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    • 1. 发明授权
    • N-oxide anthranylamide derivatives and their use as medicaments
    • N-氧化物苯甲酰胺衍生物及其作为药物的用途
    • US07459470B2
    • 2008-12-02
    • US10476755
    • 2002-05-03
    • Alexander ErnstAndreas HuthMartin KruegerKarl-Heniz ThierauchAndreas MenradMartin Haberey
    • Alexander ErnstAndreas HuthMartin KruegerKarl-Heniz ThierauchAndreas MenradMartin Haberey
    • A61K31/47C07D213/89
    • C07D213/89C07D401/12C07D405/12
    • Substituted N-oxidanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.
    • 描述了取代的N-氧化邻氨基苯甲酰胺衍生物,其作为用于治疗由持续性血管生成触发的疾病的药剂的生产和用途被描述。 根据本发明的化合物可以用作银屑病,卡波西肉瘤,再狭窄,子宫内膜异位症,克罗恩病,霍奇金病,白血病,牛皮癣, 关节炎,如类风湿关节炎,血管瘤,血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变,新生血管性青光眼; 肾脏疾病如肾小球性肾炎,糖尿病肾病,恶性肾硬化,血栓性微血管病综合征,移植排斥反应和肾小球病; 纤维化疾病,如肝硬化,肾小球膜细胞增生性疾病,动脉硬化,神经组织损伤,以及球囊导管治疗后血管再狭窄的抑制,血管修复术或机械装置用于保持血管开放的诸如 例如作为免疫抑制剂的支架,作为无疤痕愈合的支持,老年角化病和接触性皮炎。 在淋巴管生成的情况下,根据本发明的化合物也可以用作VEGFR-3抑制剂。