1-(5-oxo-1,2,3,9b-tetrahydropyrrolo[2,1-a]isoindol-9-yl)-3-(5-pyrrolidin-2-yl-1H-pyrazol-3-yl)urea

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 1-(5-oxo-1,2,3,9b-tetrahydropyrrolo[2,1-a]isoindol-9-yl)-3-(5-pyrrolidin-2-yl-1H-pyrazol-3-yl)urea
• 化学式: C₁₉H₂₂N₆O₂
• 分子量: 366.4
• InChiKey: IWOOJEZSDPRYAZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  102
• 氢给体数：
  4
• 氢受体数：
  4

文献信息

• [EN] PROTECTION OF RENAL TISSUES FROM SCHEMA THROUGH INHIBITION OF THE PROLIFERATIVE KISSES CDK4 AND CDK6<br/>[FR] PROTECTION DES TISSUS RÉNAUX CONTRE L'ISCHÉMIE PAR LE BIAIS DE L'INHIBITION DES KINASES PROLIFÉRATIVES CDK4 ET CDK6
  申请人：UNIV NORTH CAROLINA

  公开号：WO2012068381A2

  公开（公告）日：2012-05-24

  The presently disclosed subject matter relates to methods and compositions for protecting cells and or tissues from damage due to ischemia. In particular, the presently disclosed subject matter relates to the protective action of cyclin dependent kinase 4/6 (CDK4/6) inhibitors administered to subjects that have been exposed to, or that are at risk of, ischemia.

  目前公开的主题涉及保护细胞和/或组织免受缺血损伤的方法和组合物。特别是，目前公开的主题涉及给予曾经接触或有缺血风险的受试者使用细胞周期蛋白依赖性激酶4/6（CDK4/6）抑制剂的保护作用。
• [EN] HEMATOPOIETIC PROTECTION AGAINST CHEMOTHERAPEUTIC COMPOUNDS USING SELECTIVE CYCLIN-DEPENDENT KINASE 4/6 INHIBITORS<br/>[FR] PROTECTION HÉMATOPOÏÉTIQUE CONTRE LES COMPOSÉS CHIMIOTHÉRAPEUTIQUES AU MOYEN D'INHIBITEURS SÉLECTIFS DES KINASES DÉPENDANT DES CYCLINES 4/6
  申请人：UNIV NORTH CAROLINA

  公开号：WO2010039997A2

  公开（公告）日：2010-04-08

  Methods for reducing or preventing the effects of cytotoxic compounds in healthy cells are provided. The methods relate to the use of selective cyclin- dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Also described is a method of selecting compounds for reducing or preventing the effects of cytotoxic agents compounds in healthy cells.

  本文提供了减少或预防细胞毒性化合物对健康细胞影响的方法。该方法涉及使用选择性细胞周期蛋白依赖性激酶（CDK）4/6抑制剂，在CDK4/6依赖性细胞（如造血干细胞和/或造血祖细胞）中诱导短暂的静止状态。还描述了一种选择化合物以减少或预防细胞毒性化合物对健康细胞影响的方法。
• [EN] CYCLIN DEPENDENT KINASE INHIBITORS AND METHODS OF USE<br/>[FR] INHIBITEURS DE KINASES CYCLINE-DÉPENDANTES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：UNIV NORTH CAROLINA

  公开号：WO2010132725A2

  公开（公告）日：2010-11-18

  The presently disclosed subject matter relates to methods and compositions for protecting healthy cells from damage due to DNA damaging agents. In particular, the presently disclosed subject matter relates to the protective action of selective cyclin dependent kinase 4/6 (CDK4/6) inhibitors administered to subjects that have been exposed to or that are at risk of exposure to DNA damage.

  目前披露的主题涉及保护健康细胞免受DNA损伤剂的损害的方法和组合物。具体而言，目前披露的主题涉及选择性环素依赖性激酶4/6（CDK4/6）抑制剂的保护作用，该抑制剂被施用于已经接触或有接触DNA损伤风险的对象身上。
• CYCLIN DEPENDENT KINASE INHIBITORS AND METHODS OF USE
  申请人：The University of North Carolina at Chapel Hill

  公开号：EP2429566B1

  公开（公告）日：2016-01-06
• HEMATOPOIETIC PROTECTION AGAINST CHEMOTHERAPEUTIC COMPOUNDS USING SELECTIVE CYCLIN-DEPENDENT KINASE 4/6 INHIBITORS
  申请人：Sharpless Norman E.

  公开号：US20110224227A1

  公开（公告）日：2011-09-15

  Methods for reducing or preventing the effects of cytotoxic compounds in healthy cells are provided. The methods relate to the use of selective cyclin-dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Also described is a method of selecting compounds for reducing or preventing the effects of cytotoxic agents compounds in healthy cells.