(S)-2-(1,1-Dioxo-llambda*6*-thiomorpholin-4-yl)-1-methyl-ethylamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻嗪类
• 英文名称: (S)-2-(1,1-Dioxo-llambda*6*-thiomorpholin-4-yl)-1-methyl-ethylamine
• 英文别名: (2S)-1-(1,1-dioxo-1,4-thiazinan-4-yl)propan-2-amine
• 化学式: C₇H₁₆N₂O₂S
• 分子量: 192.28
• InChiKey: GDHWDXUUUBHDSN-ZETCQYMHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  71.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-amino-1-(1,1-dioxo-1λ6-thiomorpholin-4-yl)-propan-1-one 在 甲醇 、 盐酸 作用下， 以 四氢呋喃 为溶剂， 反应 66.0h， 以to give (S)-2-(1,1-Dioxo-1lambda*6*-thiomorpholin-4-yl)-1-methyl-ethylamine (4.5 g) as white solid, yield 90%的产率得到(S)-2-(1,1-Dioxo-llambda*6*-thiomorpholin-4-yl)-1-methyl-ethylamine
  参考文献：
  名称：

  Tetrazole-substituted arylamides as P2X3 and P2X2/3 antagonists

  摘要：

  公式I的化合物或其药学上可接受的盐，其中，R1是可选取代的四唑基，R2是可选取代的苯基，可选取代的吡啶基或可选取代的噻吩基，而R3、R4、R5、R6、R7和R8的定义如本文所述。还提供了使用这些化合物治疗与P2X3和/或P2X2/3受体拮抗剂相关的疾病的方法和制备这些化合物的方法。

  公开号：

  US08048905B2

文献信息

• Tetrazole-Substituted Arylamides as P2X3 and P2X2/3 Antagonists
  申请人：Dillon Michael Patrick

  公开号：US20090326220A1

  公开（公告）日：2009-12-31

  Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R 1 is optionally substituted tetrazolyl, R 2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R 3 , R 4 , R 5 and R 6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the compounds.

  化合物I的公式或其药学上可接受的盐，其中，R1是可选的取代四唑基，R2是可选的取代苯基，可选的取代吡啶基或可选的取代噻吩基，而R3、R4、R5和R6如本文所定义。还提供使用该化合物治疗与P2X3和/或P2X2/3受体拮抗剂相关的疾病的方法以及制备该化合物的方法。
• Thiazole and oxazole-substituted arylamides as P2X3 and P2X2/3 antagonists
  申请人：Dillon Michael Patrick

  公开号：US20080132494A1

  公开（公告）日：2008-06-05

  Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R 1 is a group of formula A or formula B, and X, R 2 , R 3 , R 4 , R 5 , R 6 , R a and R b are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the subject compounds.

  公式I的化合物或其药学上可接受的盐，其中R1是公式A或公式B的基团，X、R2、R3、R4、R5、R6、Ra和Rb的定义如本文所述。还提供了使用这些化合物治疗由P2X3和/或P2X2/3受体拮抗剂介导的疾病的方法以及制备这些化合物的方法。
• Triazole-substituted arylamides as P2X3 and P2X2/3 antagonists
  申请人：Roche Palo Alto LLC

  公开号：US07989637B2

  公开（公告）日：2011-08-02

  Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted triazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

  化合物I的公式：或其药学上可接受的盐，其中，R1是可选取代的三唑基，R2、R3、R4、R5、R6、R7和R8如此处所定义。还公开了使用该化合物治疗与P2X3和/或P2X2/3受体拮抗剂相关的疾病的方法以及制备该化合物的方法。
• THIADIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
  申请人：Chen Li

  公开号：US20100152203A1

  公开（公告）日：2010-06-17

  Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R 1 is optionally substituted thiadiazolyl, and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X 3 and/or a P2X 2/3 receptor antagonists and methods of making the compounds.

  本发明涉及化合物I的配方或其药学上可接受的盐，其中，R1是可选取代的噻二唑基，而R2、R3、R4、R5、R6、R7和R8如本文所定义。本发明还公开了使用该化合物治疗与P2X3和/或P2X2/3受体拮抗剂相关疾病的方法以及制备该化合物的方法。
• Thiadiazole-substituted arylamides as P2X3 and P2X2/3 antagonists
  申请人：Roche Palo Alto LLP

  公开号：US08119644B2

  公开（公告）日：2012-02-21

  Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

  公式I的化合物或其药学上可接受的盐，其中，R1是可选取代的噻二唑基，R2、R3、R4、R5、R6、R7和R8如本文所定义。还公开了使用这些化合物治疗与P2X3和/或P2X2/3受体拮抗剂相关的疾病的方法以及制备这些化合物的方法。