Sanofi-A Ventis Deutschland Gmbh

Holger Wagner

Gerhard Jaehne

Karl Schoenafinger

Georg Tschank

Christian Buning

Ulrich Werner

Elisabeth Defossa

Lothar Schwink

Holger Gaul

Andreas Lindenschmidt

Klaus-ulrich Weithmann

Sven Grueneberg

Jochen Beninga

The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.

Substituted, bicyclic 8-pyrrolidinoxanthines, and methods for their use as inhibitors of dipeptidyl peptidase

Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are hereinafter defined. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds. Particular blood glucose disorders treatable thereby include type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerotic diseases and the like.

Substituted bicyclic 8-pyrrolidinoxanthines, methods for their production, pharmaceutical formulations and their use

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

The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional derivatives and process for their preparation. The compounds are suitable for the treatment of disorders of metabolism, such as type 2 diabetes.

Cyanopyrrolidides, process for their preparation and their use as medicaments

The invention relates to compounds of the formula Iin which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The compounds are suitable for the treatment of metabohlic disorders such as type 2 diabetes.

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Biberach/Mettenberg, Germany

Holger Wagner