2-(4-cyclopropylpiperazin-1-yl)ethanamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-(4-cyclopropylpiperazin-1-yl)ethanamine
• 化学式: C₉H₁₉N₃
• 分子量: 169.27
• InChiKey: PXTHYXXLWIZEQS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-((4-((4-(3-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)ureido)naphthalen-1-yl)oxy)pyridin-2-yl)amino)-2-methoxybenzoic acid hydrochloride 、 2-(4-cyclopropylpiperazin-1-yl)ethanamine 在 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以48 mg的产率得到4-((4-((4-(3-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)ureido)naphthalen-1-yl)oxy)pyridin-2-yl)amino)-N-(2-(4-cyclopropylpiperazin-1-yl)ethyl)-2-methoxybenzamide
  参考文献：
  名称：

  [EN] DIARYL UREA DERIVATIVES AS P38 KINASE INHIBITORS
  [FR] DÉRIVÉS DE DIARYLE-URÉE EN TANT QU'INHIBITEURS DE KINASE P38

  摘要：

  提供了具有公式I的化合物，其中R1A至R1E，R2至R4，R5a，L和X1至X3的含义如描述中所示，这些化合物具有抗炎活性（例如，通过抑制p38丝裂原活化蛋白激酶酶家族中的一个或多个成员；Syk激酶；和酪氨酸激酶Src家族成员）并用于治疗，包括在药物组合中，特别是用于治疗包括肺部、眼睛和肠道炎症疾病在内的炎症性疾病。

  公开号：

  WO2016051187A1

文献信息

• KINASE INHIBITORS
  申请人：RESPIVERT LIMITED

  公开号：US20160102059A1

  公开（公告）日：2016-04-14

  There are provided compounds of formula I, wherein R 1A to R 1E , R 2 to R 4 , R 5a , L and X 1 to X 3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

  提供了化合物I的公式，其中R1A至R1E、R2至R4、R5a、L和X1至X3具有描述中给出的含义，这些化合物具有抗炎活性（例如通过抑制p38有丝分裂原活化蛋白激酶酶家族的一个或多个成员、Syk激酶以及酪氨酸激酶Src家族的成员之一），并且在治疗中有用，包括在药物组合中，特别是用于治疗炎症性疾病，包括肺部、眼部和肠道的炎症性疾病。
• Kinase inhibitors
  申请人：Respivert Limited

  公开号：US10125100B2

  公开（公告）日：2018-11-13

  There are provided compounds of formulas III and VIIa: or a salt or protected derivative thereof, wherein Z2 represents a structural fragment of formula V, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity, for example through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

  提供了式 III 和 VIIa 的化合物：或其盐或受保护的衍生物，其中 Z2 代表式 V 的结构片段，其中 R1A 至 R1E、R2 至 R4、R5a、L 和 X1 至 X3 具有描述中给出的含义，这些化合物具有抗炎活性，例如通过抑制以下成员中的一种或多种：p38 丝裂原活化蛋白激酶家族；Syk 激酶；以及 Src 家族酪氨酸激酶），并具有治疗用途，包括用于药物组合，特别是用于治疗： p38丝裂原活化蛋白激酶家族；Syk激酶；酪氨酸激酶Src家族成员），可用于治疗，包括药物组合，特别是治疗炎症性疾病，包括肺、眼和肠道的炎症性疾病。
• Triterpene amine derivatives
  申请人：DFH THERAPEUTICS

  公开号：US11236122B2

  公开（公告）日：2022-02-01

  The present invention concerns novel pharmaceutically active triterpene amine derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the triterpene amine compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C-28 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus-1 (HIV-1).

  本发明涉及新型具有药用活性的三萜胺衍生物、含有三萜胺衍生物的药物组合物、其作为药物的用途，以及使用这些化合物制造特定药物。本发明还涉及一种涉及三萜胺化合物给药的治疗方法。具体来说，这些化合物是白桦脂酸的衍生物，在 C-3、C-28 和 C-19 位上有一个或多个取代位，如本文进一步描述的那样。这些新型化合物可用作抗逆转录病毒药物。特别是，这些新型化合物可用于治疗人类免疫缺陷病毒-1（HIV-1）。
• EP3201179A1
  申请人：——

  公开号：EP3201179A1

  公开（公告）日：2017-08-09
• TRITERPENE AMINE DERIVATIVES
  申请人：DFH THERAPEUTICS

  公开号：US20210253627A1

  公开（公告）日：2021-08-19

  The present invention concerns novel pharmaceutically active triterpene amine derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the triterpene amine compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C-28 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus-1 (HIV-1).