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    • 5. 发明授权
    • VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
    • VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶
    • US07517894B2
    • 2009-04-14
    • US10870491
    • 2004-06-18
    • Andreas HuthLudwig ZornMartin KruegerStuart InceKarl Heinz ThierauchAndreas MenradMartin HabereyHolger Hess-Stumpp
    • Andreas HuthLudwig ZornMartin KruegerStuart InceKarl Heinz ThierauchAndreas MenradMartin HabereyHolger Hess-Stumpp
    • A61K31/4439C07D401/04
    • C07D213/61C07D213/73C07D213/74C07D213/75C07D401/04C07D401/12C07D401/14C07D409/12C07D413/04C07D413/14C07D417/04
    • VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced 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VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺,其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途,以及用于制备化合物的中间产物。 根据本发明的化合物可用于或在肿瘤或转移生长的情况下,牛皮癣,卡波西肉瘤,再狭窄,例如支架诱导的再狭窄,子宫内膜异位,克罗恩病,霍奇金病,白血病; 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假体中或使用机械装置用于保持血管开放(例如,支架)作为免疫抑制剂的抑制,作为免疫抑制剂 无疤痕愈合,老年角化病和接触性皮炎的支持。 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。
    • 6. 发明申请
    • VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
    • VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶
    • US20070015794A1
    • 2007-01-18
    • US11525091
    • 2006-09-22
    • Andreas HuthLudwig ZornMartin KrugerStuart InceKarl-Heinz ThierauchAndreas MenradMartin HabereyHolger Hess-Stumpp
    • Andreas HuthLudwig ZornMartin KrugerStuart InceKarl-Heinz ThierauchAndreas MenradMartin HabereyHolger Hess-Stumpp
    • A61K31/444A61K31/44C07D401/02C07D213/72
    • C07D213/72C07D401/02
    • VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced 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VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺,其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途,以及用于制备化合物的中间产物。 根据本发明的化合物可用于或在肿瘤或转移生长的情况下,牛皮癣,卡波西肉瘤,再狭窄,例如支架诱导的再狭窄,子宫内膜异位,克罗恩病,霍奇金病,白血病; 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。
    • 8. 发明授权
    • VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
    • VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶
    • US07615565B2
    • 2009-11-10
    • US11525091
    • 2006-09-22
    • Andreas HuthLudwig ZornMartin KrugerStuat InceKarl-Heinz ThierauchAndreas MenradMartin HabereyHolger Hess-Stumpp
    • Andreas HuthLudwig ZornMartin KrugerStuat InceKarl-Heinz ThierauchAndreas MenradMartin HabereyHolger Hess-Stumpp
    • A61K31/47C07D217/22
    • C07D213/72C07D401/02
    • VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced 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VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺,其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途,以及用于制备化合物的中间产物。 根据本发明的化合物可用于或在肿瘤或转移生长的情况下,牛皮癣,卡波西肉瘤,再狭窄,例如支架诱导的再狭窄,子宫内膜异位,克罗恩病,霍奇金病,白血病; 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。