5-(5-Bromo-2-oxo-1,2-Dihydroindol-3-Ylidenemethyl)-2-Isopropyl-4-Phenyl-1H-Pyrrole-3-Carboxylic Acid (3-Pyrrolidin-1-Ylpropyl)Amide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 5-(5-Bromo-2-oxo-1,2-Dihydroindol-3-Ylidenemethyl)-2-Isopropyl-4-Phenyl-1H-Pyrrole-3-Carboxylic Acid (3-Pyrrolidin-1-Ylpropyl)Amide
• 英文别名: 5-[(Z)-(5-bromo-2-oxo-1H-indol-3-ylidene)methyl]-4-phenyl-2-propan-2-yl-N-(3-pyrrolidin-1-ylpropyl)-1H-pyrrole-3-carboxamide
• 化学式: C₃₀H₃₃BrN₄O₂
• 分子量: 561.522
• InChiKey: YDWVTTCFDHDHIH-NKFKGCMQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  37
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  77.2
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-(3-氨基丙基)吡咯烷 、 5-(5-Bromo-2-oxo-1,2-Dihydroindol-3-Ylidenemethyl)-2-Isopropyl-4-Phenyl-1H-Pyrrole-3-Carboxylic Acid 以140 mg (66%)的产率得到5-(5-Bromo-2-oxo-1,2-Dihydroindol-3-Ylidenemethyl)-2-Isopropyl-4-Phenyl-1H-Pyrrole-3-Carboxylic Acid (3-Pyrrolidin-1-Ylpropyl)Amide
  参考文献：
  名称：

  Combination therapy for the treatment of cancer

  摘要：

  本发明涉及使用蛋白酪氨酸激酶抑制剂与环氧合酶抑制剂，特别是环氧合酶-2选择性抑制剂，联合治疗或预防肿瘤性疾病的方法。

  公开号：

  US20030216410A1

文献信息

• Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
  申请人：Sugen. Inc.

  公开号：US20030100555A1

  公开（公告）日：2003-05-29

  The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

  本发明涉及吡咯替代的2-吲哚酮化合物及其药学上可接受的盐，这些化合物调节蛋白激酶的活性，因此预计在预防和治疗蛋白激酶相关的细胞疾病，如癌症方面具有用处。
• Pyrrole substituted 2-indolinone protein kinase inhibitors
  申请人：Tang Cho Peng

  公开号：US20070010569A1

  公开（公告）日：2007-01-11

  The present invention relates to pyrrole substituted-2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

  本发明涉及吡咯取代的2-吲哚酮化合物及其药学上可接受的盐，它们调节蛋白激酶的活性，因此有望在预防和治疗蛋白激酶相关的细胞疾病，如癌症方面发挥作用。
• Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates
  申请人：Riggs-Sauthier Jennifer

  公开号：US20120094998A1

  公开（公告）日：2012-04-19

  The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.

  本发明涉及寡聚体-PTK抑制剂偶联物及相关化合物（除其他事项外）。本发明的化合物在通过任何一种给药途径进行治疗时，相较于缺乏水溶性非肽寡聚体的PTK抑制剂化合物，表现出优势。
• AGENT FOR PREVENTING AND/OR TREATING AMYOTROPHIC LATERAL SCLEROSIS
  申请人：KYOTO UNIVERSITY

  公开号：US20180000771A1

  公开（公告）日：2018-01-04

  The present invention provides a prophylactic and/or therapeutic agent for amyotrophic lateral sclerosis (ALS), which contains one or more kinase inhibitors selected from the group consisting of an epithelial cell growth factor receptor (EGFR) inhibitor, a fibroblast growth factor receptor (FGFR) inhibitor, an Aurorakinase inhibitor, a protein kinase A (PKA) inhibitor, a protein kinase C (PKC) inhibitor, an MEK inhibitor, an Met inhibitor, a JNK inhibitor, a Syk inhibitor and a JAK inhibitor, a prostaglandin analogue and an estrogen receptor antagonist, or one or more kinase inhibitors selected from the group consisting of Tivozanib and an analog thereof, SB 216763, Cdk2 Inhibitor II, BUDESONIDE, RIBOFLAVIN, alpha-TOCHOPHEROL, AMODIAQUINE, SU9516, Sunitinib and an analog thereof, GSK-3 Inhibitor XIII, Bisindolylmaleimide I, HYDROQUINONE, FLUNISOLIDE, MGCD-265, Indirubin-3′-monoxime, HYDRASTINE (1R,9S), PIPERINE, BUTAMBEN, Axitinib and an analog thereof, APOMORPHINE, FENBUFEN, Bosutinib (SKI-606) and an analog thereof, a Wee1 Inhibitor, Cdk2 Inhibitor IV, NU6140, 3-hydroxybutyric acid, AT9283, Imatinib, Nilotinib, Rebastinib, and Bafetinib for the prophylaxis and/or treatment of ALS. Particularly, using a compound already on the market as a pharmaceutical product, a pharmaceutical product for the prophylaxis or treatment of ALS can be developed rapidly at a low cost.
• US7320996B2
  申请人：——

  公开号：US7320996B2

  公开（公告）日：2008-01-22