3-(2-bromo-3,4-dihydroxyphenyl)-N-(3,4,5-trihydroxy-benzyl)thioacrylamide | 1198078-60-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 3-(2-bromo-3,4-dihydroxyphenyl)-N-(3,4,5-trihydroxy-benzyl)thioacrylamide
• 英文别名: Nt-219；(E)-3-(2-bromo-3,4-dihydroxyphenyl)-N-[(3,4,5-trihydroxyphenyl)methyl]prop-2-enethioamide
• CAS: 1198078-60-2
• 化学式: C₁₆H₁₄BrNO₅S
• 分子量: 412.261
• InChiKey: XDDQKKXXQHUUHJ-DUXPYHPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  145
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  3-(2-bromo-3,4-dimethoxyphenyl)-N-(3,4,5-trimethoxy-benzyl)thioacrylamide 在 三溴化硼 作用下， 以 二氯甲烷 为溶剂， 生成 3-(2-bromo-3,4-dihydroxyphenyl)-N-(3,4,5-trihydroxy-benzyl)thioacrylamide
  参考文献：
  名称：

  CN115466205

  摘要：

  公开号：

文献信息

• IGF-1R SIGNALING PATHWAY INHIBITORS USEFUL IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
  申请人：YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD.

  公开号：US20160158243A1

  公开（公告）日：2016-06-09

  The present invention provides compounds acting as Insulin/IGF signaling modulators useful in the treatment of neurodegenerative diseases and disorders. The invention provides pharmaceutical compositions including such compounds, and methods of using these compounds and compositions for the treatment of neurodegenerative diseases, in particular neurodegenerative diseases caused by proteotoxicity such as Alzheimer's disease.

  本发明提供了作为胰岛素/IGF信号调节剂的化合物，用于治疗神经退行性疾病和紊乱。该发明提供了包括这些化合物的药物组合物，以及利用这些化合物和组合物治疗神经退行性疾病的方法，特别是由蛋白毒性引起的神经退行性疾病，如阿尔茨海默病。
• [EN] NOVEL MODULATORS OF PROTEIN KINASE SIGNALING<br/>[FR] NOUVEAUX MODULATEURS DE LA SIGNALISATION DE PROTÉINES KINASES
  申请人：NOVOTYR THERAPEUTICS LTD

  公开号：WO2009147682A1

  公开（公告）日：2009-12-10

  The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.

  本发明提供了新的酪氨酸激酶抑制剂衍生物，可作为蛋白激酶（PK）和受体激酶（RK）信号调节剂。该发明还提供了它们的制备方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物的方法，特别是作为化疗药物，用于预防和治疗PK和RK相关疾病，如代谢性、炎症性、纤维化和细胞增殖性疾病，特别是癌症。
• NOVEL MODULATORS OF PROTEIN KINASE SIGNALING
  申请人：Reuveni Hadas

  公开号：US20110105618A1

  公开（公告）日：2011-05-05

  The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.

  本发明提供了新的酪氨酸激酶（PK）和受体激酶（RK）信号调节剂的酪氨酸激酶抑制剂衍生物。本发明还提供了其制备方法，包括这些化合物的制药组合物，以及使用这些化合物和组合物的方法，特别是作为化疗药物，用于预防和治疗PK和RK相关疾病，如代谢性、炎症性、纤维化和细胞增生性疾病，特别是癌症。
• IGF-1R signaling pathway inhibitors useful in the treatment of neurodegenerative diseases
  申请人：YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD.

  公开号：US10188659B2

  公开（公告）日：2019-01-29

  The present invention provides compounds acting as Insulin/IGF signaling modulators useful in the treatment of neurodegenerative diseases and disorders. The invention provides pharmaceutical compositions including such compounds, and methods of using these compounds and compositions for the treatment of neurodegenerative diseases, in particular neurodegenerative diseases caused by proteotoxicity such as Alzheimer's disease.

  本发明提供了可作为胰岛素/IGF 信号调节剂用于治疗神经退行性疾病和紊乱的化合物。本发明提供了包括此类化合物的药物组合物，以及使用这些化合物和组合物治疗神经退行性疾病的方法，特别是由蛋白毒性引起的神经退行性疾病，如阿尔茨海默病。
• Combinations of IRS/Stat3 dual modulators and anti-cancer agents for treating cancer
  申请人：TYRNOVO LTD.

  公开号：US10912745B2

  公开（公告）日：2021-02-09

  Provided is a treatment of cancer using a dual modulator of Insulin Receptor Substrate (IRS) and signal transducer and activator of transcription 3 (Stat3), as well with other agents. The combination can be used to treat a tumor that has developed resistance to an EGFR inhibitor, EGFR antibody, mTOR inhibitor, MEK inhibitor, mutated B-Raf inhibitor, chemotherapeutic agents, and certain combinations thereof, or to prevent acquired resistance of a tumor to any of said inhibitors or agents, or to prevent tumor recurrence following cease of treatment with any of said inhibitors or agents or a combination thereof. The subject matter further provides a treatment of cancer using combination therapy comprising a dual modulator of IRS and Stat3, in combination with an immunotherapy agent. The combination can be used to sensitize a tumor to immunotherapy.

  本发明提供了一种利用胰岛素受体底物（IRS）和信号转导及转录激活因子3（Stat3）双重调节剂以及其他药物治疗癌症的方法。该组合可用于治疗对表皮生长因子受体抑制剂、表皮生长因子受体抗体、mTOR抑制剂、MEK抑制剂、突变B-Raf抑制剂、化疗药物及其某些组合产生耐药性的肿瘤，或用于防止肿瘤对上述任何抑制剂或药物产生获得性耐药性，或用于防止在停止使用上述任何抑制剂或药物或其组合治疗后肿瘤复发。本发明的主题进一步提供了使用联合疗法治疗癌症的方法，联合疗法包括 IRS 和 Stat3 的双重调节剂以及免疫疗法制剂。该组合可用于使肿瘤对免疫疗法敏感。