3,6-SUBSTITUTED 5-ARYLAMINO-1H-PYRIDINE-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS POLY(ADP-RIBOSE)POLYMERASE (PARP) INHIBITORS IN THE TREATMENT OF TISSUE DAMAGE OR DISEASE CAUSED BY NECROSIS OR APOPTOSIS

摘要

The invention relates to compounds of formula (I), wherein R1 and R3 independently represent fluorine, methoxy, -OCF3, C2-C3-alkenyl or C1-C4-Alkyl which is optionally substituted with chlorine, methoxy or one, two or three fluorine atoms; R2 represents hydrogen, fluorine, methoxy, -OCF3, C2-C3-alkenyl or C1-C4-alkyl which is optionally substituted with chlorine, methoxy or one, two or three fluorine atoms; X represents O, S, NH or N(C1-C3-Alkyl); Ar represents unsubstituted or at least mono-substituted aryl or heteroaryl. Said compounds are inhibitors of poly(ADP-ribose)polymerase (PARP) and are used in medicaments for the treatment of a disease which is selected from the following: tissue damage resulting from cell damage or cell death based on necrosis or apoptosis, neuronally mediated tissue damage or diseases, cerebral ischaemia, head trauma, cerebral apoplexy, reperfusion damage, neurological disorders and neurodegenerative diseases, vascular accidents, cardiovascular disorders, myocardial infarction, myocardial ischaemia, experimental allergic encephalomyelitis (EAE), multiple sklerosis (MS), ischaemia related to heart-surgery, age-related macular degeneration, arthritis, Arterosclerosis, cancer, sceletal- muscle degenerative diseases resulting in replicative senescence, diabetes and diabetic myocardial diseases.