7-溴-1H-吲哚-5-胺 | 196205-07-9

• 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
• 中文名称: 7-溴-1H-吲哚-5-胺
• 英文名称: 7-bromo-1H-indol-5-amine
• 英文别名: 5-Amino-7-bromo-1H-indole
• CAS: 196205-07-9
• 化学式: C₈H₇BrN₂
• 分子量: 211.061
• InChiKey: IDSDTLAEQBFCMV-UHFFFAOYSA-N

物化性质

• 沸点：
  405.6±25.0 °C(Predicted)
• 密度：
  1.753±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  41.8
• 氢给体数：
  2
• 氢受体数：
  1

安全信息

• 危险等级：
  IRRITANT
• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  7-溴-1H-吲哚-5-胺 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 、 potassium acetate 、 三乙胺 作用下， 以 1,4-二氧六环 、 乙醇 为溶剂， 反应 2.0h， 生成 2-[7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indol-5-yl]-4-(trifluoromethyl)-3H-isoindol-1-one
  参考文献：
  名称：

  [EN] CBL-B MODULATORS AND USES THEREOF
  [FR] MODULATEURS DE CBL-B ET LEURS UTILISATIONS

  摘要：

  本发明提供了化合物、其组合物以及使用它们的方法，用于抑制Cbl-b和治疗Cbl-b介导的疾病。

  公开号：

  WO2022217276A1
• 作为产物：
  描述：

  7-溴-5-硝基-1H-吲哚 在 锌 碳酸氢钠 、 Sodium sulfate-III 、 乙酸乙酯 、 正己烷 作用下， 以 溶剂黄146 为溶剂， 反应 2.0h， 以afforded 153 mg of the title compound的产率得到7-溴-1H-吲哚-5-胺
  参考文献：
  名称：

  Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists

  摘要：

  本发明涉及由结构式I表示的某些新化合物：##STR1##或其药学上可接受的盐，其中R.sup.3，R.sup.6，R.sup.7，R.sup.8，R.sup.11，R.sup.12，R.sup.13，A，m，n和虚线在此定义。本发明还涉及包含这些新化合物作为活性成分的制药配方以及新化合物及其配方在治疗某些疾病中的使用。本发明的化合物是缩短肽受体拮抗剂，可用于治疗炎症性疾病、疼痛或偏头痛、哮喘和呕吐。

  公开号：

  US05929094A1

文献信息

• 5- and 6-(2-imidazolin-2-ylamino) and
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US05677321A1

  公开（公告）日：1997-10-14

  This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  这项发明涉及选择性作用于克隆人类α2受体的吲哚和苯并噻唑化合物。该发明还涉及这些化合物在任何需要使用α2激动剂的适应症中的用途。具体包括用作镇痛剂、镇静剂和麻醉剂。此外，该发明包括使用这些化合物降低眼内压、治疗老花眼、偏头痛、高血压、酒精戒断、药物成瘾、类风湿性关节炎、缺血性疼痛、痉挛、腹泻、鼻塞、尿失禁，以及用作认知增强剂和眼部血管收缩剂。该发明还提供一种包含上述定义化合物的治疗有效量和药用可接受载体的药物组合物。
• Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists
  申请人：Merck & Co., Inc.

  公开号：US05929094A1

  公开（公告）日：1999-07-27

  The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.

  本发明涉及由结构式I表示的某些新化合物：##STR1##或其药学上可接受的盐，其中R.sup.3、R.sup.6、R.sup.7、R.sup.8、R.sup.11、R.sup.12、R.sup.13、A、m、n和虚线在此处定义。本发明还涉及包含这些新化合物作为活性成分的药物配方，以及在治疗某些疾病中使用这些新化合物及其配方。本发明的化合物是催吐肽受体拮抗剂，可用于治疗炎症性疾病、疼痛或偏头痛、哮喘和呕吐。
• Novel indole and benzothiazole derivatives
  申请人：SYNAPTIC PHARMACEUTICAL CORPORATION

  公开号：US20020049239A1

  公开（公告）日：2002-04-25

  This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  本发明涉及新型的吲哚和苯并噻唑化合物，这些化合物对克隆的人类α2受体具有选择性。本发明还涉及这些化合物在任何需要使用α2激动剂的适应症中的用途。具体包括用作镇痛剂、镇静剂和麻醉剂。此外，本发明还包括使用这些化合物降低眼内压、治疗老视、偏头痛、高血压、酒精戒断、药物成瘾、类风湿性关节炎、缺血性疼痛、痉挛、腹泻、鼻塞、尿失禁以及用作认知增强剂和眼部血管收缩剂。本发明还提供了一种药物组合物，其中包括上述定义的化合物的治疗有效量和药学可接受的载体。
• Benzimidazoles and benzothiazoles and uses thereof
  申请人：SYNAPTIC PHARMACEUTICAL CORPORATION

  公开号：US20030105147A1

  公开（公告）日：2003-06-05

  This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  本发明涉及一种新型的吲哚和苯并噻唑化合物，其对克隆人类α2受体具有选择性。本发明还涉及使用这些化合物的用途，适用于任何需要使用α2激动剂的情况。具体来说，这包括用作镇痛剂、镇静剂和麻醉剂。此外，本发明还包括使用这些化合物降低眼压、老视、治疗偏头痛、高血压、酒精戒断、药物成瘾、类风湿性关节炎、缺血性疼痛、痉挛、腹泻、鼻塞、尿失禁以及用作认知增强剂和眼部血管收缩剂。本发明还提供了一种包含上述定义化合物的治疗有效量和药学上可接受的载体的药物组合物。
• Substituted indoles and uses thereof
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US06040451A1

  公开（公告）日：2000-03-21

  This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  本发明涉及一种新型的吲哚和苯并噻唑化合物，其对克隆的人类α2受体具有选择性。本发明还涉及这些化合物在任何需要使用α2激动剂的适应症中的用途。具体包括用作镇痛剂、镇静剂和麻醉剂。此外，本发明还包括使用这些化合物降低眼压、治疗老视眼、偏头痛、高血压、酒精戒断、药物成瘾、类风湿性关节炎、缺血性疼痛、痉挛、腹泻、鼻塞和尿失禁，以及用作认知增强剂和眼部血管收缩剂。本发明还提供一种药物组合物，其中包括上述定义的化合物的治疗有效量和药学上可接受的载体。