Merckle Gmbh

Heparegenix Gmbh

C-a-i-r Biosciences Gmbh

Eberhard-karls-universitat Tubingen

Baden-wurttemberg Stiftung Ggmbh

Stefan Laufer

Wolfgang Albrecht

Hans-Guenter Striegel

Karola Tollmann

Roland Selig

Gerd Dannhardt

Philipp Merckle

Hans Gunther Striegel

Thomas Kammermeier

Hans-Günter Striegel

Bent Praefke

Susanne Tries

Philip Klövekorn

Bent Präfke

Phillip Klövekorn

Lars Zender

Michael Schindler

Michael Juchum

Karola Neher

Hans-G&uuml;nter Striegel

Dunja Kotschenreuther

Hans-Gunter Striegel

Natalia Ruetalo Buschinger

Marcel Günther

Melanie Henning

Dirk Flötgen

Tatu Pantsar

Juliander J Reiner

Cornelia Greim

Karl Kenji Schorpp

Philip KLÖVEKORN

Linda Wiltzer-Bach

The invention relates to compounds of formula (I) which are inhibitors of MKK4 (mitogen-activated protein kinase kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The compounds selectively inhibit protein kinase MKK4 over protein kinases JNK1 and MKK7. In formula (I), especially, Ris —NRSOR; either a) Rand Rare F and Rand Rare H; or b) R, Rand Rare independently halogen and Ris H; Ris substituted phenyl or pyrimidinyl.

3-benzoyl-1H-pyrrolo[2,3-b]pyridine derivatives as MKK4 inhibitors for treating liver diseases

The invention relates to pyrazolo-pyridine compounds which inhibit mitogen-activated protein kinase kinase 4 (MKK4) and in particular, selectively inhibit MKK4 over protein kinases JNK1 and MKK7. The compounds are useful for promoting liver regeneration or reducing or preventing hepatocyte death. They are further useful for treating osteoarthritis or rheumatoid arthritis, or CNS-related diseases.

Protein kinase MKK4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death

The invention relates to compounds of formula (I) which are inhibitors of MKK4 (mitogen-activated protein kinase kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The compounds selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7. (I), wherein R, R, Rand Rare selected from: a) Rand Rare F and Rand Rare H; b) R, Rand Rare independently halogen and Ris H; c) RRand Rare independently halogen and Ris H; and d) RRand Rare independently halogen and Ris H.

Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death

Tricyclic mitogen-activated protein kinases kinase 4 (MKK4) inhibitor compounds useful for promoting liver regeneration or reducing hepatocyte death by selectively inhibiting MKK4 over protein kinases JNK and MKK7.

Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death

The invention relates to MKK4 (mitogen-activated protein kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The MKK4 inhibitors selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7.

The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1&#x3b2; and/or TNF-&#x3b1;. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.

Dibenzocycloheptatone derivatives and pharmaceutical agents containing said compounds

The present invention relates to the choline and tromethamine salt of Licofelone.

Choline and tromethamine salt of licofelone

The present invention relates to a new crystalline modification of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,S-dihydro-1H-pyrrolizin-S-ylacetic acid which is referred to as polymorph B. It has a peak in the solid stateC-NMR spectrum (with adamantane as external reference standard; CH group d=29.45 ppm) in the range from 179.8 to 180.2 ppm and can be processed directly to a pharmaceutical formulation.

Polymorphic form of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1h-pyrrolizin-5-ylacetic acid

The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R, R, Rand m are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.

2-thio-substituted imidazole derivatives and their use in pharmaceutics

The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R, R, R, Rand p are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.

The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R, R, Rand Rare as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.

2-thio-substituted imidazole derivatives and the use thereof in the pharmaceutical industry

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

The present invention relates to fused pyrrole compounds of the formula 1.in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl. These compounds are in particular pyrrolizines, indolizines and heteroanalogues having selective inhibitory action on isoenzyme-2 of prostaglandin H synthase (COX-2). The invention also relates to pharmaceutical compositions which contain these compounds; and the use of these compounds for the treatment of disorders of the rheumatic type.

Fused pyrrole compounds, pharmaceutical agents containing the same, and the use thereof

The present invention relates to compounds of the formula Iin which one of the radicals R8 and R9 is a hydrogen atom or an alkyl group and the other is hydroxyl, alkoxy or acyloxy or where R8 and R9, together with the carbon atom to which they are bonded, are a carbonyl group and the radicals R1 to R7 have the meanings indicated in the description. The compounds inhibit the release of various mediators of the arachidonic acid cascade and can thus be used for the prevention of allergically induced disorders or for the treatment of disorders of the rheumatic type.

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Blaubeuren, Germany

Stefan Laufer