(S,Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-N-(2-hydroxy-3-morpholinopropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide

• 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,Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-N-(2-hydroxy-3-morpholinopropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
• 英文别名: 5-[(E)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
• 化学式: C₂₃H₂₇FN₄O₄
• 分子量: 442.5
• InChiKey: CTNPALGJUAXMMC-HKJBKDEOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  107
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Treatment of acute myeloid leukemia with indolinone compounds
  申请人：SUGEN, Inc.

  公开号：US20030130280A1

  公开（公告）日：2003-07-10

  A method of treating acute myeloid leukemia in patient positive for FLT-3-ITD is described. The treatment is accomplished by administration of a compound of Formula I or II as defined herein.

  描述了一种治疗FLT-3-ITD阳性患者急性髓系白血病的方法。该治疗通过给予本文中定义的I或II式化合物来实现。
• METHOD FOR ASSAY ON THE EFFECT OF VASCULARIZATION INHIBITOR
  申请人：Uenaka Toshimitsu

  公开号：US20100092490A1

  公开（公告）日：2010-04-15

  The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.

  本发明提供了一种预测抗血管生成抑制剂的抗肿瘤效果的方法。通过评估肿瘤细胞对表皮生长因子（EGF）增殖和/或存活的依赖性，并将其作为指标，可以预测抗血管生成抑制剂的抗肿瘤效果。由于抗血管生成抑制剂的抗肿瘤效果与肿瘤细胞对EGF增殖和/或存活的依赖性相关，因此当与具有EGF抑制活性的物质结合时，抗血管生成抑制剂能够产生出色的抗肿瘤效果。
• [EN] SALTS AND POLYMORPHS OF A PYRROLE-SUBSTITUTED INDOLINONE COMPOUND<br/>[FR] SELS ET POLYMORPHES D'UN COMPOSE D'INDOLINONE A SUBSTITUTION PYRROLIQUE
  申请人：PHARMACIA & UPJOHN CO LLC

  公开号：WO2005033098A1

  公开（公告）日：2005-04-14

  The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H--indol-3-ylidene)methyl]-N-[(2)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1 H-pyrrole-3--yarboxamide,shown in structural formula (1) such as maleate salts, and to crystalline polymorphs of these salts. The invention further relates to pharmaceutical compositions of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3--ylidene)methyl]-N-[(2S)-2-hyd carboxamide salts, and meth roxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1 H-pyrrole-3- ds of treating disorders such as cancer using such compositions.

  本发明涉及5-[(Z)-(5-氟-2-氧-1,2-二氢-3H-吲哚-3-基甲基)]-N-[(2S)-2-羟基-3-吗啡啶-4-基丙基]-2,4-二甲基-1H-吡咯-3-羧酰胺的非吸湿性盐，例如马来酸盐，并涉及这些盐的晶型多态。本发明还涉及5-[(Z)-(5-氟-2-氧-1,2-二氢-3H-吲哚-3-基甲基)]-N-[(2S)-2-羟基-3-吗啡啶-4-基丙基]-2,4-二甲基-1H-吡咯-3-羧酰胺盐和甲氧基-3-吗啡啶-4-基丙基]-2,4-二甲基-1H-吡咯-3-羧酰胺盐的制药组合物，以及使用这些组合物治疗癌症等疾病的方法。
• Process for preparing indolinone derivatives
  申请人：Jin Qingwu

  公开号：US20050171357A1

  公开（公告）日：2005-08-04

  The present invention refers to a process for preparing indolinone derivatives of the general formula (VI) as defined in the specification and intermediates of that process.

  本发明涉及一种制备通式（VI）所定义的吲哚酮衍生物及其中间体的过程。
• Combination administration of an indolinone with a chemotherapeutic agent for cell proliferation disorders
  申请人：SUGEN, Inc.

  公开号：US20040152759A1

  公开（公告）日：2004-08-05

  The invention relates to a method of treating cancer by administering a combination of an indolinone compound with another chemotherapeutic agent. The combination of an indolinone compound of Formula I: 1 with another chemotherapeutic agent provides an enhanced effect in treating cancer patients.

  本发明涉及一种治疗癌症的方法，通过给予一种吲哚酮化合物和另一种化疗药物的组合物。一种式子为I：1的吲哚酮化合物与另一种化疗药物的组合物在治疗癌症患者方面提供了增强效果。