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    • 7. 发明申请
    • Quinoline Derivatives Having Vegf Inhibiting Activity
    • 喹啉衍生物具有抑制活性
    • US20080312273A1
    • 2008-12-18
    • US11947533
    • 2007-11-29
    • Laurent Francois Andre Hennequin
    • Laurent Francois Andre Hennequin
    • A61K31/47C07D215/16A61P9/00
    • C07D401/12C07D401/14
    • The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH— or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or direct bond; Z is linked to any one of G1, G2, G3, and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of diseases states including cancer and rheumatoid arthritis.
    • 本发明涉及式(I)化合物,其中:G 1,G 2,G 3,G 4和G 5中的任一个为氮,其余四个为-CH-或G 1,G 3,G 3,G 4和G 5均为-CH- ; Z是-O-,-NH-,-S-,-CH 2 - 或直接键; Z连接到G1,G2,G3和G4中的任一个; n为0〜5的整数, m是0至3的整数; Ra表示氢或氟; 本文定义了Rb,R1和R2及其盐,制备方法使得这些化合物,含有式I化合物的药物组合物或其药学上可接受的盐作为活性成分,以及式I化合物在制备 用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物。 式I化合物及其药学上可接受的盐抑制VEGF的作用,其在治疗许多疾病状态(包括癌症和类风湿性关节炎)中是有价值的。