Boehringer Mannheim Gmbh

Wolfgang Weckerle

Rupert Herrmann

Werner Guthlein

Hans-Georg Batz

Klaus Strein

Wolfgang-Reinhold Knappe

Ulfert Deneke

Egon Roesch

Harvey Buck

Hans Wielinger

Heino Eikmeier

Helmut Michel

Manfred Kuhr

Helmut Freitag

Fritz Wiedemann

Hans-Joachim Guder

Herbert Buschek

Johann Berger

Wolfgang Kleeman

Rudolf Machat

The present invention concerns compounds having the general formula I ##STR1## in which R.sup.1 denotes hydrogen or hydroxy,

Diphenylmethane derivatives, process for their production and their use

A method of detecting hydrolase activity using as substrates the compounds of the formula ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 is C.sub.1 -C.sub.4 alkyl, or phenyl optionally substituted in the meta- or para- position by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or mono- or di-(C.sub.1 -C.sub.6)-alkylamino, or optionally substituted by an O-X group in which X is a glycosyl, phosphate or acyl moiety of a natural substrate of the corresponding glycosidase, phosphatase or esterase.

Agents for the detection of substrates with hydrolase activity

The invention provides new redox indicators and uses for these redox compounds (I): ##STR1## Wherein X is oxygen or sulphur, R.sub.1 is julolidine or tetrahydroquinoline, which can carry an alkyl radical on the nitrogen atom which, in turn, can be substituted by a sulphuric, phosphonic or carboxylic acid residues, or is (II); wherein R.sub.4 is hydroxyl or a mono- or dialkylated amino group, R.sub.5 and R.sub.6, which can be the same or different, are hydrogen, alkyl or alkoxy, R.sub.2 is hydrogen or alkyl, julolidine or tetrahydroquinoline, which can carry an alkyl on the nitrogen atom which alkyl can be substituted by sulphuric, phosphonic or carboxylic acids, or is III; wherein R.sub.5 and R.sub.6 are the same as in R.sub.1 and R'.sub.4 is hydroxyl, an amino or a mono-or dialkylated amino group, whereby the alkyl radicals can be substituted one or more times by hydroxyl, alkoxy, halogen, morpholine or a sulphuric, carboxylic or phosphonic acid residue, which acids can also be esterified, and R.sub.3 is the same as R.sub.2 or is an alkyl substituted by hydroxyl, alkoxy, dialkylamino or phenyl, or is cycloalkyl, phenyl or pyridyl; as well as the salts thereof.

New redox indicators

The present invention provides phenolsulphonphthaleinyl-.beta.-D-galactosides of the general formula: ##STR1## wherein R.sup.1 to R.sup.4, which can be the same or different, are hydrogen or halogen atoms or nitro or amino groups, R.sup.5 to R.sup.12, which can be the same or different, are hydrogen or halogen atoms or lower alkyl, hydroxyl, lower alkoxy, carboxyl or nitro groups and M.sup.+ is a proton, an alkali metal, alkaline earth metal or ammonium ion. The present invention also provides a process for preparing these galactosides and diagnostic agents containing them.

Phenolsulphonphthaleinyl-.beta.-D-galactosides and diagnostic agents

The present invention provides heteroaryloxypropanolamines and pharmaceutical compositions containing them, for combating, and for the prophylaxis of, cardiac and circulatory diseases. The heteroaryloxypropanolamines of the present invention are of the general formula: ##STR1## wherein A is a bi- or tricyclic heteroaromatic radical, which is optionally partly hydrogenated, X is a straight-chained or branched alkylene chain containing 2 to 6 carbon atoms, R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or lower alkyl or benzyl radicals, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or lower alkyl, benzyl, formyl, lower alkanoyl, cyano, hydroxymethyl, lower alkoxycarbonyl or carbamoyl radicals or the divalent substituents sulfur or oxygen and R.sub.6, R.sub.7 and R.sub.8, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, nitro, amino, lower alkylthio or lower alkoxy radicals or R.sub.6 and R.sub.7 together represent an optionally unsaturated trimethylene chain; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

Indazoloxypropanolamine derivatives and use in combating, and for the

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Grunstadt, Germany

Wolfgang Weckerle