Bayer Aktiengesellschaft

Axxam S.r.l.

Stefan Lohmer

Stefan Wohlfeil

Dirk Denzer

Hilmar Bischoff

Ulrich E Muller

Richard D Connell

Rudi Grutzmann

Siegfried Goldmann

Martin Beuck

Christoph Gerdes

James J Elting

Siegfried Zaiss

Ozkan Yalkinoglu

Ulrich M&uuml;ller

Anke Domdey-Bette

Peter Kolkhof

Matthias Muller-Gliemann

Peter Eckenberg

Ulrich Nielsch

Rudi Gr&uuml;tzmann

Matthias M uller-Gliemann

Ulrich E M Uller

Maria Foti

Rudi Gr Utzmann

Rudi Gru Tzmann

Disclosed is a photoprotein with improved luminescent activity, the use thereof as calcium indicator and in cell-based assays for the detection and measurement of intracellular calcium.

Photoprotein with improved bioluminescence

The indolyl-substituted phenylacetic acid derivatives are prepared by reacting the corresponding phenylacetic acids with the required amines. The indolyl-substituted phenylacetic acid derivatives are suitable as active compounds in medicaments, in particular in antiarteriosclerotic medicaments.

Indolyl-substituted phenylacetic acid derivatives

The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.

Bicyclic heterocyclic compounds

The pyrimido[1,2-a]indoles according to the invention are prepared by reacting appropriately substituted phenylacetic acid derivatives with phenylglycinols. The pyrimido[1,2-a]indoles can be used as active compounds in medicaments, in particular in medicaments with antiatherosclerotic activity.

Pyrimido[1,2-a]indoles

The phenylcyclohexylcarboxamides, some of which are known, are suitable as active compounds in medicaments, in particular in medicaments for the treatment of restenosis.

Use of phenylcyclohexylcarboxamides

Amides and sulphonamides of benzylamines having heterocyclic substituents are prepared by first converting the corresponding carboxylic acids into the corresponding amines and then substituting these on the amine nitrogen in a corresponding manner. The new amides and sulphonamides of benzylamines having heterocyclic substituents can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

Amides and sulphonamides of benzylamines having heterocyclic substituents

Substituted xanthines of formula ##STR1## in which A represents a radical of the formula ##STR2## in which R.sup.3, R.sup.4, R.sup.6 and R.sup.7 denote hydrogen, cycloalkyl, aryl having 6 to 10 carbon atoms, or denote straight-chain of branched alkyl or alkenyl, each of which is optionally substituted; T, V, X and Y are identical or different and denote an oxygen or sulphur atom; R.sup.5 and R.sup.8 are identical or different and denote hydrogen, halogen, cycloalkyl having 3 to 8 carbon atoms or straight-chain or branched alkyl or alkenyl in each case having up to 8 carbon atoms, optionally substituted or R.sup.5 and R.sup.8 denote aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused heterocycle having up to 3 heteroatoms S, N and/or O, each of which is optionally substituted; L represents an oxygen or sulphur atom; R.sup.2 represents mercapto, hydroxyl, straight-chain or branched alkoxy having up to 8 carbon atoms or the group of the formula ##STR3## in which R.sup.13 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms; R.sup.14 denotes hydrogen, phenyl or a 5- to 6-membered aromatic heterocycle having up to 3 heteroatoms S, N and/or O; and R.sup.15 denotes hydrogen or straight-chain or branched alkyl having up to 8 carbon atom, optionally substituted by hydroxyl, and their salts are prepared by reaction of the suitable unsubstituted xanthines with halogenomethylphenylacetic acids and subsequent reaction of the carboxylic esters or acids with phenylglycinolamine. The substituted xanthines are suitable as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

Xanthines in the 7th position with a benzyl acetic acid moiety

Substituted indole derivatives are prepared by reacting appropriate carboxylic acids, if appropriate in the presence of auxiliaries, with appropriate amines. The substituted indole derivatives are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis and restenosis.

Substituted indole derivatives

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Milan, Italy

Stefan Lohmer