Abstract: 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-? converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.

Abstract: The invention concerns the use of thiopeptolides of formula R-(Xaa)n-Pro-X-Gly-S—Y-Z-Gly-(Xaa)m-R1 (I) as substrate for determining the activity of ADAMTS proteases, and a method for finding an ADAMTS protease modulator, more particularly an inhibitor.

Abstract: 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-? converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.

Abstract: 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.

Abstract: 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.

Abstract: The invention relates to a pyrimidine-4,6-dicarboxylic acid diamide compound, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use. Particularly, the pyrimidine-4,6-dicarboxylic acid diamide compound is useful for selectively inhibiting collagenase matrix metalloproteinase (MMP) 13, or for treating a degenerative joint disease.

Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.

Abstract: Pyrimidine-4,6-dicarboxylic acid diamides of the formula I 1

Abstract: 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.

Abstract: The invention is related to compounds of formula I to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds, and to methods of prevention and treatment of disorders, the progression of which involve an enhanced activity of matrix metalloproteinase 13, by administering to a patient in need thereof, a pharmaceutically effective amount of such compounds.

Abstract: 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.

Abstract: The invention is related to compounds of formula I 1

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

Abstract: Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.

Abstract: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.

Abstract: Compounds of the formula I 1

Abstract: 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.

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of conditions whose course involves an increased activity of matrix-degrading enzymes, in particular stromelysin.

Abstract: Compounds of the formula (I): 1