6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine | 1229205-59-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
• 英文别名: 6-(1,3-benzothiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
• CAS: 1229205-59-7
• 化学式: C₂₁H₁₇N₅O₂S
• 分子量: 403.464
• InChiKey: UCXIPBHIILDRHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  102
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  苯并噻唑-5-硼酸频哪醇酯 、 6-bromo-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine 在 四(三苯基膦)钯 sodium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 0.5h， 以70%的产率得到6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
  参考文献：
  名称：

  [EN] IMIDAZOPYRAZINE SYK INHIBITORS
  [FR] INHIBITEURS D'IMIDAZOPYRAZINE SYK

  摘要：

  本文提供了某些咪唑吡嗪化合物及其制药组合物。提供了治疗对Syk活性抑制响应的某些疾病和疾病的患者的方法，包括向这些患者施用至少一种有效减少疾病或疾病症状的化学实体的剂量。还提供了一种确定样本中Syk激酶存在或不存在的方法。

  公开号：

  WO2010068257A1

文献信息

• IMIDAZOPYRAZINE SYK INHIBITORS
  申请人：Mitchell Scott A.

  公开号：US20100222323A1

  公开（公告）日：2010-09-02

  Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供了某些咪唑吡嗪及其制药组合物。提供了治疗对Syk活性抑制有反应的某些疾病和疾病的患者的方法，包括向这些患者施用至少一种化学物质的有效量，以减少疾病或疾病的症状。还提供了一种确定样品中Syk激酶存在或不存在的方法。
• 6-(1H-indazol-6-yl)-N-{4-[2-methyl-1-(morpholin-4-yl)propan-2-yl]phenyl}imidazo[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a syk inhibitor
  申请人：Gilead Connecticut, Inc.

  公开号：US08765761B2

  公开（公告）日：2014-07-01

  An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供具有以下结构或其药学上可接受的盐的咪唑吡嗪化合物及其制药组合物。还提供了治疗对抑制Syk活性有反应的某些疾病和疾病的患者的方法，该方法包括向这些患者施用至少一种化学实体的有效量，以减少疾病或疾病的迹象或症状。还提供了一种确定样品中Syk激酶存在或不存在的方法。
• Imidazopyrizine syk inhibitors
  申请人：Gilead Connecticut, Inc.

  公开号：US08748607B2

  公开（公告）日：2014-06-10

  Certain imidazopyrazines having the structure of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供具有以下结构的某些咪唑吡嗪化合物（I）或其药学上可接受的盐，其中R1、R2、R3、R4和R5的定义如本文所述，以及它们的制药组合物。本文提供了治疗对Syk活性抑制有反应的某些疾病和障碍的患者的方法，包括向这些患者施用至少一种化学实体的有效剂量，以减少疾病或障碍的症状或体征。还提供了用于确定样品中Syk激酶的存在或不存在的方法。
• IMIDAZOPYRIZINE SYK INHIBITORS
  申请人：GILEAD CONNECTICUT, INC.

  公开号：US20130237521A1

  公开（公告）日：2013-09-12

  Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供了某些咪唑吡嗪和其药物组成物。提供了治疗对Syk活性抑制有反应的某些疾病和疾病的患者的方法，包括向这些患者施用至少一种化学物质的量，以减少疾病或疾病的症状或迹象。还提供了用于确定样品中Syk激酶的存在或缺失的方法。
• 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
  申请人：Mitchell Scott A.

  公开号：US08450321B2

  公开（公告）日：2013-05-28

  An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供了具有以下结构的咪唑吡嗪或其药学上可接受的盐，以及其制药组合物。本文提供了治疗对Syk活性抑制有反应的某些疾病和疾病的患者的方法，包括向这些患者投予至少一种化学物质的有效量，以减轻疾病或疾病的迹象或症状。还提供了用于确定样品中是否存在Syk激酶的方法。