4,5-dichloro-N-phenylpyridin-2-amine

• 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: 4,5-dichloro-N-phenylpyridin-2-amine
• 化学式: C₁₁H₈Cl₂N₂
• 分子量: 239.104
• InChiKey: CRQKGBYHQAOACI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  24.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4,5-dichloro-N-phenylpyridin-2-amine 在 lithium hydroxide monohydrate 、 水 、 potassium carbonate 作用下， 以 四氢呋喃 、 N,N-dimethyl-d₆-formamide 为溶剂， 反应 10.25h， 生成 1-(5-chloro-2-(phenylamino)pyridin-4-yl)-1H-imidazole-4-carboxylic acid
  参考文献：
  名称：

  HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER

  摘要：

  本申请提供了新颖的杂环化合物及其药用可接受的盐。还提供了制备这些化合物的方法。这些化合物对抑制ERK1/2有用。通过向需要治疗的患者施用式(I)的一个或多个化合物的治疗有效量，其中X、Y、Z、J、M和R1至R8在此处定义，这些化合物在治疗与RAS/RAF/MEK/ERK通路失调相关的疾病方面是有效的。可以使用这些化合物治疗各种疾病，包括以异常细胞增殖为特征的疾病。在一个实施例中，该疾病是癌症。

  公开号：

  US20160362407A1
• 作为产物：
  描述：

  2-氨基-4-氯吡啶 在 盐酸 、 tris-(dibenzylideneacetone)dipalladium(0) 、 N-氯代丁二酰亚胺 、 caesium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 1,4-二氧六环 、 吡啶 、 水 、 乙腈 为溶剂， 反应 13.0h， 生成 4,5-dichloro-N-phenylpyridin-2-amine
  参考文献：
  名称：

  HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER

  摘要：

  本申请提供了新颖的杂环化合物及其药用可接受的盐。还提供了制备这些化合物的方法。这些化合物对抑制ERK1/2有用。通过向需要治疗的患者施用式(I)的一个或多个化合物的治疗有效量，其中X、Y、Z、J、M和R1至R8在此处定义，这些化合物在治疗与RAS/RAF/MEK/ERK通路失调相关的疾病方面是有效的。可以使用这些化合物治疗各种疾病，包括以异常细胞增殖为特征的疾病。在一个实施例中，该疾病是癌症。

  公开号：

  US20160362407A1

文献信息

• HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
  申请人：Asana Biosciences, LLC

  公开号：US20160362407A1

  公开（公告）日：2016-12-15

  The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R 1 to R 8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

  本申请提供了新颖的杂环化合物及其药用可接受的盐。还提供了制备这些化合物的方法。这些化合物对抑制ERK1/2有用。通过向需要治疗的患者施用式(I)的一个或多个化合物的治疗有效量，其中X、Y、Z、J、M和R1至R8在此处定义，这些化合物在治疗与RAS/RAF/MEK/ERK通路失调相关的疾病方面是有效的。可以使用这些化合物治疗各种疾病，包括以异常细胞增殖为特征的疾病。在一个实施例中，该疾病是癌症。
• Heterocyclic inhibitors of ERK1 and ERK2 and their use in the treatment of cancer
  申请人：Asana Biosciences, LLC

  公开号：US10471051B2

  公开（公告）日：2019-11-12

  The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

  本申请提供了新型杂环化合物及其药学上可接受的盐类。还提供了制备这些化合物的方法。这些化合物可用于抑制 ERK1/2。通过向有需要的患者施用一种或多种治疗有效量的式(I)化合物，其中X、Y、Z、J、M和R1至R8在本文中定义，这些化合物可有效治疗与RAS/RAF/MEK/ERK通路失调相关的病症。使用这些化合物可以治疗多种疾病，包括以细胞异常增殖为特征的疾病。在一个实施方案中，疾病是癌症。
• HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATEMENT OF CANCER
  申请人：Asana Biosciences, LLC

  公开号：US20170362216A1

  公开（公告）日：2017-12-21

  The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R 1 to R 8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
• US9896445B2
  申请人：——

  公开号：US9896445B2

  公开（公告）日：2018-02-20
• [EN] HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] INHIBITEURS HÉTÉROCYCLIQUES DES PROTÉINES ERK1 ET ERK2 ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER
  申请人：ASANA BIOSCIENCES LLC

  公开号：WO2016205418A1

  公开（公告）日：2016-12-22

  The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERKl/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.