benzyl 6-hydroxy-1H-indole-2-carboxylate | 1427753-33-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: benzyl 6-hydroxy-1H-indole-2-carboxylate
• CAS: 1427753-33-0
• 化学式: C₁₆H₁₃NO₃
• 分子量: 267.284
• InChiKey: KSDMOMDUEZHXSV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  62.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  benzyl 6-hydroxy-1H-indole-2-carboxylate 、 2,3,4,6-tetra-O-acetyl-α-L-galactopyranosyl trichloroacetimidate 在 三氟化硼乙醚 作用下， 以 二氯甲烷 为溶剂， 以45 %的产率得到
  参考文献：
  名称：

  ANTIBODY DRUG CONJUGATES COMPRISING TOXINS WITH POLAR GROUPS AND USES THEREOF

  摘要：

  The present disclosure is directed toward drugs and toxins functionalized by at least one saccharide, sulfate or sulfonate; drug conjugates comprising said drugs or toxins and a cleavable linker; and targeted conjugates comprising said drugs or toxins, cleavable linkers, and targeting moieties. The present disclosure also relates to methods of treating cancers, auto-immune diseases, and inflammatory diseases using the compounds and conjugates of the disclosure.

  公开号：

  US20230190939A1
• 作为产物：
  描述：

  6-羟基-1H-吲哚-2-甲酸甲酯 在 lithium hydroxide monohydrate 、 水 、 三乙胺 、 N,N-二异丙基乙胺 作用下， 以 甲醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 10.0h， 生成 benzyl 6-hydroxy-1H-indole-2-carboxylate
  参考文献：
  名称：

  ANTIBODY DRUG CONJUGATES COMPRISING TOXINS WITH POLAR GROUPS AND USES THEREOF

  摘要：

  The present disclosure is directed toward drugs and toxins functionalized by at least one saccharide, sulfate or sulfonate; drug conjugates comprising said drugs or toxins and a cleavable linker; and targeted conjugates comprising said drugs or toxins, cleavable linkers, and targeting moieties. The present disclosure also relates to methods of treating cancers, auto-immune diseases, and inflammatory diseases using the compounds and conjugates of the disclosure.

  公开号：

  US20230190939A1

文献信息

• Guanidinobenzoic acid compound
  申请人：Fujiyasu Jiro

  公开号：US09199927B2

  公开（公告）日：2015-12-01

  [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

  [问题] 提供了一种化合物，可用作预防和/或治疗肾脏疾病的药剂。 [解决方法] 现有发明人对具有胰蛋白酶抑制作用的化合物进行了广泛的研究，结果发现一种鸟氨酸苯甲酸化合物具有胰蛋白酶抑制作用，从而完成了本发明。本发明的鸟氨酸苯甲酸化合物可用作代替低蛋白饮食疗法的药剂，用于预防和/或治疗肾脏疾病，并且可用作预防和/或治疗与胰腺炎、胃食管反流病、肝性脑病、流感等相关的胰蛋白酶相关疾病的药剂。
• GUANIDINOBENZOIC ACID COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：EP2757093B1

  公开（公告）日：2016-12-07
• US9199927B2
  申请人：——

  公开号：US9199927B2

  公开（公告）日：2015-12-01
• ANTIBODY DRUG CONJUGATES COMPRISING TOXINS WITH POLAR GROUPS AND USES THEREOF
  申请人：IntoCell, Inc.

  公开号：US20230190939A1

  公开（公告）日：2023-06-22

  The present disclosure is directed toward drugs and toxins functionalized by at least one saccharide, sulfate or sulfonate; drug conjugates comprising said drugs or toxins and a cleavable linker; and targeted conjugates comprising said drugs or toxins, cleavable linkers, and targeting moieties. The present disclosure also relates to methods of treating cancers, auto-immune diseases, and inflammatory diseases using the compounds and conjugates of the disclosure.