5-溴-8-甲氧基异喹啉 | 679433-91-1

• 物质功能分类: 医药中间体 - 杂环化合物 - 异喹啉类化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 中文名称: 5-溴-8-甲氧基异喹啉
• 英文名称: 5-bromo-8-methoxyisoquinoline
• CAS: 679433-91-1
• 化学式: C₁₀H₈BrNO
• 分子量: 238.084
• InChiKey: JBWGLXQEEJHTHI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  5-溴-8-甲氧基异喹啉 在 正丁基锂 、 lithium diisopropyl amide 作用下， 以 四氢呋喃 为溶剂， 生成 α-(5-bromo-1,3-benzodioxol-4-yl)-8-methoxy-5-isoquinolinemethanol
  参考文献：
  名称：

  Synthesis and SAR exploration of dinapsoline analogues

  摘要：

  Dinapsoline is a full D-1 dopamine receptor agonist that produces robust otational activity in the unilateral 6-OHDA rat model. This compound is orally active, and shows a low tendency to cause tolerance in rat models. The active enantiomer was determined to have the S-(+) configuration, and the opposite enantiomer is essentially devoid of biological activity. Taken together, dinapsoline has significant metabolic and pharmacological advantages over previous D-1 agonists. In an attempt to define the structure-activity relationships (SARs) and to map out the key elements surrounding the unique structure of dinapsoline, core analogues and substitution analogues of the parent tetracyclic condensed ring structure were prepared. Based on a recently developed synthesis of dinapsoline and its enantiomers, both core and substitution analogues on all four rings (A, B, C and D ring) of dinapsoline were synthesized. It was found that affinity for both D-1 and D-2 receptors was decreased by most substituents on the A, B', and C rings, whereas D ring substitutions preserved much of the dopamine receptor binding activity. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2003.11.015
• 作为产物：
  描述：

  5-溴-2-甲氧基苯甲醛 在 氯甲酸乙酯 、 亚磷酸三乙酯 作用下， 以 氯仿 、 甲苯 为溶剂， 反应 32.0h， 生成 5-溴-8-甲氧基异喹啉
  参考文献：
  名称：

  [EN] 1,3-SUBSTITUTED CYCLOBUTYL DERIVATIVES AND USES THEREOF
  [FR] DÉRIVÉS DE CYCLOBUTYLE 1,3-SUBSTITUÉS ET LEURS UTILISATIONS

  摘要：

  本文提供了化合物和药物组合物，用于治疗由TRPV1受体介导的疾病或疾病。本发明还提供了通过向需要治疗的受体施用公式（I）的化合物或本文所述的药物组合物的治疗方法，用于治疗眼部疾病或疾病的方法。 (I)

  公开号：

  WO2022201097A1

文献信息

• Bis-aryl kinase inhibitors and method
  申请人：Kim Tae-Seong

  公开号：US20070054903A1

  公开（公告）日：2007-03-08

  Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  所选化合物对于预防和治疗疾病，如HGF介导的疾病具有有效性。该发明涵盖了新颖的化合物、类似物、前药和其药学上可接受的盐、制药组合物以及预防和治疗涉及癌症等疾病和其他病症或情况的方法。该发明还涉及制造这种化合物的过程以及在这些过程中有用的中间体。
• [EN] 1,3-SUBSTITUTED CYCLOBUTYL DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE CYCLOBUTYLE 1,3-SUBSTITUÉS ET LEURS UTILISATIONS
  申请人：NOVARTIS AG

  公开号：WO2022201097A1

  公开（公告）日：2022-09-29

  Provided herein are compounds and pharmaceutical compositions useful for treating diseases or disorders mediated by the TRPV1 receptor. The present invention also provides methods for treating ocular diseases or disorders by administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) or a pharmaceutical composition described herein. (I)

  本文提供了化合物和药物组合物，用于治疗由TRPV1受体介导的疾病或疾病。本发明还提供了通过向需要治疗的受体施用公式（I）的化合物或本文所述的药物组合物的治疗方法，用于治疗眼部疾病或疾病的方法。 (I)
• WO2007/5668
  申请人：——

  公开号：——

  公开（公告）日：——
• BIS-ARYL KINASE INHIBITORS AND THEIR USE IN THE TREATMENT OF INFLAMMATION, ANGIOGENESIS AND CANCER
  申请人：Amgen Inc.

  公开号：EP1896461A2

  公开（公告）日：2008-03-12
• INHIBITORS OF SARM1 IN COMBINATION WITH NEURO-PROTECTIVE AGENTS
  申请人：Disarm Therapeutics, Inc.

  公开号：US20220008405A1

  公开（公告）日：2022-01-13

  The present disclosure relates to methods of treating neurodegeneration and neurodegenerative diseases comprising administering to a subject in need thereof a combination of a SARM1 inhibitor and a neuroprotective agent.