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    Benzimidazole derivatives and their use as kdr kinase protein inhibitors
    6.
    发明申请
    Benzimidazole derivatives and their use as kdr kinase protein inhibitors 审中-公开
    苯并咪唑衍生物及其作为kdr激酶蛋白抑制剂的用途

    公开(公告)号：US20080125418A1

    公开(公告)日：2008-05-29

    申请号：US11943008

    申请日：2007-11-20

    申请人： Didier Babin ,  Alain Le Brun ,  Laurence Gauzy-Lazo ,  Herve Bouchard

    发明人： Didier Babin ,  Alain Le Brun ,  Laurence Gauzy-Lazo ,  Herve Bouchard

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4196 ,  A61K31/4184 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/04 ,  C07D491/04

    摘要： The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitotic agents.

    摘要翻译： 本发明公开并要求式（I）的苯并咪唑化合物：其中X是C-R2; Y为C-R2或C-R3; W和Z各自为C-R3; R 1是任选取代的芳基，杂芳基或饱和的5-或6-元单环杂环基或双环杂环基; A5是H或烷基; 或所述式（I）化合物的立体异构体，外消旋物，对映异构体或非对映异构体或其药学上可接受的盐; 使用式（I）化合物治疗血管增生障碍，不受控制的血管生成，纤维化病症，肾小球膜细胞增殖障碍，代谢紊乱，过敏，哮喘，血栓形成，疾病 神经系统，视网膜病变，银屑病，类风湿性关节炎，糖尿病，肌肉变性，实体瘤和癌症，包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物和包含式（I）化合物的药物组合物， 和一个或多个。 抗有丝分裂剂。