Schering Aktiengesellschaft

Clemens Rufer

Helmut Biere

Eberhard Schroder

Hanns Ahrens

Olaf Loge

Ekkehard Schillinger

Wolfgang Losert

Henning Koch

Hans-Joachim Kessler

Irmgard Boettcher

Ralph Schmiechen

Eberhard Schroeder

Joachim-Friedrich Kapp

Eberhard Schroeder, Deceased

Gerald Kirsch

Katica Schwarz

Irmgard Bottcher

Manfred Lehman

Hans Ahrens

Diphosphonic acid derivatives of the formula ##STR1## wherein X is cyano, 2-cyanoethyl, or 3- aminopropyl and Y is H, or X and Y together represent dimethylaminomethylene ((CH.sub.3).sub.2 NCH.dbd.), and

Diphosphonic acid derivatives and pharmaceutical preparations containing

An indanyl derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 are identical or different, and each is hydrogen, fluorine or chlorine

Indanyl derivatives, their preparation and use

Diphosphonic acid derivatives of Formula I ##STR1## wherein R is hydrogen, an alkali metal atom, an alkaline earth metal atom, or an alkyl group of 1-4 carbon atoms and

Compounds of the formula ##STR1## wherein n is 0, 1, or 2;

Benzofuran derivatives of the formula ##STR1## wherein V is hydrogen or acetyl,

Benzofuran derivatives and their pharmaceutical use

Phenylacetic acid derivatives of the formula ##STR1## wherein n is an integer of 2 to 5; ##STR2## R.sub.1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R.sub.2 and R.sub.3 each independently is hydrogen or lower alkyl; or together form an ethylene group;

Novel phenylacetic acid derivatives

Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, methanesulfonyl, or acetyl,

Indanyl derivatives and use

Indanyl derivatives of the formula ##STR1## wherein AR is phenyl, pyridyl, or phenyl or pyridyl substituted by halogen, alkyl of 1-4 carbon atoms or trifluoromethyl; X is oxygen or a sulfur; R.sub.1 is alkyl of 1-4 carbon atoms or alkyl of 1-4 carbon atoms substituted by fluorine or chlorine; A is ##STR2## Y is oxo, oximino, C.sub.1-4 -alkoximino of 1-4 carbon atoms, phenylhydrazono or p-toluenesulfonylhydrazono; n is 0, 1 or 2; R.sub.2 is alkyl of 1-4 carbon atoms, phenyl or phenyl substituted by halogen, alkyl of 1-4 carbon atoms, nitro or carboxy; Z is hydroxy, acyloxy of 1 to 6 carbon atoms, R.sub.1 SO.sub.3 -- amino, acylamino of 1 to 6 carbon atoms, R.sub.1 SO.sub.2 NH-- or cyano, and V is hydrogen, acyl of 1 to 6 carbon atoms or R.sub.1 SO.sub.2 --, and the salts thereof with physiologically acceptable bases or acids have valuable pharmacological and herbicidal activity.

Indanyl derivatives and their use

Thiophene derivatives of the formula ##STR1## WHEREIN R.sub.x is --S-CHR.sub.5 -COOH or --S-CH.sub.2 -CH.sub.2 -OH, R.sub.y is 1-2 of halogen alkoxy of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, phenyl, halophenyl or alkylcarbonyl of 1-6 carbon atoms in the alkyl group, and R.sub.5 is a hydrogen atom, when R.sub.y is a halogen atom, when R.sub.5 is alkyl, their enantiomers, and their pharmacologically acceptable salts thereof with bases, possess antilipolytic activity.

Thiophene derivatives having antilipolytic activity

Carbazoles of the formula ##STR1## wherein R.sub.1 is hydroxymethyl, alkanoyloxymethyl, tetrazolyl, cyano, oximinocarbonyl, aminocarbonyl, carboxyl and salts thereof with physiologically acceptable bases and the esters thereof with physiologically acceptable alcohols and amides thereof with physiologically acceptable amines, R.sub.2 through R.sub.6 each are a hydrogen atom, halogen atom, lower alkyl, trifluoromethyl, or lower alkoxy, or R.sub.5 and R.sub.6 collectively are a five- or six-membered isocyclic ring, and R.sub.7 is a hydrocarbon of 3-8 carbon atoms or, when at least one of the R.sub.2 through R.sub.6 is other than a hydrogen atom, a hydrogen atom, methyl or ethyl, And the corresponding compounds wherein R.sub.7 is a hydrogen atom, methyl or ethyl, And the 5,6,7,8-tetrahydrocarbazoles, possess topical anti-inflammatory activity.

5,6,7,8:Tetrahydrocarbazole-1-carboxylic acid derivatives

2-(5-Nitro-2-imidazolyl)-benzimidazoles of the formula ##STR1## wherein R.sub.1 and R.sub.2 are H, halo, alkyl, alkoxy, nitro, trifluoromethyl or carboxy; A is H, alkyl, hydroxyalkyl or an ester thereof, haloalkyl, phenyl or a tertiary aminoalkyl group; and X is alkyl, hydroxyalkyl or an ester thereof, are antimicrobials, especially against Trichomonas vaginalis.

2-(5-Nitro-2-imidazolyl)-benzimidazoles

Nitroimidazoles of the formula ##STR1## wherein R is dialkylaminoacryloyl; 3-, 4-, or 5-pyrazolyl or a mixture thereof which is unsubstituted or substituted by alkyl or, at the 1-position, by hydroxyalkyl or a nitro ester thereof, acyloxyalkyl, nitro, phenyl or phenyl p-substituted by halo, alkoxy or nitro, or, in the 3- or 5-position or a mixture thereof by nitro; 3- or 5-alkyl-4-isooxazolyl or a mixture thereof; or 4-alkyl-5-pyrimidinyl, unsubstituted or substituted by alkyl, amino, 2-furyl or 5-nitro-2-furyl, and the physiologically acceptable acid addition salts thereof, possess anti-protozoal activity, e.g., against trichomonas vaginalis and Entamoeba histolytica.

Nitroimidazole derivatives and process for the preparation thereof

Thiophene derivatives of the formula ##STR1## IN WHICH R.sub.x is --S--CHR.sub.5 --CONHOH or --S--CHR.sub.5 -5-tetrazolyl in which R.sub.5 is H or alkyl of 1-6 carbon atoms and R.sub.y is 0-2 of alkyl or alkoxy of 1-6 carbon atoms or halogen, and their pharmacologically acceptable salts with bases, possess antilipolytic activity.

Novel thiophene derivatives and their preparation

Thiophene derivatives of the formula ##STR1## WHEREIN R.sub.x is --S-CHR.sub.5 -COOH or -S-CH.sub.2 -CH.sub.2 -OH, R.sub.y is 1-2 of halogen alkoxy of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, phenyl, halophenyl or alkylcarbonyl of 1-6 carbon atoms in the alkyl group, and R.sub.5 is a hydrogen atom, when R.sub.y is a halogen atom, when R.sub.5 is alkyl, their enantiomers, and their pharmacologically acceptable salts thereof with bases, possess antilipolytic activity.

Thiophene derivatives and their preparation

Amino-substituted nitroimidazolyl-methyleneaminoimidazolidinones of the formula ##SPC1## Wherein --NR.sub.2 R.sub.3 is dialkylamino or heterocyclic amino, and the physiologically acceptable salts thereof, possess antitrichomonial activity.

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Berlin, Germany

Clemens Rufer