4-(R)-(1-Aza-bicyclo[2.2.2]oct-3-ylamino)-3-(1H-benzoimidazol-2-yl)-7-(morpholine-4-carbonyl)-1H-quinolin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-(R)-(1-Aza-bicyclo[2.2.2]oct-3-ylamino)-3-(1H-benzoimidazol-2-yl)-7-(morpholine-4-carbonyl)-1H-quinolin-2-one
• 英文别名: 4-(1-azabicyclo[2.2.2]octan-3-ylamino)-3-(1H-benzimidazol-2-yl)-7-(morpholine-4-carbonyl)-1H-quinolin-2-one
• 化学式: C₂₈H₃₀N₆O₃
• 分子量: 498.585
• InChiKey: HXCKYZBWYFASHK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  37
• 可旋转键数：
  4
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  103
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• Combination therapy with CHK1 inhibitors
  申请人：Gesner G. Thomas

  公开号：US20050256157A1

  公开（公告）日：2005-11-17

  Compounds of Structure I, and salts, tautomers, stereoisomers, and mixtures thereof may be used in methods of inhibiting checkpoint kinase 1 in subjects, in methods for inducing cell cycle progression, and in methods for increasing apoptosis in cells. Such compounds may be used to prepare pharmaceutical compositions and may be used in conjunction with DNA damaging agents.

  结构I的化合物及其盐类、互变异构体、立体异构体和混合物可用于抑制受试者中的检查点激酶1，用于诱导细胞周期进展的方法，以及用于增加细胞凋亡的方法。这些化合物可用于制备药物组合物，并且可以与DNA损伤剂联合使用。
• Inhibition of FGFR3 and treatment of multiple myeloma
  申请人：Cai Shaopei

  公开号：US20050261307A1

  公开（公告）日：2005-11-24

  Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.

  提供了抑制成纤维母细胞生长因子受体3并治疗由纤维母细胞生长因子受体3介导的各种疾病的方法，包括向受试者施用结构I的化合物，其药学上可接受的盐，其互变异构体，或其互变异构体的药学上可接受的盐。具有结构I的化合物具有以下结构，其中具有本文描述的变量。这些化合物可用于制备用于抑制纤维母细胞生长因子受体3和用于治疗由纤维母细胞生长因子受体3介导的疾病，如多发性骨髓瘤的药物。
• Benzimidazole quinolinones and uses thereof
  申请人：Chiron Corporation

  公开号：US20040092535A1

  公开（公告）日：2004-05-13

  Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes. 1

  提供了抑制各种酶和治疗各种疾病的方法，包括向受试者给予结构式I或IB的化合物、其药学上可接受的盐、其互变异构体或其药学上可接受的互变异构体盐。具有结构式I和IB的化合物具有以下结构，并具有此处描述的变量。这些化合物可用于制备药物，用于抑制各种酶的使用和用于治疗由这些酶介导的疾病。
• BENZIMIDAZOLE QUINOLINONES AND USES THEREOF
  申请人：Chiron Corporation

  公开号：EP1539754A2

  公开（公告）日：2005-06-15
• EP1539754A4
  申请人：——

  公开号：EP1539754A4

  公开（公告）日：2009-02-25