1-(2-methoxypyridin-4-yl)ethan-1-amine | 1060807-28-4

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(2-methoxypyridin-4-yl)ethan-1-amine
• 英文别名: 1-(2-Methoxypyridin-4-YL)ethanamine；1-(2-methoxypyridin-4-yl)ethanamine
• CAS: 1060807-28-4
• 化学式: C₈H₁₂N₂O
• mdl: MFCD13188773
• 分子量: 152.196
• InChiKey: FFQSFIMSXWJIAT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.375
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-ethoxy-5-isobutyramidobenzoic acid 、 1-(2-methoxypyridin-4-yl)ethan-1-amine 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以70.5 %的产率得到2-ethoxy-5-isobutyramido-N-(1-(2-methoxypyridin-4-yl)ethyl)-benzamide
  参考文献：
  名称：

  Discovery of 2-Ethoxy-5-isobutyramido-N-1-substituted Benzamide Derivatives as Selective Kv2.1 Inhibitors with In Vivo Neuroprotective Effects

  摘要：

  DOI：

  10.1021/acs.jmedchem.3c01245
• 作为产物：
  描述：

  1-(2-methoxypyridin-4-yl)ethan-1-one oxime 在 palladium 10% on activated carbon 、 甲酸铵 作用下， 以 甲醇 为溶剂， 生成 1-(2-methoxypyridin-4-yl)ethan-1-amine
  参考文献：
  名称：

  Discovery of 2-Ethoxy-5-isobutyramido-N-1-substituted Benzamide Derivatives as Selective Kv2.1 Inhibitors with In Vivo Neuroprotective Effects

  摘要：

  DOI：

  10.1021/acs.jmedchem.3c01245

文献信息

• [EN] MAP4K1 INHIBITORS<br/>[FR] INHIBITEURS DE MAP4K1
  申请人：BAYER AG

  公开号：WO2022167627A1

  公开（公告）日：2022-08-11

  The present invention relates to Map4K1 inhibitors of formula (I) (I), wherein A, E, G, Q, R1, R2and R4have the same meaning as defined in the description, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

  本发明涉及公式（I）（I）的MAP4K1抑制剂，其中A，E，G，Q，R1，R2和R4的含义与说明中定义的相同，涉及包含根据本发明的化合物的制药组合物和组合物，以及创新化合物的预防和治疗用途，分别用于制造用于治疗或预防疾病的制药组合物，特别是用于肿瘤性疾病，或与异常MAP4K1信号相关的其他紊乱免疫反应或其他疾病，作为唯一药物或与其他活性成分联合使用。本发明还涉及用于制造用于治疗或预防良性增生，动脉粥样硬化疾病，败血症，自身免疫性疾病，血管疾病，病毒感染，神经退行性疾病，炎症性疾病，动脉粥样硬化疾病和男性生育控制的制药组合物的使用，分别使用上述化合物制造制药组合物。
• PYRAZOLYL-CONTAINING TRICYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

  公开号：EP3699179A1

  公开（公告）日：2020-08-26

  The present invention relates to pyrazolyl-containing tricyclic derivative, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in the general formula (I), a preparation method therefor and a pharmaceutical composition containing the compound, and the use thereof as a protease such as ERK (MAPK) inhibitor in the treatment of cancers, bone diseases, inflammatory diseases, immunological diseases, nervous system diseases, metabolic diseases, respiratory diseases and heart diseases, wherein the definition of each substituent in the general formula (I) is the same as defined in the description.

  本发明涉及含吡唑的三环衍生物、其制备方法及其用途。特别是，本发明涉及通式（I）所示的化合物、其制备方法和含有该化合物的药物组合物，以及其作为ERK（MAPK）等蛋白酶抑制剂在治疗癌症、骨病、炎症性疾病、免疫性疾病、神经系统疾病、代谢性疾病、呼吸系统疾病和心脏病中的用途，其中通式（I）中各取代基的定义与说明中的定义相同。