Johannes Gutenberg-Universität Mainz

Merckle Gmbh

UniversitÄtsmedizin Der Johannes Gutenberg-Universitat Mainz

Other

Beiersdorf Ag

Johannes Gutenberg-universitatis

Gerd Dannhardt

Stefan Laufer

Stanislav Plutizki

Hans Gunther Striegel

Jan-Peter Kramb

Markus Möhler

Christopher Ganser

Eva Lauermann

Philipp Merckle

Thomas Kammermeier

Matthias Lehr

Hans-Günter Striegel

Annett Maderer

Ludwig Steindl

Linda Hahn

Andreas Luxenburger

Philip Prech

Holger Ulbrich

Christian Peifer

Florian Heidel

Thomas Fischer

Annett Müller

René Mönnikes

Markus Moehler

Annett Mueller

Rene Monnikes

Markus Mohler

René MÖNNIKES

The present invention relates to 3-(5-fluoroindolyl)-4-arylmaleimide compounds and pharmaceutical compositions containing them. The compounds of the present invention are protein kinases (GSK-3beta, VEGFR-2 and FLT-3) with antineoplastic activity. They can therefore be used for the treatment or prevention of tumors, in particular solid tumors. 

3-(5-fluoroindolyl)-4-arylmaleimide compounds and their use in tumor treatment

The present invention relates to the use of a compound of formula (I) wherein Rand Rare as defined in the description and Ris a phenyl group which is substituted with 2 or 3 C-Calkoxy groups, or a physiologically acceptable salt thereof, or a solvate of the compound of formula (I) or of the salt thereof, for treatment of colorectal or gastric adenocarcinoma. 

3-(indolyl)- or 3-(azaindolyl)- 4-arylmaleimide derivatives for use in the treatment of colon and gastric adenocarcinoma

The present invention relates to a compound of formula (I) wherein R, Rand Rare as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors. 

3-(indolyl)- or 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment

The present invention relates to 3-(Indolyl)- and 3-(azaindolyl)-4-phenylmaleimide compounds of formula (I) wherein R, Rand Rare as defined in the description, and the physiologically acceptable salts, solvates and solvates of the salts of the compounds of formula (I). The compounds of formula (I) are suitable for treating tumors. 

Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment

The present invention relates to the use of a compound of formula (I) wherein Ris H, C-C-alkyl, phenyl-C-C-alkyl or phenyl, Ris a phenyl group which is substituted with 2 or 3 C-C-alkoxy groups and Ris indolyl or azaindolyl which may carry one or two substituents independently selected from C-C-alkyl, C-C-alkoxy, phenyl, OH, halogen, NH, C-C-alkylamino, di-C-C-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S, or heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S, a physiologically acceptable salt thereof, or a solvate of the compound of formula (I) or of the salt thereof, for the prevention or treatment of leukemia. 

Use of 3-(indolyl)- or 3-(azaindolyl)-4-arylmaleimide derivatives in leukemia management

The present invention relates to a compound of formula (I) wherein Ris H, C-C-alkyl, phenyl-C-C-alkyl or phenyl, Ris a phenyl group which is substituted with 2 or 3 C-C-alkoxy groups and Ris indolyl or azaindolyl which may carry one or two substituents independently selected from C-C-alkyl, C-C-alkoxy, phenyl, OH, halogen, NH, C-C-alkylamino, di-C-C-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula 1 and of the salts thereof. The compounds of formula (I) are suitable for controlling angiogenesis. 

3-(indolyl)-4-arylmaleimide derivatives and their use as angiogenesis inhibitors

A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1 is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.

Non-glycosidic and non-peptidic inhibitors of selectin, and the use thereof

The invention relates to the 2-mercapto-4,5-diarylimidazole derivatives of formula (I), wherein R, R, Rand Rare defined as in the description. The inventive compounds have an immunomodulatory and cyclooxygenase-inhibiting activity and are therefore suitable for the treatment of diseases that are associated with a disturbed immune system.

2-mercapto-4,5-diarylimidazole derivatives and the use thereof as cyclooxygenase inhibitors

The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with &#x3c9;-bromo-4-chloroacetophenone with formation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine and the acetic acid group is introduced into the 5-position, 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole being obtained by hydrogenation of 2,2-dimethyl-4-oxo-5-phenylvaleronitrile or a ketal thereof. The invention also relates to processes for the preparation of intermediates occurring in the above process.

Method for the production of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1h-pyrrolizin-5-ylacetic acid

�A!-anellated pyrrole derivatives and their use in pharmacology

�a!-Annelated pyrrole derivatives and pharmaceutical use thereof

�A!-annellated pyrrole derivatives and their use in pharmacology

The invention concerns substituted pyrrole compounds and their pharmaceutical applications. The compounds of the invention are potent inhibitors of lipoxygenase and cyclo-oxygenase and therefore are suitable to treat the set of rheumatic illnesses and to prevent allergically induced ailments. The compounds have the general formula: ##STR1## where R.sup.1 denotes a C.sub.1 -C.sub.12 alkyl group, R.sup.2 denotes a hydrogen atom or a C.sub.1 -C.sub.12 alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom and the nitrogen atom to which they are bound form a ring of 5 to 8 links which may contain a sulfur heteroatom or a carbonyl group and may be substituted with one or two C.sub.1 -C.sub.4 alkyl groups,

Substituted pyrrole compounds and use thereof in pharmaceutical

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Mainz, Germany

Gerd Dannhardt