7-Methyl-2-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzofuran | 1072812-57-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 7-Methyl-2-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzofuran
• 英文别名: 4,4,5,5-Tetramethyl-2-(7-methylbenzofuran-2-yl)-1,3,2-dioxaborolane；4,4,5,5-tetramethyl-2-(7-methyl-1-benzofuran-2-yl)-1,3,2-dioxaborolane
• CAS: 1072812-57-7
• 化学式: C₁₅H₁₉BO₃
• 分子量: 258.125
• InChiKey: OVINLUCADNOQQL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.04
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  31.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  7-氯吲哚-2-硼酸频那醇酯 、 7-甲基苯并呋喃 生成 7-Methyl-2-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzofuran
  参考文献：
  名称：

  Fused bicyclic mTOR inhibitors

  摘要：

  化合物I式（或其药学上可接受的盐）是mTOR抑制剂，可用于治疗癌症。

  公开号：

  US08796455B2

文献信息

• 一种高效催化五元杂环选择性发生硼化反应的方法
  申请人：台州学院

  公开号：CN111039967A

  公开（公告）日：2020-04-21

  本发明涉及一种高效催化五元杂环选择性发生硼化反应的方法。顺利实现以廉价的钌金属的络合物为催化剂，在温和条件下即可方便地催化呋喃、噻吩衍生物与廉价易得的有机硼试剂发生选择性硼化反应来制备杂环硼酸酯产物。与已报道方法相比，该方法具备反应选择性专一、催化剂用量低、操作便捷、不需要添加反应溶剂等明显优势，为杂环硼酸酯产物的实验室制备或工业生产提供了一种高效、高选择性的反应策略。
• Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors
  申请人：Buck A. Elizabeth

  公开号：US20070280928A1

  公开（公告）日：2007-12-06

  The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).

  本发明提供了一种治疗患有非小细胞肺癌、胰腺癌、结肠癌或乳腺癌肿瘤或转移瘤的患者的方法，包括同时或顺序给患者施用治疗有效量的EGFR激酶抑制剂和一种使肿瘤细胞对EGFR激酶抑制剂产生敏感作用的药物，其中该药物为mTOR抑制剂，可以加入其他抗癌药物或放疗等额外的药物或治疗方法。本发明还提供了一种治疗患者肿瘤或转移瘤的方法，包括同时或顺序给患者施用治疗有效量的EGFR激酶抑制剂和一种使肿瘤细胞对EGFR激酶抑制剂产生敏感作用的药物，其中该药物为一种mTOR抑制剂，可结合并直接抑制mTORC1和mTORC2激酶。本发明还提供了一种制药组合物，包括一种EGFR激酶抑制剂和一种可结合并直接抑制mTORC1和mTORC2激酶的mTOR抑制剂，以及药学上可接受的载体。本发明中可用于实施方法的EGFR激酶抑制剂的首选示例是化合物依洛替尼盐酸盐（也称为TARCEVA®）。
• Combination anti-cancer therapy
  申请人：Bhagwat Shripad

  公开号：US20090274698A1

  公开（公告）日：2009-11-05

  The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an anti-cancer agent or treatment that elevates pAkt levels in tumor cells and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. Examples of such anti-cancer agents or treatments include doxorubicin, cisplatin, or ionizing radiation. The present invention also provides a pharmaceutical composition comprising an anti-cancer agent or treatment that elevates pAkt levels in tumor cells and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of the anti-cancer agent melphalan or 5-FU, and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases.

  本发明提供了一种治疗患者肿瘤或肿瘤转移的方法，包括同时或顺序给患者施用抗癌药物或提高肿瘤细胞pAkt水平的治疗剂量和结合并直接抑制mTORC1和mTORC2激酶的mTOR抑制剂。这样的抗癌药物或治疗剂包括多柔比星、顺铂或电离辐射。本发明还提供了一种药物组合，包括抗癌药物或提高肿瘤细胞pAkt水平的治疗剂量和结合并直接抑制mTORC1和mTORC2激酶的mTOR抑制剂，以及药学上可接受的载体。本发明还提供了一种治疗患者肿瘤或肿瘤转移的方法，包括同时或顺序给患者施用治疗剂量的抗癌药物美法仑或5-FU和结合并直接抑制mTORC1和mTORC2激酶的mTOR抑制剂。
• FUSED BICYCLIC mTOR INHIBITORS
  申请人：Chen Xin

  公开号：US20100099679A1

  公开（公告）日：2010-04-22

  Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

  公式（I）所代表的化合物或其药学上可接受的盐，是mTOR的抑制剂，可用于癌症的治疗。
• Fused Bicyclic mTOR Inhibitors
  申请人：Chen Xin

  公开号：US20110218183A1

  公开（公告）日：2011-09-08

  Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

  公式（I）所代表的化合物或其药学上可接受的盐，是mTOR的抑制剂，可用于癌症的治疗。