Boehringer Mannheim Gmbh

Roche Diagnostics Gmbh

Otto-Henning Wilhelms

Walter-Gunar Friebe

Wolfgang Kampe

Androniki Roesch

Max Thiel

Werner Winter

Wolfgang Schaumann

Egon Roesch

Peter Stahl

Erhard Reinholz

Jurgen Mertin

Herbert Von Der Eltz

Gisbert Sponer

Hans Seidel

Kurt Stach, Deceased

Heidrun Anke

Peter Wunderwald

By Werner Plattner, Administrator

Fritz Hansske

Erika Von Mullendorff

Herman Hindermayr

Robert Umminger

Marcel Linssen

The present invention relates to the method of treating leukemia, lymphoma or inhibiting the proliferation of cells with a compound of formula I.

Use of thiadiazolo&lsqb;4,3-a&rsqb;pyridine derivatives

Pyridine compounds which have useful pharmaceutical activity

Use of macrolactones as anti-allergics

The present invention provides a one-step process for the detection of the presence of an allergy and for the specific detection of the allergen responsible for the allergy, in which the leukocytes of a sample to be investigated are incubated with an allergen or with another stimulation factor in an aqueous medium together with a chromogenic protease substrate and calcium ions, the liberated protease is reacted with the chromogen and the resulting chromophor is determined. The protease activity is measured kinetically after an incubation period by the increase of the chromophor concentration. The present invention also provides a reagent and a device for carrying out this process, as well as a process for the determination of antiallergic and anti-inflammatory substances. The device consists of a microtiter plate with a plurality of different reagents arranged in rows.

Process for the detection of an allergy or an anti-allergic substance

The present invention provides compounds of the general formula: ##STR1## wherein Ar is a phenyl radical optionally substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, A is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 aliphatic hydrocarbon radical which is optionally substituted by a hydroxyl group, n is 0, 1 or 2, B is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 -aliphatic hydrocarbon radical and R is 5-(1H)-tetrazolyl, --CO--NH-tetrazolyl, ##STR2## Cn, SCN, OH, halogen, 5-(1H)-tetrazolylthio, ##STR3## or CO--O--NH--R.sub.1, wherein R.sub.1 is a hydrogen atom, an alkyl radical optionally substituted by cycloalkyl or an alkenyl, cycloalkyl, aralkyl or aryl radical, wherein the aromatic moiety can be substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen; and the pharmacologically acceptable salts thereof. The present invention also provides processes for preparing these compounds and pharmaceutical compositions containing them for combating allergic diseases.

Tetrazolyl substituted thioethers, pharmaceutical compositions and

The present invention provides compounds of the general formula: ##STR1## wherein Ar is a phenyl radical optionally substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, A is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 aliphatic hydrocarbon radical which is optionally substituted by a hydroxyl group, n is 0, 1 or 2, B is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 -aliphatic hydrocarbon radical and R is 5-(1H)-tetrazolyl, --CO--NH-tetrazolyl, ##STR2## CN, SCN, OH, halogen, 5-(1H)-tetrazolylthio, ##STR3## or CO--O--NH--R.sub.1, wherein R.sub.1 is a hydrogen atom, an alkyl radical optionally substituted by cycloalkyl or an alkenyl, cycloalkyl, aralkyl or aryl radical, wherein the aromatic moiety can be substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen; and the pharmacologically acceptable salts thereof. The present invention also provides processes for preparing these compounds and pharmaceutical compositions containing them for combating allergic diseases.

