Schering Aktiengesellschaft

Sinoxa Pharma Gmbh

Neurobiotec Gmbh

Reinhard Horowski

Helmut Wachtel

Wolfgang Kehr

Dieter Palenschat

Gert Paschelke

Ralph Schmiechen

Rainer Dorow

Rudolf Wiechert

Gerhard Sauer

Ulrich Kerb

Johannes Wilhelm Tack

Peter-Andreas Loschmann

Dieter Seidelmann

Herbert H Schneider

Ulrich Eder

Karl Petzoldt

Dieter Rahtz

Eberhard Schroder

Klaus Kieslich

Paul-Eberhard Schulze

Otto Engelfried

Bernard Acksteiner

Gertrud Schroeder

Hans Peter Lorenz

Rudolf Reiter

Gunter Stock

Walther Birkmayer

Jorg Birkmayer

Bernd Aufdembrinke

Irmgard Suchy

Johannes Tack

Heinz Palla

The present invention relates to the use of ergot derivatives or ergolines, and in particular of lisuride and terguride for the prophylaxis and treatment of constrictive capillary arteriopathy. Constrictive capillary arteriopathy refers to the diseases pulmonary arterial hypertension, endogenously induced or exogenously induced glomerulosclerosis as well as secondary Raynaud's syndrome.

Pharmaceutical compositions for the treatment of capillary arteriopathy

The invention relates to the use of a dopamine agonist in the form of an agent consisting of at least two spatially discrete compositions, of which one is a transdermal therapeutic system (TTS) containing the dopaminergic agent and another one or more are preparations for oral and/or parenteral application containing that same dopaminergic agent for the treatment of dopaminergically treatable diseases with the following elements: a) the TTS is continuously applied, b) within the duration of application in a) the composition for oral or parenteral dosage is administered.

Combination of a transdermal therapeutic system and an oral and/or parenteral preparation containing dopamine agonists for the treatment of dopaminergic disease states

The enzyme cofactor nicotinamide adenine dinucleotide or a salt thereof is useful for the treatment of Parkinson's disease.

Agent for treatment of Parkinson's disease

Compounds of general Formula I labeled with .sup.121 I, .sup.122 I, .sup.123 I, .sup.124 I, .sup.125 I, .sup.131 I and .sup.132 I isotopes ##STR1## wherein R.sup.6 is a C.sub.1-6 aliphatic hydrocarbon residue and

I*-diagnostics for monoamine receptors using ergolines

Terguride and its physiologically compatible salts can be used for the treatment of geriatric deficiencies, e.g., in doses of 0.1-5.0 mg/day.

Use of terguride as a geriatric agent

The treatment of psychosis with N-(D-6-methyl-8-isoergolin)-N'N-diethylurea.

Trans-dihydrolisuride antipsychotic

Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl of 2-6 carbon atoms, ##STR2## n is 1, or 2, m is 0 or 1,

(Erolinyl)-N,N-diethylurea derivatives, and their preparation and use

4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms at least one being other than methyl, a heterocyclic ring, or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl or an amino group; R' is H, alkyl, aryl or acyl; and X is O or S; possess neuropsychotropic activity. The compounds wherein X is O can be produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-amino-butyric acid or alkyl ester thereof. The pyrrolidones can be converted to the corresponding thiopyrrolidones by reaction with phosphorous pentasulfide in the presence of base.

4-(Polyalkoxy phenyl)-2-pyrrolidones

Diacylapomorphines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are both acyl of 1-17 carbons are symptomatically effective agents in the treatment of motor disorders of the type associated with a dopamine deficiency of the extrapyramidal system of the central nervous system, e.g. Parkinson's disease. Pharmaceutical compositions containing these compounds as an active ingredient are described, as well as new compunds of the above formula wherein R.sub.1 and R.sub.2 are formyl or acyl of 3-17 carbon atoms.

Diacylapomorphines

D-homo-20-ketopregnanes of the formula ##STR1## wherein R.sub.1 is oxygen, ##STR2## in which R.sub.5 is hydrogen or lower acyl; R.sub.2 is hydrogen or methyl; R.sub.3 is oxygen, ##STR3## or two hydrogen atoms; R.sub.4 is hydrogen, hydroxy or acyloxy; R.sub.6 is hydrogen or methyl; and R.sub.7 is hydrogen, acetyl, hydroxy or lower acyloxy in the .alpha.- or .beta.-position possess CNS-depressant activity, including anesthesia upon parenteral administration, and are produced by hydrogenating the corresponding steroids having double bonded C.sub.5 and/or C.sub.16 carbon atoms.

D-Homo-20-ketopregnanes

18-Methyl-19-nor-20-keto steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 collectively are an oxygen atom, or each is hydrogen, or one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy, and R.sub.3 is a ketonic oxygen atom or two hydrogen atoms, possess CNS-depressant activity, especially anesthetic-narcotic activity.

18-Methyl-19-nor-20-ketopregnanes and process for the preparation thereof

Benzomorphans of the formula ##STR1## wherein R.sub.1 is H, CH.sub.3 or C.sub.2 H.sub.5 ; R.sub.2 is CH.sub.3 or C.sub.2 H.sub.5 and R.sub.3 and R.sub.4, which can be alike or different, each are lower alkyl, and the acid addition salts thereof with physiologically acceptable acids have CNS activity, including analgesic, morphine antagonistic, anti-convulsive, muscle relaxant, sedative and neuroleptic activity.

Benzomorphan derivatives

4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl, carboxamido or amino or collectively are alkylene of 1-3 carbon atoms, R.sub.3 is H or OCH.sub.3, R.sub.4 is H, alkyl, aryl or acyl and X is O or S possess neuropsychotropic activity. The compounds wherein X is O are produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-aminobutyric acid or alkyl ester thereof. The pyrrolidones are converted to corresponding thiopyrrolidones in a conventional manner, e.g., by reaction with phosphorous pentasulfide in the presence of base.

Growing community of inventors

Berlin, Germany

Reinhard Horowski