Boehringer Mannheim Gmbh

Rainer Haag

Elmar Bosies

Dieter Herrmann

Christos Tsaklakidis

Walter-Gunar Friebe

Wolfgang Kampe

Joachim Dickhaut

Wolfgang Von Der Saal

Herbert Leinert

Uwe Bicker

Frank Grams

Wulf Pahlke

Michael Schultz

The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I. The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.

Azulene derivatives

The subject of the present invention is the use of imexon for the production of pharmaceutical compositions with an immunosuppressive action. The present invention also provides pharmaceutical compositions containing imexon and further active materials.

Use of imexon as an immune suppressive and pharmaceutical compositions

Compounds of the formula I ##STR1## wherein R is a hydrogen atom or an alkyl radical, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or a cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a cycloalkyl ring, X is a valency bond or an alkylene or vinylene radical, R.sub.3 is an aromatic heterocyclic five-membered ring containing 1 to 4 heteroatoms or pyridinyl which the five- and six-membered rings are optionaly substituted one or more times by alkyl, alkoxy, alkoxycarbonyl, carboxyl, alkylthio, hydroxyl, nitro, amino, halogen or cyano and the tautomers, optically-active forms and physiologically acceptable salts thereof with inorganic and organic acids. These compounds are useful for treatment of immunological disorders or autoimmune diseases such as aids/ARC, rheumatoid arthritis, lupus erythematosus and to suppress rejection reactions after organ/tissue transplants.

Pharmaceutically active pyridinyl substituted

The present invention provides compounds of the general formulae: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.5 -alkyl radicals, C.sub.3 -C.sub.5 -alkenyl radicals or phenyl radicals or, together with the carbon atom to which they are attached, form a saturated or unsaturated C.sub.3 -C.sub.7 ring, R.sub.3 and R.sub.4, which can be the same or different, are hydrogen atoms, straight-chained or branched C.sub.1 -C.sub.10 -alkyl radicals, straight-chained or branched C.sub.3 -C.sub.7 -alkenyl radicals, C.sub.3 -C.sub.7 -cycloalkyl radicals, C.sub.3 -C.sub.7 -cycloalkenyl radicals, phenyl, arylalkyl or hetarylalkyl radicals, R.sub.5 is a hydrogen atom or a lower alkyl radical and X is an oxygen or sulphur atom or an imino group. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions with immunosuppressive action containing them.

Imidazolidine derivatives as immunosuppressives

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Ladenburg, Germany

Rainer Haag