2-nitro-4-pyridin-4-ylphenylamine | 1404562-18-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-nitro-4-pyridin-4-ylphenylamine
• 英文别名: 2-Nitro-5-pyridin-4-yl-phenylamine；2-nitro-5-pyridin-4-ylaniline
• CAS: 1404562-18-0
• 化学式: C₁₁H₉N₃O₂
• 分子量: 215.211
• InChiKey: ARNZVGBZRQCFQE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  84.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-nitro-4-pyridin-4-ylphenylamine 在 palladium on activated charcoal 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 为溶剂， 反应 7.0h， 生成 N-(2-amino-5-pyridin-4-ylphenyl)-1,3-dihydropyrrolo[3,4-c]pyridine-2-carboxamide
  参考文献：
  名称：

  [EN] HETEROBICYCLIC N-AMINOPHENYL-AMIDES AS INHIBITORS OF HISTONE DEACETYLASE
  [FR] N-AMINOPHÉNYL-AMIDES HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE L'HISTONE DÉSACÉTYLASE

  摘要：

  这项发明提供了抑制HDAC2的化合物。这些化合物（例如，符合式（I）的化合物或化合物100-175中的任何一种）可用于治疗、缓解或预防受试者中的某种疾病，如神经系统疾病、记忆或认知功能障碍或损伤、消退学习障碍、真菌疾病或感染、炎症性疾病、血液疾病或肿瘤性疾病，或用于改善记忆或治疗、缓解或预防记忆丧失或损伤。

  公开号：

  WO2017007755A1
• 作为产物：
  描述：

  5-溴-2-硝基苯胺 、 吡啶-4-硼酸 在 四(三苯基膦)钯 、 caesium carbonate 作用下， 以 1,4-二氧六环 为溶剂， 以58%的产率得到2-nitro-4-pyridin-4-ylphenylamine
  参考文献：
  名称：

  [EN] HETEROBICYCLIC N-AMINOPHENYL-AMIDES AS INHIBITORS OF HISTONE DEACETYLASE
  [FR] N-AMINOPHÉNYL-AMIDES HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE L'HISTONE DÉSACÉTYLASE

  摘要：

  这项发明提供了抑制HDAC2的化合物。这些化合物（例如，符合式（I）的化合物或化合物100-175中的任何一种）可用于治疗、缓解或预防受试者中的某种疾病，如神经系统疾病、记忆或认知功能障碍或损伤、消退学习障碍、真菌疾病或感染、炎症性疾病、血液疾病或肿瘤性疾病，或用于改善记忆或治疗、缓解或预防记忆丧失或损伤。

  公开号：

  WO2017007755A1

文献信息

• Inhibitors of Histone Deacetylase
  申请人：The Broad Institute, Inc.

  公开号：US20140080800A1

  公开（公告）日：2014-03-20

  The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R 2a , R 2b , R 2c , R 5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

  本发明涉及式（I）的化合物：或其药学上可接受的盐、水合物、溶剂合物或前药，其中U、J、V、X、R2a、R2b、R2c、R5和t如本文所述。本发明通常涉及组织脱乙酰化酶抑制剂及其制备和使用方法。这些化合物有助于促进认知功能和增强学习和记忆形成。此外，这些化合物对于治疗、缓解和/或预防各种疾病有用，包括但不限于神经系统疾病、记忆和认知功能障碍、消退学习障碍、真菌病和感染、炎症性疾病、血液病和动物的肿瘤疾病。
• INHIBITORS OF HISTONE DEACETYLASE
  申请人：The Broad Institute, Inc.

  公开号：US20160251351A1

  公开（公告）日：2016-09-01

  The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R 1a , R 2b , R 2c , R 5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

  本发明涉及化合物式(I)或其药学上可接受的盐、水合物、溶剂合物或前药，其中U、J、V、X、R1a、R2b、R2c、R5和t如本文所述。本发明通常涉及组织脱乙酰化酶抑制剂及其制备和使用方法。这些化合物有助于促进认知功能，增强学习和记忆形成。此外，这些化合物在治疗、缓解和/或预防各种疾病方面也很有用，包括例如神经系统疾病、记忆和认知功能障碍、消退学习障碍、真菌疾病和感染、炎症性疾病、血液疾病和动物的肿瘤性疾病。
• Inhibitors of histone deacetylase
  申请人：The Broad Institute, Inc.

  公开号：US10662199B2

  公开（公告）日：2020-05-26

  The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

  本发明涉及式（I）化合物： 或其药学上可接受的盐、水合物、溶液或原药，其中 U、J、V、X、R2a、R2b、R2c、R5 和 t 如本文所述。本发明一般涉及组蛋白去乙酰化酶抑制剂及其制造和使用方法。这些化合物有助于促进认知功能，增强学习和记忆的形成。此外，这些化合物还可用于治疗、减轻和/或预防各种病症，包括例如人类和动物的神经系统疾病、记忆和认知功能障碍/损伤、绝迹学习障碍、真菌疾病和感染、炎症性疾病、血液病和肿瘤性疾病。
• WO2006/47302
  申请人：——

  公开号：——

  公开（公告）日：——
• HETEROBICYCLIC N-AMINOPHENYL-AMIDES AS INHIBITORS OF HISTONE DEACETYLASE
  申请人：RODIN THERAPEUTICS, INC.

  公开号：US20180194760A1

  公开（公告）日：2018-07-12

  This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I) or any one of Compounds 100-175) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.