2-Amino[1,3]thiazolo[5,4-b]pyridin-5-ol dihydrobromide | 1174229-36-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-Amino[1,3]thiazolo[5,4-b]pyridin-5-ol dihydrobromide
• 英文别名: 2-amino-4H-[1,3]thiazolo[5,4-b]pyridin-5-one;dihydrobromide
• CAS: 1174229-36-7
• 化学式: C6H7Br2N3OS
• 分子量: 329.01
• InChiKey: SDGXLJXEVIAQEK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.72
• 重原子数：
  13
• 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：
  96.2
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5-甲氧基三阿咪唑 、 氢溴酸 以 溶剂黄146 为溶剂， 反应 3.0h， 以to give 2-amino[1,3]thiazolo[5,4-b]pyridin-5-ol dihydrobromide (9.11 g的产率得到2-Amino[1,3]thiazolo[5,4-b]pyridin-5-ol dihydrobromide
  参考文献：
  名称：

  Oxime derivative and preparations thereof

  摘要：

  本发明的问题是提供一种有用的化合物作为葡萄糖激酶激活剂，其为公式[I]的肟衍生物：其中，环A为芳基或杂环芳基；Q为环烷基，杂环，烷基或烯基；环T为杂环芳基或杂环；R1和R2独立地为氢原子，卤原子，环烷基磺酰基或类似物；R3和R4独立地为氢原子，羟基，氧代，卤原子或类似物；R5为氢原子，卤原子，氰基，硝基，四唑基或类似物；或其药学上可接受的盐。

  公开号：

  US07514439B2

文献信息

• Oxime Derivative and Preparations Thereof
  申请人：Sugawara Kazutoshi

  公开号：US20080132479A1

  公开（公告）日：2008-06-05

  The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R 1 and R 2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R 3 and R 4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R 5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.

  本发明的问题是提供一种有用的化合物作为葡萄糖激酶活化剂，其为式[I]的肟衍生物：其中，环A是芳基或杂芳基；Q是环烷基，杂环，烷基或烯基；环T是杂芳基或杂环；R1和R2分别是氢原子，卤素原子，环烷基磺酰基或类似物；R3和R4分别是氢原子，羟基，氧代，卤素原子或类似物；R5是氢原子，卤素原子，氰基，硝基，四唑基或类似物；或其药学上可接受的盐。
• OXIME DERIVATIVE AND PREPARATIONS THEREOF
  申请人：Sugawara Kazutoshi

  公开号：US20090291936A1

  公开（公告）日：2009-11-26

  The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R 1 and R 2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R 3 and R 4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R 5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.

  本发明的问题是提供一种有用的化合物作为葡萄糖激酶活化剂，该化合物是公式[I]的肟衍生物： 其中，环A是芳基或杂环芳基；Q是环烷基、杂环、烷基或烯基；环T是杂环芳基或杂环；R1和R2分别是氢原子、卤素原子、环烷基磺酰基或类似物；R3和R4分别是氢原子、羟基、氧代、卤素原子或类似物；R5是氢原子、卤素原子、氰基、硝基、四唑基或类似物；或其药学上可接受的盐。
• Imaging Agents Useful for Identifying AD Pathology
  申请人：Kolb Hartmuth C.

  公开号：US20100098634A1

  公开（公告）日：2010-04-22

  Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

  本文提供的化合物和组合物包含如下所述的公式，其中该化合物是一种淀粉样蛋白结合化合物。本发明的淀粉样蛋白结合化合物可以以适量的方式用于体内成像淀粉样沉积物，以区分含有淀粉样沉积物的神经组织和正常神经组织。本发明的淀粉样探针可以用于检测和定量测量包括唐氏综合症、家族性阿尔茨海默病在内的疾病中的淀粉样沉积物。在另一实施例中，这些化合物可以用于治疗或预防神经退行性疾病。本文还提供了一种使化合物分布到脑组织中并成像脑组织的方法，其中与正常结合水平相比，化合物与脑组织的结合增加表明哺乳动物正在患有或有发展神经退行性疾病的风险。
• Imaging agents useful for identifying AD pathology
  申请人：Kolb Hartmuth C.

  公开号：US08420052B2

  公开（公告）日：2013-04-16

  Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

  本文提供了包含所述配方的化合物和组合物，其中该化合物是一种淀粉样蛋白结合化合物。根据本发明，可以将淀粉样蛋白结合化合物以适当的剂量用于体内成像淀粉样沉积物，并区分带有淀粉样沉积物和正常神经组织的神经组织。本发明的淀粉样探针可用于检测和定量测定包括唐氏综合症、家族性阿尔茨海默病等疾病中的淀粉样沉积物。在另一实施方案中，这些化合物可用于治疗或预防神经退行性疾病。本文还提供了一种使化合物分布到脑组织中并成像脑组织的方法，其中与正常结合水平相比，化合物与脑组织的结合增加表明哺乳动物正在患有或有发展神经退行性疾病的风险。
• AN OXIME DERIVATIVE AND PREPARATIONS THEREOF
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1907387A1

  公开（公告）日：2008-04-09