2-ethyl-4-(1-methyl-1H-pyrazol-4-yl)aniline | 1449669-06-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-ethyl-4-(1-methyl-1H-pyrazol-4-yl)aniline
• 英文别名: 2-Ethyl-4-(1-methyl-1H-pyrazol-4-yl)aniline；2-ethyl-4-(1-methylpyrazol-4-yl)aniline
• CAS: 1449669-06-0
• 化学式: C₁₂H₁₅N₃
• 分子量: 201.271
• InChiKey: AZOWLGREMRBIRN-UHFFFAOYSA-N

物化性质

• 沸点：
  355.4±30.0 °C(Predicted)
• 密度：
  1.12±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-ethyl-4-(1-methyl-1H-pyrazol-4-yl)aniline 、 6-氯-1-甲基-1H-咪唑并[4,5-c]吡啶 在 tris-(dibenzylideneacetone)dipalladium(0) 、 sodium t-butanolate 、 2-二环己基磷-2,4,6-三异丙基联苯 作用下， 以 1,4-二氧六环 为溶剂， 反应 24.0h， 生成 N-(2-ethyl-4-(1-methyl-1H-pyrazol-4-yl)phenyl)-1-methyl-1H-imidazo[4,5-c]pyridin-6-amine
  参考文献：
  名称：

  [EN] IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  [FR] DÉRIVÉS D'IMIDAZO[4, 5-C]PYRIDINES UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES

  摘要：

  在此，R1、L1、R3、R4、Cy、L2和R5的定义如下。根据公式I披露了新型咪唑吡啶类化合物，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如过敏性或炎症性疾病、自身免疫疾病、增生性疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形以及与IL6或干扰素过度分泌相关的疾病。

  公开号：

  WO2013117645A1
• 作为产物：
  描述：

  4-溴-2-乙基苯胺 、 1-甲基-1H-吡唑-4-硼酸 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 caesium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 24.0h， 生成 2-ethyl-4-(1-methyl-1H-pyrazol-4-yl)aniline
  参考文献：
  名称：

  [EN] IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  [FR] DÉRIVÉS D'IMIDAZO[4, 5-C]PYRIDINES UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES

  摘要：

  在此，R1、L1、R3、R4、Cy、L2和R5的定义如下。根据公式I披露了新型咪唑吡啶类化合物，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如过敏性或炎症性疾病、自身免疫疾病、增生性疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形以及与IL6或干扰素过度分泌相关的疾病。

  公开号：

  WO2013117645A1

文献信息

• [EN] NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS PHARMACEUTIQUES LES COMPRENANT POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2017012647A1

  公开（公告）日：2017-01-26

  The present invention discloses compounds according to Formula (I), wherein R1, R3, R4, R5, L1, and Cy are as defined herein. The present invention also provides compounds, methods for the production of said compounds of the invention, pharmaceutical compositions comprising the same and their use in allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 and/or interferons. The present invention also methods for the prevention and/or treatment of the aforementioned diseases by administering a compound of the invention.

  本发明公开了根据式（I）的化合物，其中R1、R3、R4、R5、L1和Cy如本文所定义。本发明还提供了该发明的化合物、制备该化合物的方法、包括相同化合物的药物组合物以及它们在过敏或炎症症状、自身免疫疾病、增殖性疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形和/或与IL6和/或干扰素过度分泌相关的疾病中的使用。本发明还提供了通过给予该发明的化合物来预防和/或治疗上述疾病的方法。
• [EN] INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS
  申请人：CANCER REC TECH LTD

  公开号：WO2014037750A1

  公开（公告）日：2014-03-13

  The present invention relates to compounds of formula (I), wherein R, R, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

  本发明涉及式(I)的化合物，其中R、R、Ar、W、X和Z均如本文所定义。本发明的化合物已知可以通过直接或间接地与Mps1激酶本身相互作用来抑制单丝粒体1（Mps1，也称为TTK）激酶的纺锤体检查点功能。具体而言，本发明涉及将这些化合物用作治疗和/或预防增殖性疾病，如癌症的治疗剂。本发明还涉及制备这些化合物的方法，以及包含它们的药物组合物。
• NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  申请人：MENET Christel Jeanne Marie

  公开号：US20130217664A1

  公开（公告）日：2013-08-22

  Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R 1 , L 1 , R 3 , R 4 , Cy, L 2 and R 5 are as defined herein.

  公开了一种能够抑制JAK的新型咪唑吡啶化合物，其化学式为I，这些化合物可以制备成药物组合物，并可用于预防和治疗哺乳动物，包括人类的各种疾病，例如过敏或炎症性疾病、自身免疫疾病、增殖性疾病、移植排斥、涉及软骨周转障碍的疾病、先天性软骨畸形以及与IL6或干扰素过度分泌相关的疾病。其中R1、L1、R3、R4、Cy、L2和R5如本文所定义。
• INHIBITOR COMPOUNDS
  申请人：CANCER RESEARCH TECHNOLOGY

  公开号：US20150239884A1

  公开（公告）日：2015-08-27

  The present invention relates to compounds of formula I wherein R 1 , R 4 , Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

  本发明涉及式I的化合物，其中R1、R4、Ar、W、X和Z均如本文所定义。本发明的化合物已知能够直接或间接地通过与Mps1激酶本身的相互作用来抑制单纺锤体1（Mps1，也称为TTK）激酶的纺锤体检查点功能。特别地，本发明涉及使用这些化合物作为治疗和/或预防增生性疾病，如癌症的治疗剂。本发明还涉及制备这些化合物的过程，以及包含它们的药物组合物。
• Inhibitor compounds
  申请人：Cancer Research Technology Limited

  公开号：US09409907B2

  公开（公告）日：2016-08-09

  The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

  本发明涉及式I的化合物，其中R1、R4、Ar、W、X和Z的定义如本文所述。本发明的化合物已知可以直接或间接地通过与Mps1激酶本身的相互作用来抑制单纺锤体1（Mps1 - 也称为TTK）激酶的纺锤体检查点功能。特别地，本发明涉及使用这些化合物作为治疗和/或预防增生性疾病，如癌症的治疗剂。本发明还涉及制备这些化合物的过程，以及包含它们的药物组合物。