1-(thiophen-3-yl)indoline-2,3-dione | 445455-57-2

• 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: 1-(thiophen-3-yl)indoline-2,3-dione
• 英文别名: 1-(3-thienyl)-1H-indole-2,3-dione；1-thiophen-3-ylindole-2,3-dione
• CAS: 445455-57-2
• 化学式: C₁₂H₇NO₂S
• 分子量: 229.259
• InChiKey: LVOWFWVRAPVYDX-UHFFFAOYSA-N

物化性质

• 沸点：
  397.5±34.0 °C(Predicted)
• 密度：
  1.467±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  65.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(thiophen-3-yl)indoline-2,3-dione 、 乙烷,三氯氟- 在 silica 作用下， 以 glacial acetic acid methyl alcohol 为溶剂， 反应 13.0h， 以giving the desired product (14 mg, 50%)的产率得到(3E)-3-[(4-METHYLPHENYL)IMINO]-1-(3-THIENYL)-1,3-DIHYDRO-2H-INDOL-2-ONE
  参考文献：
  名称：

  Use of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods

  摘要：

  本发明涉及对GALR3受体具有拮抗作用的吲哚酮衍生物。本发明提供一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明还提供了一种药物组合物，由本发明化合物的治疗有效量和药学上可接受的载体组合制成。本发明还提供了一种制备药物组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。

  公开号：

  US20040102507A1
• 作为产物：
  描述：

  3-噻吩硼酸 、 靛红 在 copper diacetate 、 sodium docusate 、 三乙胺 、 三氟乙酸 作用下， 以 水 为溶剂， 以31 %的产率得到1-(thiophen-3-yl)indoline-2,3-dione
  参考文献：
  名称：

  Cu(II) 催化缺电子 NH-杂环的“水中”N-芳基化

  摘要：

  描述了室温下“水中” Cu( II ) 催化的缺电子 NH 杂环的N芳基化反应。NH 杂环加芳基硼酸的结构和电子变化的底物范围很宽，从而实现了产品的多样性。官能团耐受性、“克级”合成、N-芳基化产物的合成精制和后期芳基化是其独特的优势。

  DOI：

  10.1039/d3gc05163c

文献信息

• Use of GAL3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
  申请人：——

  公开号：US20030078271A1

  公开（公告）日：2003-04-24

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

  这项发明涉及嘧啶和吲哚酮衍生物，它们是选择性GAL3受体拮抗剂。该发明提供了一种包含该发明化合物的治疗有效量和药用载体的药物组合物。该发明还提供了通过结合该发明化合物的治疗有效量和药用载体制备的药物组合物。该发明进一步提供了一种制备药物组合物的方法，包括结合该发明化合物的治疗有效量和药用载体。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者施用足以治疗受试者抑郁症和/或焦虑症的该发明化合物的量。该发明还提供了一种治疗受试者抑郁症和/或焦虑症的方法，包括向受试者施用包含药用载体和治疗有效量GAL3受体拮抗剂的组合物。
• GAL3 antagonists for the treatment of neuropathic pain
  申请人：——

  公开号：US20040092570A1

  公开（公告）日：2004-05-13

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor and are useful for the treatment of neuropathic pain and other abnormalities. This invention also provides a method of treating a subject suffering from an abnormality which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's abnormality. This invention also provides a method of treating an abnormality in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

  这项发明涉及嘧啶和吲哚酮衍生物，它们是选择性的GAL3受体拮抗剂，可用于治疗神经病痛和其他异常。这项发明还提供了一种治疗患有异常的受试者的方法，包括向受试者投予本发明中的化合物的有效剂量以治疗受试者的异常。这项发明还提供了一种治疗受试者异常的方法，包括向受试者投予包含药用载体和治疗有效量的GAL3受体拮抗剂的组合物。
• Indolone compounds useful to treat cognitive impairment
  申请人：Blackburn P. Thomas

  公开号：US20070135509A1

  公开（公告）日：2007-06-14

  This invention provides a method of treating a subject suffering from a cognitive impairment or a cognitive disorder which comprises administering to the subject an amount of an indolone compound effective to treat the subject's cognitive impairment or disorder.

  这项发明提供了一种治疗患有认知障碍或认知障碍的受试者的方法，包括向受试者施用一定量的吲哚酮化合物，以有效治疗受试者的认知障碍或障碍。
• Indolone Compounds Useful To Treat Cognitive Impairment
  申请人：Blackburn P. Thomas

  公开号：US20070135510A1

  公开（公告）日：2007-06-14

  This invention provides a method of treating a subject suffering from a cognitive impairment or a cognitive disorder which comprises administering to the subject an amount of an indolone compound effective to treat the subject's cognitive impairment or disorder.

  该发明提供了一种治疗患认知障碍或认知障碍的受试者的方法，包括向受试者施用有效治疗受试者认知障碍或障碍的吲哚酮化合物的剂量。
• GAL3 receptor antagonists for the treatment of affective disorders
  申请人：——

  公开号：US20040110821A1

  公开（公告）日：2004-06-10

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. This invention provides a method of treating a subject suffering from an affective disorder which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's affective disorder. This invention also provides a method of treating an affective disorder in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

  这项发明涉及选择性拮抗剂对GAL3受体的嘧啶和吲哚酮衍生物。该发明提供了一种治疗患有情感障碍的受试者的方法，包括向受试者施用一定量的该发明化合物，以有效治疗受试者的情感障碍。该发明还提供了一种治疗受试者情感障碍的方法，包括向受试者施用包含药用可接受载体和治疗有效量GAL3受体拮抗剂的组合物。该发明进一步提供了一种制备药物组合物的方法，包括结合该发明化合物的治疗有效量和药用可接受载体。