Boehringer Mannheim Gmbh

C.f. Boehringer & Soehne Gmbh

Max Thiel

Wolfgang Kampe

Egon Roesch

Karl Dietmann

Wolfgang Schaumann

Kurt Stach

Walter-Gunar Friebe

Gisbert Sponer

Kurt Stach, Deceased

Wolfgang Bartsch

Androniki Roesch

Otto-Henning Wilhelms

Werner Winter

Herbert Berger

Ernst-Christian Witte

Rudi Gall

Wolfgang Vomel

Fritz Wiedemann

Uwe Bicker

Erich Fauland

By Werner Plattner, Administrator

Elmar Bosies

Hans P Wolff

Franz Braun

Dietmar Boerner

Karlheinz Stegmeier

Ruth Heerdt

Felix Helmut Schmidt

Winfriede Sauer

Manfred Hubner

Harald Stork

By Werner Plattner, Executor

Gottfried Hebold

Wolfgang Juhran

Martin Senn

Erika Von Mullendorff

The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

N-Substituted aziridine-2-carboxylic acid derivatives

Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;

Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions

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

The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives

A 2-cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methane ##STR1## wherein R is a nitrile or carbamoyl group, and

2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes

An N-phenoxyalkylpiperidine derivative of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, an acyl radical or an optionally substituted aryl radical, R.sub.2 is a hydroxymethyl radical, a cyano group, an amidino group, an amidino group substituted by hydroxyl, a 1H tetrazol-5-yl radical or a --CO--R.sub.3 radical, R.sub.3 is a hydroxyl group, a lower alkoxy radical, an amino group, or an amino group substituted by a 1H-tetrazol-5-yl radical, X is an imino group or an oxymethyl radical, A is an alkylene radical containing 2 to 4 carbon atoms, and B is a valency bond or a 4-hydroxypyrimidin-2,5-diyl radical; or a pharmacologically acceptable salt thereof. The compounds exhibit anti-histaminic, anti-oedematous and anti-phlogistic activity.

N-Phenoxyalkylpiperidine derivatives

Coumarins connected via an oxyalkyl group with a piperidine ring having

The present invention provides xanthine derivatives of the general formula: ##STR1## wherein one of the symbols R.sub.1 and R.sub.2 stands for a methyl radical and the other for a radical of the general formula: ##STR2## wherein R.sub.3 is a hydrogen atom or an acyl radical; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them and is also concerned with the use thereof for the preparation of pharmaceutical compositions for the treatment of allergies.

Derivatives of xanthine

Phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl

Phenoxyalkylcarboxylic acid compounds and thrombocyte-aggregation

4-Phenoxymethyl-piperidines of the formula ##STR1## wherein R is hydrogen, halogen, nitro, lower alkyl or lower alkoxy, in the form of the free base or an acid addition salt, are provided and they are useful as intermediates in the production of anti-hypertensive agents through condensation with (a) propyl chloride and then with an adenine, or (b) a propyl indole.

4-Phenoxymethyl-piperidines

New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,

Aminopropanol substituted indole compounds and compositions for the

Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, or

Adenosine-5'-carboxylic acid amides

Novel 9-[3-(4-amino-piperidino)-propyl]-adenine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,

Pharmaceutically active derivatives of

New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;

3-Nitropyrazole compounds and anti-microbial compositions

Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms;

Growing community of inventors

Mannheim, Germany

Max Thiel