| abstract |
QUINOLINE, QUINOXALINE AND BENZO[B][1,4]OXAZINE DERIVATIVES FLUORORATED AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES. The present invention relates to compounds of formula (I): (I) wherein X is CH; R2 is (AA), R3 is (BB). The present compounds of formula (I) are inhibitors of dihydroorotate dehydrogenase (DHODH) and are useful for the treatment of inflammatory disorders, autoimmune disorders and cancer, such as, for example, lymphomas, leukemias, carcinomas and sarcomas. The present description discloses the synthesis and characterization of exemplary compounds, as well as pharmacological data thereof (e.g. pages 61 to 101; Examples 1 to 24; Tables 1 and 2). An exemplary compound is, for example, 7-(4-ethyl-3-(hydroxymethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)-6- fluoro-3-(3-fluorophenyl)-1-isopropylquinolin-4(1H)-one (Example 1): (CC). |