Klinge Pharma Gmbh

Astellas Pharma Gmbh

Astellas Deutschland Gmbh

Friedemann Reiter

Klaus Seibel

Benno Rattel

Klaus Vogt

Max Hasmann

Elfi Biedermann

Barbara Schein

Isabel Schemainda

Roland Löser

Michael Schliack

Katja Wosikowski

Roland L&ouml;ser

Helmut Grill

Roland Loser

Gerhard Lang

Hans-Helmut Henschel

Peter Jank

Kaisli Kaipainen-Reiter

Katia Wosikowski

Anke Schink

Rolf Eisenburger

Michael Schulz

The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases. 

Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents

The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression 

Pyridyl alkane acid amides as cytostatics and immunosuppressives

The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.

Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives

The invention relates to new pyridylalkane, alkene, and alkine carboxamides substituted with an imide with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to general formula (I), wherein the residue E is a cyclic imide, methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors, inhibition of abnormal cell growth and control of immune reactions, for example autoimmune diseases. 

Cyclic imide-substituted pyridylalkane, alkene, alkine carboxamides useful as cytostatic and immunosuppressive agents

The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to the general formula (I) as well as methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides

The invention relates to new piperidinyl-substituted pyridyl carboxamides of the general formula (I), wherein the structure element E has meanings (E1) or (E2) and whereby the heterocyclic ring can optionally have a double bond. These substances have especially high cytostatic activities and pronounced immunosuppressive properties which make them suitable for therapeutic treatment in broad tumor spectrum.

Piperadinyl-substituted pyridylalkane, alkene and alkine carboxamides

New biologically active compounds are described which inhibit the cellular formation of niacinamide mononucleotide, and essential intermediate of the NAD(P) biosynthesis in the cell. These compounds can represent the active ingredient of a pharmaceutical composition for the treatment of cancers, leukaemias or for immunosuppression. Furthermore, screening methods are described as a tool for detecting the above active compounds, and for examination of a given cell type for its dependency on niacinamide as a precursor for NAD synthesis.

Inhibitors of cellular niacinamide mononucleotide formation and their use in cancer therapy

The invention relates to the use of pharmacologically valuable pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides according to general formula (I) in the treatment of tumors or for immunosuppression.

Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression

The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.

The preparation of the pure enantiomers of LIFIBROL and its alkyl esters is achieved with surprisingly good yield by reacting the pure enantiomeric forms of S(-) R(+)-4-(4-tert.butylphenyl)-1,2-epoxy butane with 4-hydroxybenzoic acid alkyl ester at elevated temperature in DMF and in the presence of 4-hydroxybenzoic acid alkyl ester sodium salt. Thereafter, the raw reaction product is separated. Either the stereochemically pure LIFIBROL ester is then recovered by recrystallization or the precipitated LIFIBROL enantiomer is made in pure crystalline form by mild alkaline saponification and subsequent acidification.

Process for preparing the pure enantiomers of lifibrol and its alkyl

p-Oxybenzoic acid derivatives of the general formula (1) ##STR1## their physiologically compatible salts and their enantiomeric and diastereomeric forms have hypolipemic properties and are therefore suitable for the preparation of drugs with hypolipemic action.

p-Oxybenzoic acid derivatives, process for the preparation thereof and

The invention relates to p-oxibenzoic acid derivatives of the general formula (1) where: ##STR1## their diastereomers and enantiomers in pure form or as mixture of stereoisomeric forms and their physiologically compatible salts, a process for the preparation thereof and the use thereof for preparing drugs with hypolipemic effect.

New p-oxibenzoic acid derivatives, process for their preparation and

Para substituted benzoic acid derivatives of general formula (1) ##STR1## and their physiologically compatible salts, where R.sup.1 may be H, isopropyl, t-butyl p0 X may be ##STR2## and R.sup.2 may be --OH, --OR', where R' is a linear or branched, saturated or unsaturated C.sub.1 to C.sub.3 alkylmoiety, or a --NHCH.sub.2 COOH-- group, have hypolipedemic activity. They may be obtained by known methods either from the corresponding unsaturated ketones or from saturated hydroxycompounds, where the esterified benzoic acid moiety may be saponified or converted to a carboxymethylamide.

New benzoic acid derivatives, as well as processes for their production

P-oxybenzoic acid derivatives of formula (1) ##STR1## wherein R.sup.1 is hydrogen, or straight or branched alkyl of one to four carbon atoms;

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Putzbrunn, Germany

Friedemann Reiter