N-(4-amino-3-methoxybenzyl)acetamide | 705256-58-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: N-(4-amino-3-methoxybenzyl)acetamide
• 英文别名: N-[(4-amino-3-methoxyphenyl)methyl]acetamide
• CAS: 705256-58-2
• 化学式: C₁₀H₁₄N₂O₂
• 分子量: 194.233
• InChiKey: CFVKTNXMYZXRQC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  64.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-(4-amino-3-methoxybenzyl)acetamide 、 溴乙酸甲酯 在 N,N-二异丙基乙胺 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 生成 methyl N-{4-[(acetylamino)methyl]-2-methoxyphenyl}glycinate
  参考文献：
  名称：

  [EN] 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXIDE DERIVATIVES AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE PTP1B
  [FR] DERIVES DE 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXYDE UTILISES EN TANT QU'INHIBITEURS DE LA PROTEINE TYROSINE PHOSPHATASE PTP1B

  摘要：

  该发明涉及式(I)的化合物或其在药学上可接受的盐中，其中R1、R2、R3、R4和R5具有描述中定义的任何含义。还描述了制备式(I)化合物的方法、含有它们的组合物、它们作为蛋白酪氨酸磷酸酶PTP1B抑制剂的用途以及它们用于治疗糖尿病的用途。

  公开号：

  WO2004050646A1
• 作为产物：
  描述：

  N-(3-methoxy-4-nitrobenzyl)acetamide 在 palladium 10% on activated carbon 氢气 作用下， 以 乙醇 为溶剂， 反应 2.0h， 生成 N-(4-amino-3-methoxybenzyl)acetamide
  参考文献：
  名称：

  [EN] 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXIDE DERIVATIVES AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE PTP1B
  [FR] DERIVES DE 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXYDE UTILISES EN TANT QU'INHIBITEURS DE LA PROTEINE TYROSINE PHOSPHATASE PTP1B

  摘要：

  该发明涉及式(I)的化合物或其在药学上可接受的盐中，其中R1、R2、R3、R4和R5具有描述中定义的任何含义。还描述了制备式(I)化合物的方法、含有它们的组合物、它们作为蛋白酪氨酸磷酸酶PTP1B抑制剂的用途以及它们用于治疗糖尿病的用途。

  公开号：

  WO2004050646A1

文献信息

• [EN] NEW SUBSTITUTED AZAINDOLINE DERIVATIVES AS NIK INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS D'AZAINDOLINE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE NIK
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2019008011A1

  公开（公告）日：2019-01-10

  The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

  本发明涉及对哺乳动物治疗和/或预防有用的药物，特别是对NF-κB诱导激酶（NIK - 也称为MAP3K14）的抑制剂，用于治疗癌症、炎症性疾病、代谢性疾病和自身免疫性疾病。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物或药物组合物预防或治疗癌症、炎症性疾病、包括肥胖和糖尿病在内的代谢性疾病，以及自身免疫性疾病。
• Substituted azaindoline derivatives as NIK inhibitors
  申请人：Janssen Pharmaceutica NV

  公开号：US11236084B2

  公开（公告）日：2022-02-01

  The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

  本发明涉及可用于哺乳动物治疗和/或预防的药物制剂，尤其涉及可用于治疗癌症、炎症性疾病、代谢性疾病和自身免疫性疾病等疾病的NF-κB诱导激酶（NIK-又称MAP3K14）抑制剂。本发明还涉及包含此类化合物的药物组合物，以及使用此类化合物或药物组合物预防或治疗癌症、炎症性疾病、代谢紊乱（包括肥胖和糖尿病）和自身免疫性疾病等疾病。
• SUBSTITUTED AZAINDOLINE DERIVATIVES AS NIK INHIBITORS
  申请人：Janssen Pharmaceutica NV

  公开号：EP3649127B1

  公开（公告）日：2021-09-08
• NEW SUBSTITUTED AZAINDOLINE DERIVATIVES AS NIK INHIBITORS
  申请人：Janssen Pharmaceutica NV

  公开号：US20210188840A1

  公开（公告）日：2021-06-24

  The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoinmmune disorders.
• [EN] 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXIDE DERIVATIVES AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE PTP1B<br/>[FR] DERIVES DE 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXYDE UTILISES EN TANT QU'INHIBITEURS DE LA PROTEINE TYROSINE PHOSPHATASE PTP1B
  申请人：ASTRAZENECA AB

  公开号：WO2004050646A1

  公开（公告）日：2004-06-17

  The invention concerns compounds of the formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, and R5 have any of the meanings defined in the description.Processes for the manufacture of compounds of formula (I), compositions containing them, their use as inhibitors of protein tyrosine phosphatase PTP1B and their use for the treatment of diabetes mellitus are also described.

  该发明涉及式(I)的化合物或其在药学上可接受的盐中，其中R1、R2、R3、R4和R5具有描述中定义的任何含义。还描述了制备式(I)化合物的方法、含有它们的组合物、它们作为蛋白酪氨酸磷酸酶PTP1B抑制剂的用途以及它们用于治疗糖尿病的用途。