3-(4-羟基苯亚甲基)-5,6-二甲氧基吲哚啉-2-酮 | 269730-03-2

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 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
• 中文名称: 3-(4-羟基苯亚甲基)-5,6-二甲氧基吲哚啉-2-酮
• 中文别名: 化合物RPI-1；1,3-二氢-5,6-二甲氧基-3-[(4-羟苯基)亚甲基]-1H-吲哚-2-酮
• 英文名称: 1,3-Dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one
• 英文别名: (3Z)-3-[(4-hydroxyphenyl)methylidene]-5,6-dimethoxy-1H-indol-2-one
• CAS: 269730-03-2
• 化学式: C₁₇H₁₅NO₄
• 分子量: 297.3
• InChiKey: JGSMCYNBVCGIHC-QPEQYQDCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  67.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Compounds and Methods of Treatment
  申请人：LACKEY Karen Elizabeth

  公开号：US20080234267A1

  公开（公告）日：2008-09-25

  A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.

  本文描述了一种作为Ret酪氨酸激酶抑制剂有用的衍生物。所述发明还包括使用相同物质治疗由不当的Ret酪氨酸激酶活性介导的疾病的方法。
• [EN] INDOLINONE DERIVATIVES AS RECEPTOR TYROSINE KINASE IHIBITORS<br/>[FR] DERIVES D'INDOLINONE EN TANT QU'INHIBITEURS DE TYROSINE KINASE DE RECEPTEURS
  申请人：CELL THERAPEUTICS EUROPE SRL

  公开号：WO2005068424A1

  公开（公告）日：2005-07-28

  Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1, FGF-R3, Kit and the oncoproteins of the Ret family are involved.

  化合物（E）-1,3-二氢-5,6-二甲氧基-3-[(4-羟基苯基)亚甲基]-2H-吲哚-2-酮的新衍生物及其用于制备治疗涉及酪氨酸激酶活性蛋白Met、PDGF-R、FGF-R1、FGF-R3、Kit和Ret家族的oncoproteins的药物的用途。
• Indolinone derivatives
  申请人：Menta Ernesto

  公开号：US20050209195A1

  公开（公告）日：2005-09-22

  Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1, FGF-R3, Kit and the oncoproteins of the Ret family are involved.

  (E)-1,3-二氢-5,6-二甲氧基-3-[(4-羟基苯基)亚甲基]-2H-吲哚-2-酮的新衍生物及其用于制备治疗涉及Met、PDGF-R、FGF-R1、FGF-R3、Kit蛋白的酪氨酸激酶活性和Ret家族的致癌蛋白的肿瘤药物。
• [EN] ANTITUMOR COMPOUND AND THERAPEUTIC USES THEREOF<br/>[FR] COMPOSE ANTITUMORAL ET SES UTILISATIONS THERAPEUTIQUES
  申请人：NOVUSPHARMA SPA

  公开号：WO2004009083A1

  公开（公告）日：2004-01-29

  The use of an arylidene 2-indolinone derivative for treating tumors involving Met, PDGF-R, FGF-RI, FGF-R3 and Kit tyrosine kinases, or the oncoproteins of Ret family is disclosed. The invention also provides pharmaceutical compositions comprising laid arylidene 2-indolinone derivative as well as a kit comprising, in separate containers, said derivative and an anti-cancer or anti-tumor agent.

  本发明揭示了一种使用芳基亚甲基2-吲哚酮衍生物治疗涉及Met、PDGF-R、FGF-RI、FGF-R3和Kit酪氨酸激酶或Ret家族的癌基因蛋白的肿瘤的方法。本发明还提供包含该芳基亚甲基2-吲哚酮衍生物的药物组合物以及一个工具包，其中分别包含该衍生物和抗癌或抗肿瘤药物。
• Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors
  申请人：Array Biopharma Inc.

  公开号：US11524963B2

  公开（公告）日：2022-12-13

  Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R 1 and R 2 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

  本文提供了式 I 的化合物：及其同系物和药学上可接受的盐和溶剂，其中 R 1 和 R 2 具有说明书中给出的含义，它们是 RET 激酶的抑制剂，可用于治疗和预防可用 RET 激酶抑制剂治疗的疾病，包括 RET 相关疾病和紊乱。