1420998-43-1Relevant articles and documents
FLUORINATED QUINOLINE AND QUINOXALINE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES
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Page/Page column 73-74, (2021/05/07)
The present invention discloses compounds formula (I): (I) wherein X is CH; The present compounds of formula (I) are dihydroorotate dehydrogenase (DHODH) inhibitors, and are useful for the treatment of inflammatory disorders, autoimmune disorders and cancer, such as e.g. lymphomas, leukemias, carcinomas, and sarcomas. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 60 to 136; examples 1 to 39; tables 1 and 2). An exemplary compound is e.g. : 4-ethyl-1-(7-fluoro-4-isopropyl-2- (2-methoxyphenyl)quinolin-6-yl)-3-(hydroxymethyl)-1H-1,2,4- triazol-5(4H)-one (example 1): (AA)
OXAZOLE AND THIAZOLE DERIVATIVES AS SELECTIVE PROTEIN KINASE INHIBITORS (C-KIT)
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Page/Page column 78-80, (2013/03/26)
The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, A, Q, W and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.