Hydroxamic acids and pharmaceutical compositions containing them, and

The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use

The present invention provides N.sup.6 -disubstituted purine derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.4 are the same or different and each represents a hydrogen or halogen atom or an --NR.sub.6 R.sub.7 group, R.sub.2 and R.sub.3 are the same or different and each represents a C.sub.1 -C.sub.6 alkyl radical, a C.sub.2 -C.sub.6 alkenyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, a phenalkyl radical containing up to 4 carbon atoms in the alkyl moiety, which can be straight-chained or branched, the phenyl moiety of which can be substituted one or more times by halogen, hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or trifluoromethyl; a furylmethyl or furylethyl radical, a thiophenemethyl or thiopheneethyl radical, a pyridylmethyl or pyridylethyl radical optionally substituted by a C.sub.1 -C.sub.4 alkyl radical, an indanyl radical or a tetrahydronaphthyl radical, R.sub.5 is a hydrogen atom, a tetrahydrofuranyl or tetrahydropyranyl radical or a C.sub.1 -C.sub.10 radical which is optionally substituted one or more times by hydroxyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 carboxyalkanoyloxy, C.sub.2 -C.sub.6 hydroxyalkoxy, C.sub.3 -c.sub.6 dihydroxyalkoxy, carboxyl, cyano or 1H-tetrazol-5-yl radical, R.sub.6 and R.sub.7 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical or together represent a C.sub.2 -C.sub.5 alkylene radical optionally interrupted by oxygen, sulphur or an NR.sub.8 group and R.sub.8 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical; as well as the pharmacologically acceptable salts thereof.

N.sup.6 -disubstituted purine derivatives, and pharmaceutical

Pyrrothine derivatives and pharmaceutical use thereof

The present invention is concerned with the use of adenosine derivatives for the treatment of allergic diseases, as well as for bronchosphatic and broncho-constrictive reactions brought about by inflammation. The above adenosine derivatives can be used alone or together with xanthine derivatives. The invention is further concerned with compositions containing compounds of adenosine derivatives and optionally compounds of xanthine derivatives together with appropriate pharmaceutical carriers.

Use of adenosine derivatives as anti-allergic compounds and

The present invention provides thioethers of the general formula: ##STR1## wherein Ar is a phenyl radical which is optionally substituted one, two or three times by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, Q is an oxygen or sulphur atom or an NH group, A is a straight-chained or branched C.sub.2 -C.sub.8 alkylene radical which is optionally substituted by a hydroxyl group or can be interrupted by an ethenylene or ethynylene group, n is 0, 1 or 2, and R is a hydrogen atom or a straight-chained or branched alkyl radical which is optionally substituted one or more times by the same or different radicals selected from alkoxycarbonyl, alkoxy, hydroxyl, carboxyl or optionally substituted carbamoyl or amino; as well as the pharmacologically acceptable salts thereof, with the proviso that A cannot be ethylene when Ar is a phenyl radical, Q is an oxygen atom and R is the group --CH.sub.2 COOH. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

Thioethers and pharmaceutical compositions containing them

The present invention provides a process for the detection of the presence of an allergy and for the specific detection of the allergen responsible for the allergy, based on the cellular principle, wherein leukocytes of a sample to be investigated are incubated with an allergen or another stimulation factor of degranulation, such as anti-IgE, in an aqueous medium, the leukocytes are then separated off and the remaining solution is incubated with a compound of the general formula:

Process for the detection of the presence of an allergy and for the

The present invention provides benzopyranyl ethers of the general formula: ##STR1## wherein A is an alkylene radical containing 2 to 4 carbon atoms and R is a hydrogen atom or an acyl radical; as well as the salts thereof with pharmacologically acceptable acids. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for treating allergic diseases.

Benzopyran compounds, pharmaceutical compositions containing them and

The present invention provides aryl ether derivatives of the general formula: ##STR1## wherein A is an oxygen atom or the group &gt;N--R.sub.1, R.sub.1 being a hydrogen atom or a lower alkyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.4 is a hydrogen atom or a hydroxyl group, R.sub.5 is a hydrogen atom or an acyl radical, R.sub.7 is a hydrogen atom, a lower alkyl radical or a lower alkanoyl radical and R.sub.8 is a hydrogen atom, a lower alkyl radical, a lower alkoxy radical or a hydroxyl group; and the pharmacologically acceptable salts thereof. The present invention also provides a process for the preparation of these compounds and pharmaceutical compositions containing them. It is also concerned with the use of these compounds for combating allergic diseases.

1,2-Dihydroquinolines connected via an oxyalkyl group with a piperidine

An aryl ether derivative of the formula ##STR1## in which A is an oxygen atom or an &gt;N--R.sub.1 grouping,

Growing community of inventors

Weinheim-Rittenweier, Germany

Otto-Henning Wilhelms