5-{4-[2-(Indol-3-yl)ethoxy]benzyl}thiazolidine-2.4dione | 172647-51-7

• 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: 5-{4-[2-(Indol-3-yl)ethoxy]benzyl}thiazolidine-2.4dione
• 英文别名: 5-{4-[2-(Indol-3-yl)ethoxy]benzyl}thiazolidine-2,4-dione；5-[[4-[2-(1H-indol-3-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
• CAS: 172647-51-7
• 化学式: C₂₀H₁₈N₂O₃S
• 分子量: 366.441
• InChiKey: WTBHXADKJKKYIG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  96.5
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5-{4-[2-(indol-3-yl)ethoxy]benzyl}-3-triphenylmethylthiazolidine-2,4-dione 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 5-{4-[2-(Indol-3-yl)ethoxy]benzyl}thiazolidine-2.4dione
  参考文献：
  名称：

  Heterocyclic compounds having anti-diabetic activity and their use

  摘要：

  式(I)的化合物：##STR1## [其中：X代表未取代或取代的吲哚基、吲哚啉基、氮杂吲哚基、氮杂吲哚啉基、咪唑吡啶基或咪唑吡嘧啶基；Y代表氧原子或硫原子；Z代表2,4-二氧代噻唑啉-5-基甲基、2,4-二氧代噻唑啉-5-基甲基、2,4-二氧代噁唑啉-5-基甲基、3,5-二氧代噁二唑啉-2-基甲基或N-羟基脲基甲基；R代表氢原子、烷基、烷氧基、卤原子、羟基、硝基、芳基烷基或未取代或取代的氨基；m为1至5的整数]具有降血糖和抗糖尿病活性。

  公开号：

  US05624935A1

文献信息

• [EN] APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS<br/>[FR] INHIBITEURS DE KINASE 1 DE RÉGULATION DE SIGNAL D'APOPTOSE
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2009123986A1

  公开（公告）日：2009-10-08

  The present invention relates to apoptosis signal-regulating kinase 1 ("ASK1") inhibiting compounds of the formula (I); wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

  本发明涉及具有以下结构的凋亡信号调节激酶1（"ASK1"）抑制化合物（I）；其中变量如本文所定义。该发明还涉及包含这些化合物的药物组合物、试剂盒和制造品；用于制备这些化合物的有用中间体和方法；以及使用这些化合物的方法。
• [EN] APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS<br/>[FR] INHIBITEURS DE KINASE 1 RÉGULANT LE SIGNAL D'APOPTOSE
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2011097079A1

  公开（公告）日：2011-08-11

  The present invention relates to apoptosis signal-regulating kinase 1 ("ASK1") inhibiting compounds of the formula (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

  本发明涉及式(I)的凋亡信号调节激酶1（"ASK1"）抑制化合物，其中变量如本文所定义。该发明还涉及包括这种化合物的药物组合物、工具包和制造品；用于制备这些化合物的方法和中间体；以及使用这些化合物的方法。
• [EN] PYRAZOLO [1, 5-A] PYRIMIDINE DERIVATIVES AS APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS<br/>[FR] DÉRIVÉS PYRAZOLO [1, 5-A] PYRIMIDINES COMME INHIBITEURS DE KINASE 1 RÉGULATRICE DE SIGNAL D'APOPTOSE
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2011041293A1

  公开（公告）日：2011-04-07

  The present invention relates to apoptosis signal-regulating kinase 1 ("ASK1") inhibiting compounds of the formula (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

  本发明涉及具有以下式(I)的抑制凋亡信号调节激酶1（"ASK1"）的化合物，其中变量如本文所定义。该发明还涉及包含这些化合物的药物组合物、试剂盒和制造品；用于制备这些化合物的方法和中间体；以及使用这些化合物的方法。
• Intermediate compounds in the preparation of heterocyclic compounds
  申请人：Sankyo Company, Limited

  公开号：US05739345A1

  公开（公告）日：1998-04-14

  Compounds of formula (I): ##STR1## \x9bwherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrimidinyl group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxo-thiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethyl group; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group; and m is an integer of from 1 to 5! have hypoglycemic and anti-diabetic activities. Disclosed also are intermediate compounds for the preparation of compounds of formula I.

  式(I)的化合物：##STR1## 其中：X代表未取代或取代的吲哚基、吲哚啉基、氮杂吲哚基、氮杂吲哚啉基、咪唑吡啶基或咪唑嘧啶基；Y代表氧原子或硫原子；Z代表2,4-二氧代噻唑啉-5-亚甲基、2,4-二氧代噻唑啉-5-基甲基、2,4-二氧代噁唑啉-5-基甲基、3,5-二氧代氧杂噻唑啉-2-基甲基或N-羟基脲甲基；R代表氢原子、烷基、烷氧基、卤素原子、羟基、硝基、芳基烷基或未取代或取代的氨基；m为1至5的整数！具有降血糖和抗糖尿病活性。还公开了制备式(I)化合物的中间体化合物。
• Heterocyclic compound having anti-diabetic activity
  申请人：Sankyo Company, Limited

  公开号：US05977365A1

  公开（公告）日：1999-11-02

  Compounds of formula (I): ##STR1## [wherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrinidinyl group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxo-thiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxo-oxadiazolidin-2-ylmethyl or N-hydroxyureidom ethyl group; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group; and m is an inzeger of from 1 to 5] have hypoglycemic and anti-diabetic activities.

  式(I)的化合物：##STR1## [其中：X代表未取代或取代的吲哚基、吲哚啉基、氮杂吲哚基、氮杂吲哚啉基、咪唑吡啶基或咪唑吡啶啉基；Y代表氧原子或硫原子；Z代表2,4-二氧代噻唑啉-5-亚甲基基、2,4-二氧代噻唑啉-5-基甲基、2,4-二氧代噁唑啉-5-基甲基、3,5-二氧代氧化噻唑啉-2-基甲基或N-羟基脲基乙基基团；R代表氢原子、烷基、烷氧基、卤原子、羟基、硝基、芳基烷基或未取代或取代的氨基基团；m为1至5的整数]具有降血糖和抗糖尿病活性。