(3Z)-N-[1-(4-chlorophenyl)propyl]-3-({3,5-dimethyl-4-[(2-pyrrolidin-1-ylethyl)carbamoyl]-1H-pyrrol-2-yl}methylene)-2-oxoindoline-5-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: (3Z)-N-[1-(4-chlorophenyl)propyl]-3-({3,5-dimethyl-4-[(2-pyrrolidin-1-ylethyl)carbamoyl]-1H-pyrrol-2-yl}methylene)-2-oxoindoline-5-carboxamide
• 英文别名: (3Z)-N-[1-(4-chlorophenyl)propyl]-3-[[3,5-dimethyl-4-(2-pyrrolidin-1-ylethylcarbamoyl)-1H-pyrrol-2-yl]methylidene]-2-oxo-1H-indole-5-carboxamide
• 化学式: C₃₂H₃₆ClN₅O₃
• 分子量: 574.123
• InChiKey: ZLDKZIOVVZXDET-BWAHOGKJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  41
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  106
• 氢给体数：
  4
• 氢受体数：
  4

文献信息

• [EN] INDOLINONE DERIVATIVES AS GRK5 MODULATORS<br/>[FR] UTILISATION DE DÉRIVÉS D'INDOLINONE COMME MODULATEURS DE LA GRK5
  申请人：MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V

  公开号：WO2015022437A1

  公开（公告）日：2015-02-19

  The present invention relates to benzopyrrolidone derivatives of formula (I) and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of metabolic diseases and cancer, and pharmaceutical compositions containing at least one of said benzopyrrolidone derivatives and/or pharmaceutically acceptable salts thereof. Metabolic diseases include diabetes, obesity and impaired adipogenesis. Furthermore, the present invention relates to the use of said benzoypyrrolidone derivatives as GRK5 inhibitors, thereby regulating the glucose dependent insulin production and/or release.

  本发明涉及化学式（I）的苯并吡咯酮衍生物和/或其药学上可接受的盐，这些衍生物作为药用活性剂的用途，特别是用于预防和/或治疗代谢性疾病和癌症，以及含有至少一种上述苯并吡咯酮衍生物和/或其药学上可接受的盐的药物组合物。代谢性疾病包括糖尿病、肥胖和受损的脂肪生成。此外，本发明涉及将上述苯并吡咯酮衍生物用作GRK5抑制剂，从而调节葡萄糖依赖性胰岛素的产生和/或释放。
• Indolinone derivatives as GRK5 modulators
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2837626A1

  公开（公告）日：2015-02-18

  The present invention relates to benzo-pyrrolidone derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cancer or metabolic diseases, which include diabetes, obesity and impaired adipogenesis, and pharmaceutical compositions containing at least one of said benzo-pyrrolidone derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said benzo-pyrrolidone derivatives as GRK5 inhibitors, thereby regulating the glucose dependent insulin production and/or release.

  本发明涉及苯并吡咯酮衍生物和/或其药用盐，这些衍生物作为药用活性剂的用途，特别用于预防和/或治疗癌症或代谢性疾病，包括糖尿病、肥胖和脂肪生成障碍，以及含有至少一种上述苯并吡咯酮衍生物和/或其药用盐的药物组合物。此外，本发明涉及将上述苯并吡咯酮衍生物用作GRK5抑制剂，从而调节葡萄糖依赖的胰岛素产生和/或释放。
• KINASES AS TARGETS FOR ANTI-DIABETIC THERAPY
  申请人：MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V.

  公开号：US20150079108A1

  公开（公告）日：2015-03-19

  The present invention is related to compound capable of modulating the activity and/or expression of the protein kinase GRK5, thereby enhancing the expression and/or release of insulin. The invention is further related to methods of identifying said compounds for the treatment of diseases of the carbohydrate metabolism. The invention is further related to methods of treatment of diseases of the carbohydrate metabolism, particularly diabetes mellitus type 2.
• US9458463B2
  申请人：——

  公开号：US9458463B2

  公开（公告）日：2016-10-04