(S)-4-((2-carbamoyl-5-chloro-3-((2-(phenoxymethyl)morpholino)sulfonyl)-1H-indol-7-yl)amino)-4-oxobutanoic acid | 1403506-16-0

• 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: (S)-4-((2-carbamoyl-5-chloro-3-((2-(phenoxymethyl)morpholino)sulfonyl)-1H-indol-7-yl)amino)-4-oxobutanoic acid
• 英文别名: (S)-4-((2-Carbamoyl-5-chloro-3-((2-(phenoxymethyl)morpholino) sulfonyl)-1H-indol-7-yl)amino)-4-oxobutanoic acid；4-[[2-carbamoyl-5-chloro-3-[(2S)-2-(phenoxymethyl)morpholin-4-yl]sulfonyl-1H-indol-7-yl]amino]-4-oxobutanoic acid
• CAS: 1403506-16-0
• 化学式: C₂₄H₂₅ClN₄O₈S
• 分子量: 565.004
• InChiKey: MQWZIZZCHCQAMA-INIZCTEOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  38
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  190
• 氢给体数：
  4
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  (S)-4-((2-carbamoyl-5-chloro-3-((2-(phenoxymethyl)morpholino)sulfonyl)-1H-indol-7-yl)amino)-4-oxobutanoic acid 、 (S)-7-amino-5-chloro-3-(2-(phenoxymethyl)morpholinosulfonyl)-1H-indole-2-carboxamide 、 3-氧杂二环[3.1.0]己烷-2,4-二酮 生成 2-((2-carbamoyl-5-chloro-3-(((S)-2-(phenoxymethyl)morpholino)sulfonyl)-1H-indol-7-yl) carbamoyl)cyclopropanecarboxylic acid
  参考文献：
  名称：

  PROCESS FOR THE PREPARATION OF MORPHOLINO SULFONYL INDOLE DERIVATIVES

  摘要：

  本发明涉及一种制备公式（I）化合物的方法，该化合物是吗啡啶磺酰基吲哚衍生物。公式（I）化合物能够抑制、调节或调节胰岛素样生长因子I受体或胰岛素受体。本发明还涉及制备公式（I）化合物的药物可接受的盐的方法。

  公开号：

  US20140046059A1
• 作为产物：
  描述：

  4-氯-2-硝基苯胺 在 N,N-二甲基甲酰胺 草酰氯 、 硫酸 、 氨 、 乙酸酐 、 铁粉 、 氯化铵 、 三乙胺 、 potassium hydroxide 作用下， 以 乙醇 、 二氯甲烷 、 水 、 异丙醇 、 甲苯 为溶剂， 反应 18.5h， 生成 (S)-4-((2-carbamoyl-5-chloro-3-((2-(phenoxymethyl)morpholino)sulfonyl)-1H-indol-7-yl)amino)-4-oxobutanoic acid
  参考文献：
  名称：

  [EN] A PROCESS FOR THE PREPARATION OF MORPHOLINO SULFONYL INDOLE DERIVATIVES
  [FR] PROCÉDÉ POUR LA PRÉPARATION DE DÉRIVÉS DE MORPHOLINOSULFONYLINDOLE

  摘要：

  本发明涉及一种制备式(I)化合物的方法，这些化合物是吗啡啶磺酰基吲哚衍生物。式(I)化合物能够抑制、调节或调控胰岛素样生长因子I受体或胰岛素受体。本发明还涉及制备式(I)化合物的药用可接受盐的方法。

  公开号：

  WO2012143874A1

文献信息

• Insulin-Like Growth Factor-1 Receptor Inhibitors
  申请人：Balachandran Sarala

  公开号：US20140045832A1

  公开（公告）日：2014-02-13

  The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.

  本发明涉及一种能够抑制、调节和/或调节胰岛素样生长因子I受体和胰岛素受体的化合物。本发明的化合物具有包含磺酰基吲哚基团的核心结构。本发明还涉及这些化合物的药学上可接受的盐、水合物和立体异构体。
• COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS INCLUDING SUBSTITUTED NAPHTHALIMIDES SUCH AS AMONAFIDE FOR THE TREATMENT OF IMMUNOLOGICAL, METABOLIC, INFECTIOUS, AND BENIGN OR NEOPLASTIC HYPERPROLIFERATIVE DISEASE CONDITIONS
  申请人：BROWN Dennis M.

  公开号：US20160067241A1

  公开（公告）日：2016-03-10

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.
• [EN] COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS INCLUDING SUBSTITUTED NAPHTHALIMIDES SUCH AS AMONAFIDE FOR THE TREATMENT OF IMMUNOLOGICAL, METABOLIC, INFECTIOUS, AND BENIGN OR NEOPLASTIC HYPERPROLIFERATIVE DISEASE CONDITIONS<br/>[FR] COMPOSITIONS ET PROCÉDÉS PERMETTANT D'AMÉLIORER LE BÉNÉFICE THÉRAPEUTIQUE DES COMPOSÉS CHIMIQUES ADMINISTRÉS DE MANIÈRE SUBOPTIMALE COMPRENANT DES NAPHTALIMIDES SUBSTITUÉS TELS QUE L'AMONAFIDE POUR LE TRAITEMENT DES MALADIES IMMUNOLOGIQUES, MÉTABOLIQUES, INFECTIEUSES ET INFECTIEUSES OU HYPERPROLIFÉRATIVES ET NÉOPLASTIQUES.
  申请人：BROWN DENNIS M

  公开号：WO2014179528A2

  公开（公告）日：2014-11-06

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.
• [EN] A PROCESS FOR THE PREPARATION OF MORPHOLINO SULFONYL INDOLE DERIVATIVES<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION DE DÉRIVÉS DE MORPHOLINOSULFONYLINDOLE
  申请人：PIRAMAL HEALTHCARE LTD

  公开号：WO2012143874A1

  公开（公告）日：2012-10-26

  The present invention relates to a process for the preparation of the compounds of formula (I) which are morpholino sulphonyl indole derivatives. The compounds of formula (I) are capable of inhibiting, modulating or regulating Insulin-Like-Growth Factor I Receptors or Insulin Receptors. The present invention also relates to the processes for preparation of the pharmaceutically acceptable salts of the compounds of formula (I).

  本发明涉及一种制备式(I)化合物的方法，这些化合物是吗啡啶磺酰基吲哚衍生物。式(I)化合物能够抑制、调节或调控胰岛素样生长因子I受体或胰岛素受体。本发明还涉及制备式(I)化合物的药用可接受盐的方法。
• PROCESS FOR THE PREPARATION OF MORPHOLINO SULFONYL INDOLE DERIVATIVES
  申请人：Mascarenhas Malcolm

  公开号：US20140046059A1

  公开（公告）日：2014-02-13

  The present invention relates to a process for the preparation of the compounds of formula (I) which are morpholino sulphonyl indole derivatives. The compounds of formula (I) are capable of inhibiting, modulating or regulating Insulin-Like-Growth Factor I Receptors or Insulin Receptors. The present invention also relates to the processes for preparation of the pharmaceutically acceptable salts of the compounds of formula (I).

  本发明涉及一种制备公式（I）化合物的方法，该化合物是吗啡啶磺酰基吲哚衍生物。公式（I）化合物能够抑制、调节或调节胰岛素样生长因子I受体或胰岛素受体。本发明还涉及制备公式（I）化合物的药物可接受的盐的方法。