3-methoxy-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-nitrobenzamide

• 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: 3-methoxy-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-nitrobenzamide
• 英文别名: 3-methoxy-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]-4-nitrobenzamide
• 化学式: C₁₈H₁₅N₃O₅S
• 分子量: 385.4
• InChiKey: VVLJUZLXDIBIRI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  135
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  3-methoxy-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-nitrobenzamide 在 palladium 10% on activated carbon 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 生成 3-methoxy-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-((2-morpholino-2-oxoethyl)amino)benzamide
  参考文献：
  名称：

  [EN] MODULATORS OF MYOCYTE LIPID ACCUMULATION AND INSULIN RESISTANCE AND METHODS OF USE THEREOF
  [FR] MODULATEURS D'ACCUMULATION DE LIPIDES DE MYOCYTES ET D'INSULINORÉSISTANCE ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  已开发了用于降低血糖和/或增加受试者胰岛素信号的配方和方法。这些配方包括SBI-477和基于SBI-477的化合物，即SBI-477类似物（统称为SBI-477化合物）和/或Mondo家族抑制剂，以有效量抑制细胞内脂质积累和/或增加细胞葡萄糖摄取，与未施用该组合物的对照受试者相比。还公开了用于减少细胞内脂质积累和/或增加受试者葡萄糖摄取的方法。该方法包括向受试者施用足够量的SBI-477化合物和/或Mondo家族抑制剂，以减少受试者细胞内脂质积累和/或增加葡萄糖摄取。还公开了用于治疗一种或多种Myc驱动的癌症的方法，包括神经母细胞瘤、肺鳞状细胞癌/肺腺癌、肝细胞癌、结肠腺癌、急性髓系白血病和乳腺浸润性癌。

  公开号：

  WO2017019772A1
• 作为产物：
  描述：

  4-(4-甲氧基苯基)-1,3-噻唑-2-胺 、 3-甲氧基-4-硝基苯甲酸 在 三乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 乙腈 为溶剂， 以82%的产率得到3-methoxy-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-nitrobenzamide
  参考文献：
  名称：

  [EN] MODULATORS OF MYOCYTE LIPID ACCUMULATION AND INSULIN RESISTANCE AND METHODS OF USE THEREOF
  [FR] MODULATEURS D'ACCUMULATION DE LIPIDES DE MYOCYTES ET D'INSULINORÉSISTANCE ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  已开发了用于降低血糖和/或增加受试者胰岛素信号的配方和方法。这些配方包括SBI-477和基于SBI-477的化合物，即SBI-477类似物（统称为SBI-477化合物）和/或Mondo家族抑制剂，以有效量抑制细胞内脂质积累和/或增加细胞葡萄糖摄取，与未施用该组合物的对照受试者相比。还公开了用于减少细胞内脂质积累和/或增加受试者葡萄糖摄取的方法。该方法包括向受试者施用足够量的SBI-477化合物和/或Mondo家族抑制剂，以减少受试者细胞内脂质积累和/或增加葡萄糖摄取。还公开了用于治疗一种或多种Myc驱动的癌症的方法，包括神经母细胞瘤、肺鳞状细胞癌/肺腺癌、肝细胞癌、结肠腺癌、急性髓系白血病和乳腺浸润性癌。

  公开号：

  WO2017019772A1

文献信息

• Modulators of myocyte lipid accumulation and insulin resistance and methods of use thereof
  申请人：Sanford Burnham Prebys Medical Discovery Institute

  公开号：US11028061B2

  公开（公告）日：2021-06-08

  Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject. Also disclosed are method for treating one or more Myc-driven cancers, including neuroblastoma, lung squamous cell carcinoma/lung adenocarcinoma, liver hepatocellular carcinoma, colon adenocarcinoma, acute myeloid leukemia, and breast invasive carcinoma.

  用于降低受试者血糖和/或增加胰岛素信号传导的制剂和方法已经研制成功。这些制剂包括SBI-477和基于SBI-477的化合物，即SBI-477类似物（统称为SBI-477化合物）和/或蒙多家族抑制剂，与未施用该组合物的对照组相比，其有效量可抑制细胞内脂质积累和/或增加细胞葡萄糖摄取。还公开了减少有需要的受试者细胞内脂质积累和/或增加葡萄糖摄取的方法。该方法包括向受试者施用有效量的 SBI-477 化合物和/或蒙多家族抑制剂，以减少细胞内脂质积累和/或增加受试者的葡萄糖摄取。还公开了治疗一种或多种Myc驱动的癌症的方法，包括神经母细胞瘤、肺鳞癌/肺腺癌、肝肝细胞癌、结肠腺癌、急性髓性白血病和乳腺浸润性癌。
• MODULATORS OF MYOCYTE LIPID ACCUMULATION AND INSULIN RESISTANCE AND METHODS OF USE THEREOF
  申请人：Sanford Burnham Prebys Medical Discovery Institute

  公开号：US20180222874A1

  公开（公告）日：2018-08-09

  Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject. Also disclosed are method for treating one or more Myc-driven cancers, including neuroblastoma, lung squamous cell carcinoma/lung adenocarcinoma, liver hepatocellular carcinoma, colon adenocarcinoma, acute myeloid leukemia, and breast invasive carcinoma.
• [EN] MODULATORS OF MYOCYTE LIPID ACCUMULATION AND INSULIN RESISTANCE AND METHODS OF USE THEREOF<br/>[FR] MODULATEURS D'ACCUMULATION DE LIPIDES DE MYOCYTES ET D'INSULINORÉSISTANCE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INST

  公开号：WO2017019772A1

  公开（公告）日：2017-02-02

  Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject. Also disclosed are method for treating one or more Myc-driven cancers, including neuroblastoma, lung squamous cell carcinoma/lung adenocarcinoma, liver hepatocellular carcinoma, colon adenocarcinoma, acute myeloid leukemia, and breast invasive carcinoma.

  已开发了用于降低血糖和/或增加受试者胰岛素信号的配方和方法。这些配方包括SBI-477和基于SBI-477的化合物，即SBI-477类似物（统称为SBI-477化合物）和/或Mondo家族抑制剂，以有效量抑制细胞内脂质积累和/或增加细胞葡萄糖摄取，与未施用该组合物的对照受试者相比。还公开了用于减少细胞内脂质积累和/或增加受试者葡萄糖摄取的方法。该方法包括向受试者施用足够量的SBI-477化合物和/或Mondo家族抑制剂，以减少受试者细胞内脂质积累和/或增加葡萄糖摄取。还公开了用于治疗一种或多种Myc驱动的癌症的方法，包括神经母细胞瘤、肺鳞状细胞癌/肺腺癌、肝细胞癌、结肠腺癌、急性髓系白血病和乳腺浸润性癌。