Sanofi-a Ventis Deutschland Gmbh

Aventis Pharmaceuticals Inc.

Uwe Schwahn

Stefan Peukert

Armin Hofmeister

Herman Schreuder

Stefan Guessregen

Philip M Weintraub

Shujaath Mehdi

Paul Robert Eastwood

Kwon Yon Musick

John Ziqi Jiang

Sungtaek Lim

Neil Moorcroft

David Stefany

Paul R Eastwood

David W Stefany

The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R, R, Rand Rare as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5'-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Substituted pyridones as inhibitors of poly(ADP-ribose) polymerase (PARP)

This invention relates to compounds of formula (I), wherein R1 and R3 independently represent fluorine, methoxy, &#x2014;OCF, C-C-alkenyl or C-C-alkyl which is optionally substituted by chlorine, methoxy or one, two or three fluorine atoms; R2 represents hydrogen, fluorine, methoxy, &#x2014;OCF, C-C-alkenyl or C-C-alkyl which is optionally substituted by chlorine, methoxy or one, two or three fluorine atoms; X represents O, S, NH or N(C-C-alkyl); and Ar represents an unsubstituted or at least monosubstituted aryl or heteroaryl. Said compounds are inhibitors of poly(ADP-ribose) polymerase (PARP), and may be used for the treatment of a variety of disorders.

Substituted 2-pyridone derivatives, method for their preparation and their use as medicament

This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments. These compounds are poly(ADP-ribose) polymerase (PARP) inhibitors.

Substituted tetrahydro-2H-isoquinolin-1-one derivatives, and methods for the production and use thereof

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Sulzbach, Germany

Uwe Schwahn