3-[1-(4-{(R)-2-[(Cyclopropylmethyl-amino)-methyl]-pyrrolidine-1-carbonyl }-3,5-dimethyl-1H-pyrrol-2-yl)-meth-(Z)-ylidene]-5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one | 477576-47-9

• 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: 3-[1-(4-{(R)-2-[(Cyclopropylmethyl-amino)-methyl]-pyrrolidine-1-carbonyl }-3,5-dimethyl-1H-pyrrol-2-yl)-meth-(Z)-ylidene]-5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one
• 英文别名: 3-[1-(4-{(R)-2-[(Cyclopropylmethyl-amino)-methyl]-pyrrolidine-1-carbonyl}-3,5-dimethyl-1H-pyrrol-2-yl)-meth-(Z)-ylidene]-5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one；(3Z)-3-[[4-[(2R)-2-[(cyclopropylmethylamino)methyl]pyrrolidine-1-carbonyl]-3,5-dimethyl-1H-pyrrol-2-yl]methylidene]-5-[(2,6-dichlorophenyl)methylsulfonyl]-1H-indol-2-one
• CAS: 477576-47-9
• 化学式: C₃₂H₃₄Cl₂N₄O₄S
• 分子量: 641.618
• InChiKey: OQWOTWGGUHFOSD-ZPZBNPFISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  43
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  120
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  cyclopropyl-methyl-(S)-1-pyrrolidin-2-ylmethyl-amine 、 (Z)-5-[{5-(2,6-dichlorobenzylsulfonyl)-2-oxoindolin-3-ylidene}methyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid 在 EDAC 、 三乙醇胺 、 1-羟基苯并三唑 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以133 mg (71%)的产率得到3-[1-(4-{(R)-2-[(Cyclopropylmethyl-amino)-methyl]-pyrrolidine-1-carbonyl }-3,5-dimethyl-1H-pyrrol-2-yl)-meth-(Z)-ylidene]-5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one
  参考文献：
  名称：

  5-ARALKYSUFONYL-3-(PYRROL-2-YLMETHYLIDENE)-2-INDOLINONE DERIVATIVES AS KINASE INHIBITORS

  摘要：

  本发明涉及某些抑制激酶的5-烷基磺酰基-3-(吡咯-2-基甲烯基)-2-吲哚酮衍生物，特别是met激酶。还公开了包含这些化合物的药物组合物、利用包含这些化合物的药物组合物治疗激酶介导的疾病的方法，以及它们的制备方法。

  公开号：

  US20030125370A1

文献信息

• [EN] DIFFERENTIATION MODULATING AGENTS AND USES THEREFOR<br/>[FR] AGENTS DE MODULATION DE LA DIFFERENCIATION ET UTILISATIONS ASSOCIEES
  申请人：UNIV QUEENSLAND

  公开号：WO2005065686A1

  公开（公告）日：2005-07-21

  This invention discloses methods and agents for modulating the differentiation potential and/or proliferation of preadipocytes. More particularly, the present invention discloses methods and agents for modulating a fibroblast growth factor (FGF) signalling pathway, especially the FGF-1 or FGF-2 signalling pathway, for treating or preventing adiposity-related conditions including, but not limited to, obesity, lipoma and lipomatosis.

  该发明揭示了调节前脂肪细胞分化潜能和/或增殖的方法和药剂。更具体地，本发明揭示了调节成纤维细胞生长因子（FGF）信号通路的方法和药剂，特别是FGF-1或FGF-2信号通路，用于治疗或预防与脂肪相关的疾病，包括但不限于肥胖、脂肪瘤和脂肪增生。
• 5-aralkysufonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
  申请人：Sugen, Inc.

  公开号：US06599902B2

  公开（公告）日：2003-07-29

  The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.

  本发明涉及某些5-芳基磺酰基-3-(吡咯-2-基甲基亚甲基)-2-吲哚酮衍生物，其抑制激酶，特别是MET激酶。还公开了包含这些化合物的制药组合物，利用包含这些化合物的制药组合物治疗由激酶介导的疾病的方法，以及制备它们的方法。
• Differentiation modulating agents and uses therefor
  申请人：Prins Bernhard Johannes

  公开号：US20050282733A1

  公开（公告）日：2005-12-22

  The present invention is directed to methods and agents for modulating the differentiation potential and/or proliferation of preadipocytes. More particularly, the present invention discloses methods and agents for modulating a fibroblast growth factor (FGF) signaling pathway, especially the FGF-1 or FGF-2 signaling pathway, for treating or preventing adiposity-related conditions including, but not limited to, obesity, lipoma, lipomatosis, cachexia or lipodystrophy or the loss of adipose tissue in trauma or atrophic conditions.
• DIFFERENTIATION MODULATING AGENTS AND USES THEREFOR
  申请人：Prins Johannes Bernhard

  公开号：US20120059047A1

  公开（公告）日：2012-03-08

  The present invention is directed to methods and agents for modulating the differentiation potential and/or proliferation of preadipocytes. More particularly, the present invention discloses methods and agents for modulating a fibroblast growth factor (FGF) signaling pathway, especially the FGF-1 or FGF-2 signaling pathway, for treating or preventing adiposity-related conditions including, but not limited to, obesity, lipoma, lipomatosis, cachexia or lipodystrophy or the loss of adipose tissue in trauma or atrophic conditions.
• US6599902B2
  申请人：——

  公开号：US6599902B2

  公开（公告）日：2003-07-29