Hoechst Aktiengesellschaft

Aventis Pharma Deutschland, Gmbh

Sanofi-a Ventis Deutschland Gmbh

Glycorex Ab

Eckart Bartnik

Gerhard Kretzschmar

Wilfried Schwab

Manfred Schudok

Dirk Seiffge

Klaus-ulrich Weithmann

Alexander Toepfer

Gerhard Zoller

Werner Thorwart

Wolfgang Schmidt

Joerg Czech

Burkhard Haase

Ekkehard Leberer

Andreas R Klatt

Thomas Leeuw

Sebastian Barradeau

Frank B&uuml;ttner

Bruce Caterson

Bernd Eidenmueller

Clare Hughes

Frank Buettner

Michael Ahlers

Horst Kunz

Ulrich Sprengard

Brigitte Hoersch

Brigitte Horsch

Christoph Huls

Dick Seiffge

Thomas Sanofi-Aventis Deutschland Gmbh Aigner

Uwe Sanofi-Aventis Deutschland Gmbh Dietz

Annette Brimmer

The invention refers to the use of a p21-activated kinase (PAK) inhibitor as a target protein for the discovery of a PAK inhibitor as a medicament for the treatment of a joint disease.

Use of PAK inhibitor for the treatment of a joint disease

The invention refers to the use of a p21-activated kinase (PAK) inhibitor for the treatment of a joint disease such as osteoarthritis or rheumatoid arthritis or for the treatment of a joint pain and the use of PAK as a target protein for the discovery of a PAK inhibitor as a medicament for the treatment of a joint disease.

Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids

Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use

A process for preparing polyvalent, physiologically degradable carbohydrate-containing polymers by enzymatic glycosylation reactions is described. The carbohydrate-containing polymers thus prepared may be used for preparing carbohydrate building blocks. The polyvalent carbohydrate-containing polymers of the invention cause no intolerance reactions in vivo, either in their intact form or in the form of degradation products. The carbohydrate side chain of the carbohydrate-containing polymer is assembled by enzymatic glycosylation reactions in homogeneous aqueous buffer systems directly on a biodegradable polymer. The yields of the glycosylation reaction are significantly improved over known processes, and are often quantitative. This also provides a significant increase in the loading densities. A process for preparing free oligosaccharides by means of the carbohydrate-containing polymers of the invention is also described.

Process for preparing polyvalent and physiologically degradable carbohydrate-containing polymers by enzymatic glycosylation reactions and the use thereof for preparing carbohydrate building blocks

Sulfonylaminophosphinic and sulfonylaminophosphinic acid derivatives, methods for their preparation and use

Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and carboxyclic acids

The invention relates to novel recombinant substrates for aggrecanase. In one embodiment, this substrate comprises the signal sequence of CD5, the FLAG-epitope for M1 monoclonal antibody detection, the interglobular domain of human aggrecan, the hinge region of human IgG1, the CH2 region of human IgG1 and the CH3 region of human IgG1. DNA sequences encoding the recombinant substrate are also provided, as are vectors and host cells containing said DNA. Various methods are provided for: monitoring aggrecanase activity, detecting new enzymatic cleavage sites, purifying aggrecanase chromatographically, and cloning the aggrecanase cDNA, screening for aggrecanase inhibitors; and for monitoring the onset or progression of osteoarthritis. A diagnostic aid containing the recombinant substrate is also provided.

Artificial recombinant substrate (rAGG 1) and native aggrecan to determine the proteolytic activity of 'aggrecanase' in cell culture systems

The invention relates to carbohydrate mimetics, which inhibit the binding of selectin to carbohydrate ligands, of the formula I ##STR1## excluding the compounds sialyl-Lewis-X and -A and their derivatives which, instead of an N-acetyl group, carry the substituents N.sub.3, NH.sub.2 or OH or which, instead of fucose, carry glycerol, and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.

Carbohydrate mimetics having antiadhesive properties

Artificial recombinant substrate (rAGG 1) and native aggrecan to

The invention relates to novel conjugates of tetrasaccharides, preferably of sialyl-Lewis X (SLeX) and sialyl-Lewis A (SLeA), having improved activity as inhibitors of cell adhesion, a process for the preparation of these compounds, and their use as pharmacological active compounds and as diagnostics and pharmaceuticals which contain these conjugates.

Carbohydrate conjugates as inhibitors of cell adhesion

Polymer-conjugated malonic acid derivatives and their use as medicaments

The invention relates to multiply fucosylated dicarboxylic acid derivatives possessing antiadhesive properties, to a process for preparing them, to their use, and to pharmaceuticals and diagnostic agents which are prepared from these derivatives. These multiply fucosylated dicarboxylic acid derivatives are suitable for preparing pharmaceuticals or diagnostic agents for diseases which are associated with an excessive, selectin receptor-mediated cell adhesion in the tissue which is affected by the disease.

Multiply fucosylated dicarboxylic acids possessing antiadhesive

The invention relates to malonic acid derivatives, which inhibit the binding of selectin to carbohydrate ligands, and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.

Malonic acid derivatives having antiadhesive properties

Growing community of inventors

Wiesbaden, Germany

Eckart Bartnik