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    • 8. 发明授权
    • Eurotinones, and derivatives thereof, processes for preparing them, and their use
    • 欧卡因及其衍生物,其制备方法及其应用
    • US06818667B2
    • 2004-11-16
    • US10180003
    • 2002-06-26
    • Claudia EderHerbert KoglerLuigi Toti
    • Claudia EderHerbert KoglerLuigi Toti
    • A61K31335
    • C07D313/12
    • The present invention relates to novel compounds of the formula I in which R(1), R(2), R(3) and R(4) are, independently of each other, hydrogen or an alkyl radical. The compounds of the formula I are inhibitors of KDR kinase and, due to their antiangiogenic effect, are suitable for preventing and/or treating malignant diseases. The compounds of the formula I can be obtained by fermenting the microorganism Eurotium echinulatum Delacroix (DSM 13872) or by chemically derivatizing the compounds which are obtained after fermenting said microorganism. The invention consequently also relates to a process for preparing the compounds of the formula I, to the use of the compounds of the formula I for preparing a pharmaceutical for treating malignant diseases and diseases which can be treated by inhibiting KDR kinase, and also to pharmaceutical preparations which have a content of at least one compound of the formula I.
    • 本发明涉及式Iin的新化合物,其中R(1),R(2),R(3)和R(4)彼此独立地为氢或烷基。 式I的化合物是KDR激酶的抑制剂,并且由于其抗血管生成作用,适用于预防和/或治疗恶性疾病。 式I的化合物可以通过发酵微生物欧氏螺旋体(DSM 13872)或通过化学衍生在发酵所述微生物后获得的化合物而获得。 因此,本发明还涉及制备式I化合物的方法,使用式I化合物来制备治疗可通过抑制KDR激酶治疗的恶性疾病和疾病的药物,还涉及药物 具有至少一种式I化合物含量的制剂。