QUINONE SUBSTITUTED QUINAZOLINE AND QUINOLINE KINASE INHIBITORS

• Main Authors: NILAKANTAN, RAMASWAMY, INGALLS, CHARLES, FRASER, HEIDI, LEIGH, FLOYD, MIDDLETON, B., JR, WISSNER, ALLAN, DUSHIN, RUSSELL, GEORGE, JOHNSON, BERNARD, DEAN, NITTOLI, THOMAS
• Format: Patent
• Language: English; French
• Published: 08.12.2005
• Edition: 7
• Subjects: AGRICULTURE; ANIMAL HUSBANDRY; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES; CHEMISTRY; FISHING; FORESTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HUNTING; METALLURGY; ORGANIC CHEMISTRY; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF; TRAPPING

The present invention provides for compounds with the general formula: A compound of formula (1) having the structure (1) wherein Z is a radical selected from the group (a), (b), or (c) as well as methods and compositions containing these compounds useful for treatment of diseases that are characterized, at least in part, by excessive, abnormal, or inappropriate angiogenesis. These disease states, include but are not limited to, cancer, diabetic retinopathy, macular degeneration and rheumatoid arthritis. These compounds inhibit angiogenesis by inhibiting a tyrosine kinase receptor enzyme, specifically KDR, and binding to the KDR in an irreversible manner. L'invention concerne des composés de formule générale ci-après: on décrit un composé de formule (1) ayant la structure (1) sachant que Z est un radical pouvant être du groupe (a), (b), ou (c), ainsi que des procédés, et des compositions renfermant les composés, utiles pour le traitement de maladies caractérisées au moins en partie par une angiogenèse excessive, anormale ou inadéquate. Les maladies peuvent être, sans limitation : cancer, rétinopathie diabétique, dégénérescence maculaire et polyarthrite rhumatoïde. Les composés inhibent l'angiogenèse par inhibition d'enzyme de récepteur de tyrosine kinase, spécifiquement KDR, et liaison avec KDR en mode irréversible.