2-amino-N-(2-oxo-2,3-dihydro-1H-indol-6-yl)-benzamide | 474799-45-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-amino-N-(2-oxo-2,3-dihydro-1H-indol-6-yl)-benzamide
• 英文别名: 2-amino-N-(2-oxo-1,3-dihydroindol-6-yl)benzamide
• CAS: 474799-45-6
• 化学式: C₁₅H₁₃N₃O₂
• 分子量: 267.287
• InChiKey: BQBNAKFMBUHASE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  84.2
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-羟基吡啶-5-醛 、 2-amino-N-(2-oxo-2,3-dihydro-1H-indol-6-yl)-benzamide 在 溶剂黄146 、 sodium cyanoborohydride 作用下， 以 甲醇 为溶剂， 反应 24.0h， 以82%的产率得到N-(2-oxo-2,3-dihydro-1H-indol-6-yl)-2-[(6-oxo-1,6-dihydro-pyridin-3-ylmethyl)-amino]-benzamide
  参考文献：
  名称：

  Selected anthranilaminde pyridinamides and their use as pharmaceutical agents

  摘要：

  通用式I1中选择的蒽酰胺吡啶胺化合物，其中R1和R2的含义如描述中所示，作为VEGFR-2和VEGFR-3抑制剂，其生产和用途作为治疗由持续血管生成引起的各种疾病的药物代理被描述。

  公开号：

  US20040039019A1

文献信息

• Selective anthranilamide pyridine amides as inhibitors of vegfr-2 and vegfr-3
  申请人：——

  公开号：US20040254185A1

  公开（公告）日：2004-12-16

  Selective anthranilamide pyridinamides as VEGFR-2 and VEGFR-3 inhibitors, 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, 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 in hyper- and dysplastic changes of the lymphatic system.

  本发明涉及选择性蒽酰胺吡啶酰胺作为VEGFR-2和VEGFR-3抑制剂，其制备和用作治疗由持续性血管生成引起的疾病的药物。根据本发明的化合物可用于治疗银屑病、卡波西肉瘤、再狭窄（例如，支架引起的再狭窄）、子宫内膜异位症、克罗恩病、霍奇金病、白血病、关节炎（如类风湿性关节炎）、血管瘤、血管纤维瘤、眼部疾病（如糖尿病视网膜病变、新生血管性青光眼）、肾脏疾病（如肾小球肾炎、糖尿病肾病、恶性肾硬化、血栓性微血管病综合征、移植排斥和肾小球病）、纤维化疾病（如肝硬化、系膜细胞增生性疾病、动脉硬化、神经组织损伤和气球导管治疗后的血管再闭塞抑制剂、血管成形术或机械设备用于保持血管开放（如支架））、免疫抑制剂、支持无瘢痕愈合、老年性角化病和接触性皮炎。根据本发明的化合物也可用作VEGFR-3抑制剂，用于淋巴系统的高增生和异常增生变化中的淋巴生成。