[(R)-2-(7-cyclopentylamino-5-fluoro-1H-indol-2-yl)-4,5-dihydro-thiazol-4-yl]-methanol | 1120342-66-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: [(R)-2-(7-cyclopentylamino-5-fluoro-1H-indol-2-yl)-4,5-dihydro-thiazol-4-yl]-methanol
• 英文别名: [(R)-2-(5-fluoro-7-cyclopentylamino-1H-indol-2-yl)-4,5-dihydro-thiazol-4-yl]-methanol；[(4R)-2-[7-(cyclopentylamino)-5-fluoro-1H-indol-2-yl]-4,5-dihydro-1,3-thiazol-4-yl]methanol
• CAS: 1120342-66-6
• 化学式: C₁₇H₂₀FN₃OS
• 分子量: 333.43
• InChiKey: HPDNCJPIRIPRBE-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  85.7
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  [(R)-2-(7-cyclopentylamino-5-fluoro-1H-indol-2-yl)-4,5-dihydro-thiazol-4-yl]-methanol 、 溴乙酸乙酯 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 以68%的产率得到[(R)-2-(7-cyclopentylamino-5-fluoro-1H-indol-2-yl)-4,5-dihydro-thiazol-4-ylmethoxy]-acetic acid ethyl ester
  参考文献：
  名称：

  [EN] GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
  [FR] ACTIVATEURS DE LA GLUCOKINASE ET COMPOSITIONS PHARMACEUTIQUES CONTENANT CES DERNIERS EN TANT QU'INGRÉDIENT ACTIF

  摘要：

  公开号：

  WO2009082152A3

文献信息

• INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS
  申请人：Kim Soon Ha

  公开号：US20100210647A1

  公开（公告）日：2010-08-19

  The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.

  本发明涉及新的吲哚化合物，其药学上可接受的盐或异构体，用于预防或治疗细胞坏死和坏死相关疾病。本发明还涉及一种预防或治疗细胞坏死和坏死相关疾病的方法和组合物，该组合物包括所述吲哚化合物作为活性成分。
• [EN] INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS<br/>[FR] COMPOSÉS D'INDOLE EN TANT QU'INHIBITEURS DE NÉCROSE CELLULAIRE
  申请人：LG LIFE SCIENCES LTD

  公开号：WO2009025477A1

  公开（公告）日：2009-02-26

  The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.

  本发明涉及新的吲哚化合物、药学上可接受的盐或其异构体，用于预防或治疗细胞坏死和坏死相关疾病。本发明还涉及一种预防或治疗细胞坏死和坏死相关疾病的方法和组合物，其包括所述吲哚化合物作为活性成分。
• GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
  申请人：Kim Soon Ha

  公开号：US20100267708A1

  公开（公告）日：2010-10-21

  The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.

  本发明涉及公式（1）的新化合物，表现出对葡萄糖激酶的优异活性，并且包括该化合物作为活性成分的药物组合物。
• INDOLE AND INDAZOLE DERIVATIVES HAVING A CELL-, TISSUE- AND ORGAN-PRESERVING EFFECT
  申请人：Kim Soon Ha

  公开号：US20100291533A1

  公开（公告）日：2010-11-18

  The present invention relates to a composition for preserving cells, tissues and organs, comprising as an active ingredient indole and indazole compounds of formula (1), or a pharmaceutically acceptable salt or isomer thereof, which are effective for preventing injury of organs, isolated cell systems or tissues caused by cold storage, transplant operation or post-transplantation reperfusion; a preservation method; and a preparation method of the composition.

  本发明涉及一种用于保存细胞、组织和器官的组合物，其中包括作为活性成分的式（1）的吲哚和吲唑化合物，或其药用可接受的盐或异构体，对于预防由冷藏、移植手术或移植后再灌注引起的器官、分离的细胞系统或组织的损伤具有有效性；一种保存方法；以及该组合物的制备方法。
• Glucokinase activators and pharmaceutical compositions containing the same as an active ingredient
  申请人：LG Life Sciences Ltd.

  公开号：US08309586B2

  公开（公告）日：2012-11-13

  Disclosed are new compounds of formula (1) exhibiting excellent activity for glucokinase, pharmaceutical compositions having the same as an active ingredient, and a method of using the same as an active ingredient for lowering blood glucose level: in which the substituents are as defined herein.

  本发明公开了一种具有优异葡萄糖激酶活性的新化合物，其化学式为（1），以及以该化合物为活性成分的药物组合物和使用该化合物作为活性成分降低血糖水平的方法。其中，取代基的定义如下。