Deutsche Gold- Und Silber-scheideanstalt Vormals Roessler

Dolorgiet Beteiligungs Gmbh

Degussa Akteinsellschaft

Dolorgiet Gmbh & Co. Kg

Klaus Posselt

Manfred Lohner

Heribert Offermanns

Klaus Thiemer

Otto Isaac

Hans H Wagener

Horst Uthemann

Axel Kleemann

Jurgen Engel

Walter Von Bebenburg

Fritz Stroman

Ute Vogtle-Junkert

Kurt Thiele

Klaus Gruber

The agents for the treatment of conditions of severe pain, and especially of tumor pain and post-operative pain, consist of soft gelatin capsules containing from about 30 to about 50 parts by weight of ibuprofen and from about 1.5 to about 4 parts by weight of codeine and/or physiologically compatible salts thereof, partially dissolved and partially suspended in about 68.5 to about 46 parts by weight of polyoxyethylene-polyoxypropylene-diol or in a mixture comprising about 30 to about 76 parts by weight of polyoxyethylene-polyoxypropylene- diol or polyethylene-glycol or polypropyleneglycol and from about 7 to about 40 parts by weight of a physiologically compatible surfactant.

Agents for the treatment of severe pain and preparation of said agents

Soft gelatin capsules containing a solution of from 15 to 30 parts by weight of ibuprofen in from 70 to 85 parts by weight of polyoxyethylene-polyoxypropylene polymer or in a mixture of from 30 to 76 parts by weight of polyalkylene glycol and from 7 to 40 parts by weight of a surfactant have a very rapid and high bio-availability of the active ingredient. The active ingredient is not re-precipitated therefrom by aqueous media such as artificial gastric juice.

Ibuprofen-containing soft gelatin capsules and process for preparing same

An externally administrable pharmaceutical which contains an effective amount of 2-(4-isobutylphenyl)propionic acid in a base is obtained by drug dissolution in a mixture of C.sub.6-12 carboxylic acid triglycerides, glycerol monostearate-polyoxyethylene stearate mixture and polyoxyethylene-fatty acid esters. A cream is obtained by stirring this solution with an aqueous phase in the presence of heat.

Transdermal 2-(4-isobutylphenyl)-propionic acid medication and methods

There are prepared compounds of the formula: ##STR1## wherein X is the group &gt;C.dbd.O or &gt;CH(OH), Y is the group ##STR2## R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, R.sub.3 is hydrogen or a hydroxy group and R.sub.1 is the adamantyl group or a saturated or single unsaturated C.sub.3 to C.sub.16 cycloalkyl group where the C.sub.3 to C.sub.16 cycloalkyl group can be substituted by a C.sub.1 -C.sub.4 alkyl group or a halogen atom and their salts. The compounds are useful in dilating the peripheral blood vessels and in lowering blood pressure.

Cycloaliphatic ketoamines

There are prepared compounds corresponding to the general formula: ##STR1## in which R represents a 2,2-dimethylethenyl; isopropyl; nonyl; a C.sub.3 -C.sub.6 -cycloalkyl radical; a phenyl group substituted by at least one nitro group, or a C.sub.1 -C.sub.6 -alkyl group containing a morpholine group attached thereto, said morpholine ring being substituted zero to twice by C.sub.1 -C.sub.6 -alkyl groups; R.sub.3 is --CHO or --CH.sub.2 OH, their optically active forms and their salts. The compounds have cardioactivity e.g., bradycardic effect and have local anethetic, spasmolytic and antiarythmic activity.

Acyl derivatives of hellebrigenin

Compounds are prepared of the formula: ##STR1## wherein A is a straight or branched chain alkylene or alkylidene radical having 2 to 5 carbon atoms and which is substituted by an alkylthio group having 1 to 4 carbon atoms, a carboxymethyl thio group, a carboxyethyl thio group, an alkylsulfonyl group having 1 to 4 carbon atoms, a mercapto group, or the substituent on A together with --COR.sub.4 forms a 4 to 7 membered thiolactone ring, or A is substituted by an acylmercapto group wherein the acyl is benzoyl, a benzoyl radical substituted with one, two or three alkoxy groups with 1 to 6 carbon atoms, an alkanoyl radical of 1 to 6 carbon atoms, an alkenoyl radical of 3 to 6 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 are the same or different and are alkyl groups of 1 to 5 carbon atoms and one of R.sub.1, R.sub.2 and R.sub.3 also can be hydrogen or the acyl radical of an alkanoic acid of 2 to 4 carbon atoms and R.sub.4 is a hydroxy group or an alkoxy group with 1 to 5 carbon atoms and their pharmacologically acceptable salts. The compounds are pharmacodynamically active and are suited for prophylaxis and treatment of heart illnesses such as cardiac ischemia, cardiac infarct, heart rhythm and circulatory disturbances.

Sulfur containing trialkoxybenzoylamino carboxylic acids

Compounds are prepared of the formula ##STR1## The compounds of the invention possess valuable pharmacodynamic properties. They especially have a positive inotropic effect which is particularly noted in oral or enteral application. In contrast to the known compounds the compounds of the invention have more favorable pharmacological or pharmaceutical properties.

Derivative of desglucohellebrin and therapeutic use

Compounds of the formula ##STR1## wherein Ar is phenyl or naphthyl, X is oxygen or the group ##STR2## Y is substituted or unsubstituted alkylene of 1-4 carbon atoms, R.sub.1 is acyloxy, acyloxyalkoxy, acylamino or is --N(Alkyl)(Acyl, R.sub.4 is hydrogen or lower alkyl, R.sub.5 is hydrogen, lower alkyl or acyl, and R.sub.2, R.sub.3, R.sub.6 and R.sub.7 are the same or different and are hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, amino, alkylamino, dialkylamino, acylamino, nitro, lower alkyl, lower halogeno alkyl, or lower alkylthio,

Acyl derivatives of substituted bis-arylalkylamino compounds

Compounds are prepared of the formula: ##SPC1## Wherein A is a straight or branched chain alkylene or alkylidene radical having 2 to 5 carbon atoms and which is substituted by an alkylthio group having 1 to 4 carbon atoms, a carboxymethyl thio group, a carboxyethyl thio group, an alkylsulfonyl group having 1 to 4 carbon atoms, a mercapto group, or the substituent on A together with --COR.sub.4 forms a 4 to 7 membered thiolactone ring, or A is substituted by an acylmercapto group wherein the acyl is benzoyl, a benzoyl radical substituted with one, two or three alkoxy groups with 1 to 6 carbon atoms, an alkanoyl radical of 1 to 6 carbon atoms, an alkenoyl radical of 3 to 6 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 are the same or different and are alkyl groups of 1 to 5 carbon atoms and one of R.sub.1, R.sub.2 and R.sub.3 also can be hydrogen or the acyl radical of an alkanoic acid of 2 to 4 carbon atoms and R.sub.4 is a hydroxy group or an alkoxy group with 1 to 5 carbon atoms and their pharmacologically acceptable salts. The compounds are pharmacodynamically active and are suited for prophylaxis and treatment of heart illnesses such as cardiac ischemia, cardiac infarct, heart rhythm and circulatory disturbances.

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Bonn, Germany

Klaus Posselt