4-(1H-Indol-3-yl)-piperidin-1-ylamine | 1201648-31-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 4-(1H-Indol-3-yl)-piperidin-1-ylamine
• 英文别名: 4-(1H-indol-3-yl)piperidin-1-amine
• CAS: 1201648-31-8
• 化学式: C₁₃H₁₇N₃
• 分子量: 215.298
• InChiKey: ZVVCYZFVNXWPKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  45
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(1H-Indol-3-yl)-piperidin-1-ylamine 、 1-[3-(3,4,5-trifluoro-phenyl)-acryloyl]-piperidin-4-one 在 三乙酰氧基硼氢化钠 、 溶剂黄146 作用下， 以 四氢呋喃 、 1,2-二氯乙烷 为溶剂， 生成 1-{4-[4-(1H-indol-3-yl)-piperidin-1-ylamino]-piperidin-1-yl}-3-(3,4,5-trifluoro-phenyl)-propenone
  参考文献：
  名称：

  PIPERIDYL ACRYLAMIDE ANTAGONISTS OF CCR2

  摘要：

  本发明包括式I的化合物。其中：R1、R2、R3、R4、R5和X如规范中定义。该发明还包括一种治疗或改善综合征、疾病或疾病的方法，其中所述综合征、疾病或疾病是葡萄膜炎，包括急性、复发性或慢性葡萄膜炎。该发明还包括一种通过给哺乳动物施用至少一种式I化合物的治疗有效量来抑制CCR2活性的方法。

  公开号：

  US20090318498A1
• 作为产物：
  描述：

  3-(1-Nitroso-piperidin-4-yl)-1-(toluene-4-sulfonyl)-1H-indole 在 lithium aluminium tetrahydride 、 水 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 生成 4-(1H-Indol-3-yl)-piperidin-1-ylamine
  参考文献：
  名称：

  PIPERIDYL ACRYLAMIDE ANTAGONISTS OF CCR2

  摘要：

  本发明包括式I的化合物。其中：R1、R2、R3、R4、R5和X如规范中定义。该发明还包括一种治疗或改善综合征、疾病或疾病的方法，其中所述综合征、疾病或疾病是葡萄膜炎，包括急性、复发性或慢性葡萄膜炎。该发明还包括一种通过给哺乳动物施用至少一种式I化合物的治疗有效量来抑制CCR2活性的方法。

  公开号：

  US20090318498A1

文献信息

• PIPERIDYL ACRYLAMIDE ANTOGONISTS OF CCR2
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP2307363A1

  公开（公告）日：2011-04-13
• US8188287B2
  申请人：——

  公开号：US8188287B2

  公开（公告）日：2012-05-29
• [EN] PIPERIDYL ACRYLAMIDE ANTOGONISTS OF CCR2<br/>[FR] ANTAGONISTES PIPÉRIDYL-ACRYLAMIDE DE CCR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2010008761A1

  公开（公告）日：2010-01-21

  The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5 and X are as defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is uveitis, including acute, recurring or chronic uveitis. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
• [EN] PHARMACEUTICAL COMPOUND<br/>[FR] COMPOSÉ PHARMACEUTIQUE
  申请人：IOMET PHARMA LTD

  公开号：WO2015082499A2

  公开（公告）日：2015-06-11

  Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X2, X4, X10, and X11 may be the same or different and each is independently selected from C and N; X1, X3, X5, X6, X7, X8, and X9 may be the same or different and each is independently selected from C, N and O; each bond having a dotted line may independently be a double bond or a single bond, provided that valencies at each atom are maintained; the dotted lines joining X4 with the carbon atoms either side of X2 are single bonds, and are only present when X2 is absent, X3 is absent and X4 is C, and when these bonds are present the ring carbons on each side of X2 are not directly bonded to each other; each R1 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of R1 groups present is such that the valency of X1 is maintained; each R12, R13, R13', R14, R15 and R15 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valency of the ring carbon atoms is maintained; R16 may be present or absent and is selected from H and a substituted or unsubstituted organic group, provided that the number of R16 groups present is such that the valency of X2 is maintained; each R17 may be present or absent and may be the same or different and is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R17 groups present is such that the valency of X3 is maintained; each R2, R3, R4, and R5 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X6, X7, X8, and X9 are maintained; each R7, R8 and R9 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X10, X11, and X5 are maintained; and R6 is selected from H and a substituted or unsubstituted organic group, preferably H and a substituted or unsubstituted C1-C6 alkyl group; and wherein any R group may form a ring with any other R group on an adjacent and/or proximal atom.
• PIPERIDYL ACRYLAMIDE ANTAGONISTS OF CCR2
  申请人：Cai Chaozhong

  公开号：US20090318498A1

  公开（公告）日：2009-12-24

  The present invention comprises compounds of Formula I. wherein: R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is uveitis, including acute, recurring or chronic uveitis. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

  本发明包括式I的化合物。其中：R1、R2、R3、R4、R5和X如规范中定义。该发明还包括一种治疗或改善综合征、疾病或疾病的方法，其中所述综合征、疾病或疾病是葡萄膜炎，包括急性、复发性或慢性葡萄膜炎。该发明还包括一种通过给哺乳动物施用至少一种式I化合物的治疗有效量来抑制CCR2活性的方法。