5-[2-(diethylamino)ethyl]-2-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one;2-hydroxybutanedioic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 5-[2-(diethylamino)ethyl]-2-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one;2-hydroxybutanedioic acid
• 化学式: C27H33FN4O7
• 分子量: 544.6
• InChiKey: JNDRBKCNKMZANY-VSORCOHTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  39
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  163
• 氢给体数：
  5
• 氢受体数：
  9

文献信息

• Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors
  申请人：Tang Peng Cho

  公开号：US20100004239A1

  公开（公告）日：2010-01-07

  The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).

  本发明涉及Formula(I)中的吡咯[3,2-c]吡啶-4-酮-2-吲哚酮化合物及其在药学上可接受的盐，其中R1、R2、R3、R4、R5、R6、R7、R8X、Y等在说明书中有所描述。还披露了含有上述化合物的药物组合物、其制备方法和药用方法，特别是作为蛋白激酶抑制剂。Formula(I)。
• PYRROLO [3,2-C] PYRIDINE-4-ONE 2-INDOLINONE PROTEIN KINASE INHIBITORS
  申请人：TANG Peng Cho

  公开号：US20120058107A1

  公开（公告）日：2012-03-08

  The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R 1 , R2, R3, R4, R5, R6, R7, R8 X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).

  本发明涉及公式(I)中的吡咯并[3,2-c]吡啶-4-酮2-吲哚酮化合物及其药学上可接受的盐，其中R1、R2、R3、R4、R5、R6、R7、R8、X、Y具有规范中所述的含义。还公开了含有上述化合物的制药组合物、其制备方法和药物用途，特别是作为蛋白激酶抑制剂。公式(I)。
• PHARMACEUTICAL COMPOSITION COMPRISING PYRROLO-FUSED SIX-MEMBERED HETEROCYCLIC COMPOUND
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：EP3424500A1

  公开（公告）日：2019-01-09

  The present invention provides a pharmaceutical composition comprising a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt of the compound. Specifically, the invention provides a pharmaceutical composition comprising 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-met hyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof, and at least one water soluble filler. The pharmaceutical composition of the invention features rapid dissolution and good stability.

  本发明提供了一种药物组合物，其包含吡咯并六元杂环化合物或该化合物的药学上可接受的盐。具体地说，本发明提供了一种药物组合物，它包含 5-(2-二乙氨基-乙基)-2-(5-氟-2-氧代-1,2-二氢-吲哚-3-亚基-甲基)-3-甲基-1,5,6,7-四氢-吡咯并[3,2-c]吡啶-4-酮或其药学上可接受的盐，以及至少一种水溶性填料。本发明的药物组合物具有快速溶解和良好稳定性的特点。
• Method for preparing pharmaceutical composition comprising pyrrolo-fused six-membered heterocyclic compound
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：US10966964B2

  公开（公告）日：2021-04-06

  The present invention provides a method for preparing a pharmaceutical composition containing a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt thereof. Specifically, the invention provides a preparation method of a pharmaceutical composition, the method containing: mixing 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-methyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof with at least one filler, and then granulating the mixture. The pharmaceutical composition of the invention features a rapid dissolution and good stability.

  本发明提供了一种制备含有吡咯并六元杂环化合物或其药学上可接受的盐的药物组合物的方法。具体而言，本发明提供了一种药物组合物的制备方法，该方法包括：将 5-(2-二乙氨基-乙基)-2-(5-氟-2-氧代-1,2-二氢-吲哚-3-亚基甲基)-3-甲基-1,5,6,7-四氢-吡咯并[3,2-c]吡啶-4-酮或其药学上可接受的盐与至少一种填料混合，然后将混合物造粒。本发明的药物组合物具有溶解快、稳定性好的特点。
• Pharmaceutical composition comprising pyrrolo-fused six-membered heterocyclic compound
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：US10973807B2

  公开（公告）日：2021-04-13

  The present invention provides a pharmaceutical composition containing a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt of the compound. Specifically, the invention provides a pharmaceutical composition containing 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-methyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof, and at least one water soluble filler. The pharmaceutical composition of the invention features a rapid dissolution and good stability.

  本发明提供了一种含有吡咯并六元杂环化合物或该化合物的药学上可接受的盐的药物组合物。具体来说，本发明提供了一种药物组合物，含有 5-(2-二乙氨基-乙基)-2-(5-氟-2-氧代-1,2-二氢-吲哚-3-亚基-甲基)-3-甲基-1,5,6,7-四氢-吡咯并[3,2-c]吡啶-4-酮或其药学上可接受的盐，以及至少一种水溶性填料。本发明的药物组合物具有溶解快、稳定性好的特点。