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SELECTIVE ANTHRANILAMIDE PYRIDINAMIDES AS VEGFR-2 AND VEGFR-3 INHIBITORS

机译:选择性蒽酰胺吡啶类作为VEGFR-2和VEGFR-3抑制剂

摘要

The invention relates to selective anthranilamide pyridine amides asinhibitors of VEGFR-2 and VEGFR-3 and to their production and use asmedicaments for treating diseases that are caused by persistent angiogenesis.The inventive compounds can be used for example in cases of psoriasis,Kaposi's sarcoma, restenosis, such as e.g. stent-induced restenosis,endometriosis, Crohn's disease, Hodgkin's disease, leukaemia, arthritis, suchas rheumatoid arthritis, haemangioma, angiofibromatosis, in eye diseases suchas diabetic retinopathy, neovascular glaucoma, in kidney diseases such asglomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombicmicro-angiopathic syndrome, transplant rejection and glomerulopathy, infibrotic diseases such as hepatic cirrhosis, mesangial-cell proliferativediseases, arteriosclerosis, damage to the nerve tissue and inhibition of there-occlusion of vessels after balloon catheter treatment, in vesselprosthetics or after the use of mechanical devices for keeping vessels open,e.g. stents, as immunosuppressants, to support wound healing without scars andin cases of age spots and contact dermatitis. The inventive compounds can alsobe used as inhibitors of VEGFR-3 in lymphangiogenesis for hyperplastic anddysplastic changes in the lymphatic system.
机译:本发明涉及选择性的邻氨基苯甲酰胺吡啶酰胺作为抑制VEGFR-2和VEGFR-3及其生产和使用用于治疗由持续性血管生成引起的疾病的药物。本发明化合物可用于例如牛皮癣,卡波西氏肉瘤,再狭窄,例如支架引起的再狭窄子宫内膜异位症,克罗恩氏病,霍奇金氏病,白血病,关节炎等如类风湿关节炎,血管瘤,血管纤维瘤病,眼病等如糖尿病性视网膜病,新生血管性青光眼,肾脏疾病肾小球肾炎,糖尿病肾病,恶性肾硬化,血栓微血管病变综合征,移植排斥和肾小球病纤维化疾病,例如肝硬化,肾小球膜细胞增生疾病,动脉硬化,神经组织损伤和抑制球囊导管治疗后血管再次阻塞义肢或使用机械装置保持血管畅通后,例如支架,作为免疫抑制剂,可支持伤口愈合而无疤痕和如果出现老年斑和接触性皮炎。本发明的化合物还可以在增生性和淋巴管生成中用作VEGFR-3抑制剂淋巴系统异常增生的变化。

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