(2-(1-(pyrimidin-2-yl)piperidin-4-yl)thiazol-4-yl)methyl methanesulfonate | 1258604-45-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (2-(1-(pyrimidin-2-yl)piperidin-4-yl)thiazol-4-yl)methyl methanesulfonate
• 英文别名: (2-(1-(Pyrimidin-2-yl)piperidin-4-yl)thiazol-4-yl)methyl methanesulfonate；[2-(1-pyrimidin-2-ylpiperidin-4-yl)-1,3-thiazol-4-yl]methyl methanesulfonate
• CAS: 1258604-45-3
• 化学式: C₁₄H₁₈N₄O₃S₂
• 分子量: 354.454
• InChiKey: PKMVTQKUTBDCIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  122
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  4-(2,2-dimethyl-1,3-dioxan-5-yl)phenol 、 (2-(1-(pyrimidin-2-yl)piperidin-4-yl)thiazol-4-yl)methyl methanesulfonate 在 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 4-((4-(2,2-dimethyl-1,3-dioxan-5-yl)phenoxy)methyl)-2-(1-(pyrimidin-2-yl)piperidin-4-yl)thiazole
  参考文献：
  名称：

  NOVEL GPR 119 AGONISTS

  摘要：

  本发明涉及一般式（I）的新型GPR 119激动剂，其药学上可接受的盐、药学上可接受的溶剂化物、对映体、立体异构体和多晶形。本发明还涉及制备本发明化合物的过程、含有该化合物的制药组合物以及使用该化合物治疗糖尿病和肥胖症的方法。本发明针对的是G蛋白偶联受体（GPCR）激动剂，其可用于治疗肥胖症、糖尿病和相关代谢性疾病。

  公开号：

  US20120122905A1

文献信息

• [EN] NOVEL GPR 119 AGONISTS<br/>[FR] NOUVEAUX AGONISTES DE GPR 119
  申请人：CADILA HEALTHCARE LTD

  公开号：WO2010146605A1

  公开（公告）日：2010-12-23

  The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.

  本发明涉及一般式（I）的新型GPR 119激动剂，其药学上可接受的盐，药学上可接受的溶剂化物，对映体，立体异构体和多形体。本发明还涉及制备本发明化合物的方法，含有该化合物的药物组合物以及使用本发明化合物治疗糖尿病和肥胖症的方法。本发明针对的是G蛋白偶联受体（GPCR）激动剂，可用于治疗肥胖症，糖尿病和相关代谢性疾病。
• GPR 119 agonists
  申请人：Pingali Harikishore

  公开号：US08772302B2

  公开（公告）日：2014-07-08

  The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.

  本发明涉及一般式（I）的新型GPR 119激动剂，其药学上可接受的盐、药学上可接受的溶剂化物、对映体、立体异构体和多晶形。本发明还涉及制备本发明化合物的过程、含有该化合物的制药组合物以及使用该化合物治疗糖尿病和肥胖症的方法。本发明针对的是G-蛋白偶联受体（GPCR）激动剂，可用于治疗肥胖症、糖尿病和相关代谢性疾病。
• 1,3,2-DIOXATHIANE-2-OXIDE DERIVATIVES AND THEIR USE AS GPR 119 AGONISTS
  申请人：Cadila Healthcare Limited

  公开号：EP2445904B1

  公开（公告）日：2013-09-11
• US8772302B2
  申请人：——

  公开号：US8772302B2

  公开（公告）日：2014-07-08
• NOVEL GPR 119 AGONISTS
  申请人：Pingali Harikishore

  公开号：US20120122905A1

  公开（公告）日：2012-05-17

  The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.

  本发明涉及一般式（I）的新型GPR 119激动剂，其药学上可接受的盐、药学上可接受的溶剂化物、对映体、立体异构体和多晶形。本发明还涉及制备本发明化合物的过程、含有该化合物的制药组合物以及使用该化合物治疗糖尿病和肥胖症的方法。本发明针对的是G蛋白偶联受体（GPCR）激动剂，其可用于治疗肥胖症、糖尿病和相关代谢性疾病。