Aventis Pharma Deutschland, Gmbh

Sanofi-a Ventis Deutschland Gmbh

Sanofi-aventis

Klaus-ulrich Weithmann

Wilfried Schwab

Manfred Schudok

Werner Thorwart

Eckart Bartnik

Reinhard Kirsch

Volkmar Wehner

Gerhard Zoller

Burkhard Haase

Swen H&ouml;lder

Frank B&uuml;ttner

Joachim Wink

Otmar Klingler

Sven Ruf

Herbert Kogler

Andreas Lindenschmidt

Joerg Habermann

Christian Engel

Cordula Hopmann

Petra Stahl

Sven Grueneberg

Holger Wagner

Bernard Pirard

Jochen Beninga

Jörg Habermann

Martin Albert Knauf

The present invention relates to a novel compound of the formula I: and/or all stereoisomeric forms of the compound of the formula I and/or mixtures of these forms in any ratio, and/or a physiologically tolerated salt of the compound of the formula I, in which R1 to R5 and V1, V2 have the meanings stated in the claims and specification. The inventive compounds are suitable as inhibitors of metalloproteases, especially of ADAMTS proteases and TNF-&#x3b1; converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.

Cyclic ureas used as inhibitors of metalloproteases

Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.

Pyrimidine-4,6-dicarboxylic acid diamides for selectively inhibiting collagenases

Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides of formula I. These compounds are found to possess the property of selectively inhibiting collagenase (MMP). They may therefore be useful in prophylaxis and therapy of diseases whose course involves an increased activity of matrix metalloproteinase 13.

Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides and the use thereof for selectively inhibiting collagenases

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

The invention relates to a method for detecting inhibitors or ligands of binding domains, which comprises using a protein which contains at least one catalytic domain and at least one binding domain, incubating said protein with a marker substrate which binds to the catalytic domain of the protein and is converted, with a substrate which can reversibly bind to the catalytic domain and to the binding domain, and with the inhibitor and determining whether the marker substrate is converted by the protein.

Method for detecting protein inhibitors and ligands of medical value

Cyclic N-substituted alpha-imino carboxylic acids for selective inhibition of collogenase

Substituted thiadiazolesulfonamides

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

Stromelysin inhibitors

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

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

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Hofheim, Germany

Klaus-ulrich Weithmann