5-chloro-2-(4-methoxyphenyl)oxazolo[5,4-b]pyridine | 1201324-13-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-chloro-2-(4-methoxyphenyl)oxazolo[5,4-b]pyridine
• 英文别名: 5-chloro-2-(4-methoxy-phenyl)-oxazolo[5,4-b]pyridine；5-chloro-2-(4-methoxyphenyl)-[1,3]oxazolo[5,4-b]pyridine
• CAS: 1201324-13-1
• 化学式: C₁₃H₉ClN₂O₂
• 分子量: 260.68
• InChiKey: TYFRVQWVBDOBLC-UHFFFAOYSA-N

物化性质

• 沸点：
  371.2±32.0 °C(Predicted)
• 密度：
  1.343±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  48.2
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  吗啉 、 5-chloro-2-(4-methoxyphenyl)oxazolo[5,4-b]pyridine 在 copper(l) iodide potassium phosphate 、 L-脯氨酸 作用下， 以 二甲基亚砜 为溶剂， 以14%的产率得到2-(4-methoxyphenyl)-5-morpholin-4-yl-[1,3]oxazolo[5,4-b]pyridine
  参考文献：
  名称：

  [EN] NOVEL SUBSTITUTED AZABENZOXAZOLES
  [FR] NOUVEAUX AZABENZOXAZOLES SUBSTITUÉS

  摘要：

  公开号：

  WO2009155017A3
• 作为产物：
  描述：

  2,6-二氯-3-氨基吡啶 在 吡啶 、 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 生成 5-chloro-2-(4-methoxyphenyl)oxazolo[5,4-b]pyridine
  参考文献：
  名称：

  [EN] NOVEL SUBSTITUTED AZABENZOXAZOLES
  [FR] NOUVEAUX AZABENZOXAZOLES SUBSTITUÉS

  摘要：

  公开号：

  WO2009155017A3

文献信息

• PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING DEGENERATIVE BRAIN DISEASE AND METHOD OF SCREENING THE SAME
  申请人：LEE Changjoon Justin

  公开号：US20130046093A1

  公开（公告）日：2013-02-21

  A pharmaceutical composition for preventing or treating a degenerative brain disease, and a method of screening a material for preventing or treating a degenerative brain disease. The method may effectively screen a prophylactic or therapeutic candidate material for preventing or treating a degenerative brain disease. A variety of degenerative brain diseases may be effectively prevented or treated using the pharmaceutical composition including a screened material for preventing or treating a degenerative brain disease.

  一种用于预防或治疗退行性脑疾病的药物组合物，以及一种筛选预防或治疗退行性脑疾病材料的方法。该方法可以有效地筛选预防或治疗退行性脑疾病的预防性或治疗性候选材料。使用该药物组合物，包括筛选用于预防或治疗退行性脑疾病的材料，可以有效预防或治疗各种退行性脑疾病。
• NOVEL SUBSTITUTED AZABENZOXAZOLES
  申请人：Barrow James C.

  公开号：US20110085985A1

  公开（公告）日：2011-04-14

  The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH;

  本发明涉及式(I)的新型淀粉样蛋白结合化合物，以及通过测量活体患者淀粉样斑块水平的变化来测量化合物效果的方法。更具体地，本发明涉及使用本发明的化合物作为正电子发射断层扫描（PET）成像中的示踪剂，以研究体内脑部淀粉样沉积物，以诊断阿尔茨海默病。因此，本发明涉及使用新型淀粉样蛋白结合化合物作为诊断工具。本发明还涉及一种测量阿尔茨海默病治疗剂临床疗效的方法。具体而言，本发明涉及新型芳基或杂芳基取代的氮杂苯并噁唑衍生物、组成物和治疗用途，以及制备这些化合物的过程，或其药学上可接受的盐、溶剂合物或体内水解酯，其中：X为O或S；A和Y独立地为N或CH。
• Substituted azabenzoxazoles
  申请人：Barrow James C.

  公开号：US08530483B2

  公开（公告）日：2013-09-10

  The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.

  本发明涉及公式（I）的新型淀粉样结合化合物以及通过测量活体患者淀粉样斑块水平的变化来测量化合物效果的方法。更具体地说，本发明涉及使用本发明中的化合物作为正电子发射断层扫描（PET）成像中的示踪剂来研究体内脑部淀粉样沉积物，以允许诊断阿尔茨海默病的方法。因此，本发明涉及将新型淀粉样结合化合物用作诊断工具。本发明还涉及测量阿尔茨海默病治疗剂临床疗效的方法。具体而言，本发明涉及新型芳基或杂环芳基取代的氮杂苯并噁唑衍生物、组成物和治疗用途以及制备这种化合物的过程，或其药学上可接受的盐、溶剂合物或体内可水解的酯。其中：X为O或S；A和Y分别为N或CH。
• Pharmaceutical compositions for preventing or treating degenerative brain disease and method of screening the same
  申请人：Korea Institute of Science and Technology

  公开号：EP2560008A2

  公开（公告）日：2013-02-20

  A pharmaceutical composition for preventing or treating a degenerative brain disease, and a method of screening a material for preventing or treating a degenerative brain disease. The method may effectively screen a prophylactic or therapeutic candidate material for preventing or treating a degenerative brain disease. A variety of degenerative brain diseases may be effectively prevented or treated using the pharmaceutical composition including a screened material for preventing or treating a degenerative brain disease.

  一种用于预防或治疗退行性脑病的药物组合物，以及一种用于预防或治疗退行性脑病的材料筛选方法。 该方法可有效筛选出预防或治疗变性脑病的候选材料。 使用包括经筛选的用于预防或治疗退行性脑病的材料的药物组合物，可有效预防或治疗各种退行性脑病。
• US8530483B2
  申请人：——

  公开号：US8530483B2

  公开（公告）日：2013-09-10