compositions containing medicinal agents having parenteral abuse potential are rendered resistant to aqueous extraction through the incorporation of a sufficient amount of a nontoxic, water gelable material. Attempts to extract the medicinal agent for parenteral abuse are thus inhibited or prevented since the material gels in the presence of water leaving no filterable liquid.

Enteral pharmaceutical compositions

3-Hydrazinoindazoles acylated with a carbo(lower alkoxy) group in the 3-position and further being optionally substituted in one or more of the 4-, 5-, 6- and/or 7-positions are analgesic, anti-inflammatory and antipyretic agents. The compounds, of which 3-carbomethoxyhydrazino-6-chloroindazole is a typical embodiment, are prepared through treatment of the appropriate 3-hydrazinoindazole with a derivative of carbonic acid.

3-Carbo(lower alkoxy)hydrazinoindazoles

3-Aminoindazoles bearing a carbo(lower alkoxy), lower alkylamide or di(lower alkyl)amide group in the 1-or 2-position and further being optionally substituted in one or more of the 4-, 5-, 6- and/or 7-positions are analgesic, anti-inflammatory and antipyretic agents. The compounds, of which 3-amino-6-chloroindazole-1-carboxylic acid ethyl ester is a typical embodiment, are prepared through treatment of the appropriate 3-aminoindazole with a derivative of carbonic acid or through thermal isomerization.

3-Aminoindazole-1 and 2-carboxylic acid derivatives

Oximes of the formula: ##SPC1## And their acid salts, wherein A is a branched or unbranched, saturated or unsaturated alkylene chain of 0-6 carbon atoms, B is a basic nitrogen-containing group such as an amino, alkylamino, dialkylamino, cycloalkylamino, dicycloalkylamino, cycloalkylalkylamino, dicycloalkylalkylamino, alkylarylamino, alkylaralkylamino, a piperidino, pyrrolidino, hexamethyleneimino, morpholino, thiomorpholino, N-alkylpiperazino or N-(2-hydroxyalkyl)-piperazino group, n is 1 or 2 and X is --CH.sub.2 --, --(CH.sub.2).sub.3 -- or --CH = CH--, and R.sub.1 and R.sub. 2 are each hydrogen, halogen, alkyl of 1-4 carbon atoms, alkoxy, alkylmercapto groups of 1-4 carbon atoms, hydroxyl, nitro, amino or trifluoromethyl, are useful for their anti-depressant activity. Pharmaceutical compositions may be prepared which comprise an anti-depressant amount of at least one such compound in combination with a pharmaceutically acceptable inert diluent or carrier. Depression in humans and animals may be treated by administering an anti-depressant amount of such an oxime to such human or animal.

Basic oximes and their preparation

1. A compound selected from the group consisting of And pharmaceutically acceptable non-toxic acid salts thereof.

Benzomorphanes of the formula: ##SPC1## Wherein

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Wuppertal-Elberfeld, Germany

Friedrich Hoffmeister