3-(4-aminophenyl)-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-2-amine | 1449301-27-2

• 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: 3-(4-aminophenyl)-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-2-amine
• 英文别名: 3-(4-Aminophenyl)-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-2-amine；3-(4-aminophenyl)-5-[4-[[(2R)-1,4-dioxan-2-yl]methoxy]-3-methoxyphenyl]pyridin-2-amine
• CAS: 1449301-27-2
• 化学式: C₂₃H₂₅N₃O₄
• 分子量: 407.469
• InChiKey: XQFAQBFIIPTPQF-LJQANCHMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  3-(4-aminophenyl)-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-2-amine 、 5-(4-methylphenyl)-4-oxo-1-(tetrahydro-2H-pyran-4-ylmethyl)-1,4-dihydropyridine-3-carboxylic acid 在 (1-cyano-2-ethoxy-2-oxoethylidenaminooxy)dimethylaminomorpholinocarbenium hexafluorophosphate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.5h， 以69.8%的产率得到N-[4-(2-amino-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-3-yl)phenyl]-5-(4-methylphenyl)-4-oxo-1-(tetrahydro-2H-pyran-4-ylmethyl)-1,4-dihydropyridine-3-carboxamide
  参考文献：
  名称：

  PYRIDONE DERIVATIVE HAVING TETRAHYDROPYRANYLMETHYL GROUP

  摘要：

  本公开提供了新颖的化合物或其盐，或者该化合物或盐的晶体，其抑制Axl并在治疗由Axl高功能引起的疾病、与Axl高功能相关的疾病的治疗和/或涉及Axl高功能的疾病的治疗中有用。本公开提供了具有以下式（I）所代表的四氢吡喃基甲基基团的吡啶酮衍生物，具有各种取代基，或其盐，或化合物或盐的晶体，其中R1、R2、R3、R4、R5、W、X、Y和Z均如规范中定义的。

  公开号：

  US20170183329A1
• 作为产物：
  描述：

  4-羟基-3-甲氧硼酸频哪醇酯 在 四(三苯基膦)钯 、 potassium carbonate 作用下， 以 1,4-二氧六环 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 18.0h， 生成 3-(4-aminophenyl)-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-2-amine
  参考文献：
  名称：

  Pyridone Derivatives

  摘要：

  提供了抑制Axl并用于治疗由Axl高功能引起的疾病、与Axl高功能相关的疾病和/或伴随Axl高功能的疾病的新型化合物或其盐，或其晶体。提供了由式（1）所代表的吡啶酮衍生物，具有各种取代基或其盐，或其晶体（其中式（1）中的R1、R2、R3、R5、R6、A、W、X和n分别如规范中定义）。

  公开号：

  US20130281428A1

文献信息

• Pyridone derivatives
  申请人：Daiichi Sankyo Company, Limited

  公开号：US08933103B2

  公开（公告）日：2015-01-13

  Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.

  提供了抑制Axl并用于治疗由Axl高功能引起的疾病，与Axl高功能相关的疾病和/或伴随Axl高功能的疾病的新型化合物或其盐或晶体。提供了具有各种取代基的式（1）所代表的吡啶酮衍生物或其盐或晶体（其中式（1）中的R1、R2、R3、R5、R6、A、W、X和n在规范中分别定义）。
• PYRIDONE DERIVATIVE HAVING TETRAHYDROPYRANYL METHYL GROUP
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3168219A1

  公开（公告）日：2017-05-17

  It is intended to provide a novel compound or a salt thereof, or crystals of the compound or the salt, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. [Solution] The present invention provides a pyridone derivative having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or a salt thereof, or crystals of the compound or the salt (wherein R1, R2, R3, R4, R5, W, X, Y, and Z are each as defined in the specification).

  本发明旨在提供一种新型化合物或其盐，或该化合物或其盐的结晶，该化合物或其盐可抑制 Axl，并可用于治疗由 Axl 功能亢进引起的疾病、治疗与 Axl 功能亢进相关的疾病和/或治疗涉及 Axl 功能亢进的疾病。 [解决方案］ 本发明提供一种吡啶酮衍生物，该衍生物具有下式（I）所代表的具有各种取代基的四氢吡喃甲基，或其盐，或该化合物或该盐的结晶（其中R1、R2、R3、R4、R5、W、X、Y和Z各自如说明书中所定义）。
• Pyridone derivatives having tetrahydropyranylmethyl groups
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US10442797B2

  公开（公告）日：2019-10-15

  The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R1, R2, R3, R4, R5, W, X, Y, and Z are each as defined in the specification:

  本公开提供了新型化合物或其盐，或化合物或其盐的结晶，它们抑制Axl，可用于治疗由Axl功能亢进引起的疾病、治疗与Axl功能亢进相关的疾病和/或治疗涉及Axl功能亢进的疾病。 本公开提供了具有下式(I)所代表的具有各种取代基的四氢吡喃甲基的吡啶酮衍生物，或其盐，或化合物或其盐的结晶，其中R1、R2、R3、R4、R5、W、X、Y和Z各自如说明书中所定义：
• PYRIDONE DERIVATIVE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2810937B1

  公开（公告）日：2016-11-30
• PYRIDONE DERIVATIVES HAVING TETRAHYDROPYRANYLMETHYL GROUPS
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US20180148436A2

  公开（公告）日：2018-05-31

  The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Z are each as defined in the specification: