2-pyridin-2-yloxy-1H-benzimidazole | 1018987-28-4

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-pyridin-2-yloxy-1H-benzimidazole
• CAS: 1018987-28-4
• 化学式: C₁₂H₉N₃O
• 分子量: 211.223
• InChiKey: SYLABBNLHCTJEF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-羟基吡啶 、 2-(甲基磺酰基)-(9ci)-1H-苯并咪唑 在 三乙胺 作用下， 反应 15.0h， 以62%的产率得到2-pyridin-2-yloxy-1H-benzimidazole
  参考文献：
  名称：

  An efficient method to access 2-substituted benzimidazoles under solvent-free conditions

  摘要：

  An expeditious method to access 2-substituted benzimidazoles was developed. Both aromatic (phenols, anilines, and thiophenols) and alkyl nucleophiles (amines and thiols) react with 2-methylsulfonyl benzimidazole under solvent-free conditions to generate a variety of 2-substituted benzimidazoles. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2008.01.100

文献信息

• Substituted benzimidazoles and methods of preparation
  申请人：Dimitroff Martin

  公开号：US20070049622A1

  公开（公告）日：2007-03-01

  Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R 1 , R 2 , R 3 , R 4 , a, b, and c are defined herein

  提供了制备新的取代苯并咪唑化合物的方法，其化学式为（I），用于治疗激酶介导的疾病，其中R1、R2、R3、R4、a、b和c在此定义。
• Substituted benzimidazoles and methods of their use
  申请人：Alkawa E. Mina

  公开号：US20070161680A1

  公开（公告）日：2007-07-12

  New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

  本文提供了新的取代苯并咪唑化合物、组合物以及抑制人或动物主体中与肿瘤发生相关的激酶活性的方法。在某些实施例中，这些化合物和组合物能够有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。这些新的化合物和组合物可以单独使用或与至少一种额外的药物联合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的疾病，如癌症。
• SUBSTITUTED BENZIMIDAZOLES AND METHODS OF THEIR USE
  申请人：Aikawa Mina E.

  公开号：US20100234394A1

  公开（公告）日：2010-09-16

  New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

  本发明提供了新的取代苯并咪唑化合物、组合物以及抑制人类或动物主体中与肿瘤发生相关的激酶活性的方法。在某些实施例中，这些化合物和组合物能够有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。这些新的化合物和组合物可以单独使用或与至少一种额外的药物联合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的疾病，如癌症。
• SUBSTITUTED BENZIMIDAZOLES AND METHODS OF PREPARATION
  申请人：Dimitroff Martin

  公开号：US20100256375A1

  公开（公告）日：2010-10-07

  Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R 1 , R 2 , R 3 , R 4 , a, b, and c are defined herein

  提供了制备新的取代苯并咪唑化合物的方法，其化学式为(I)，用于治疗激酶介导的疾病，其中R1、R2、R3、R4、a、b和c的定义如下。
• Combination therapy
  申请人：Array BioPharma Inc.

  公开号：US10548894B2

  公开（公告）日：2020-02-04

  Reversing resistance to a B-Raf inhibitor for the treatment of a proliferative disease by obtaining a tumor sample from the patient and testing it for genetic alterations in a panel of genes comprising BRAF, CRAF, CCND1, CDK4, HER2, IGF-1R, cMET, FGFR1, FGFR2, FGFR3 EGFR, MAP2K1, MAP2K2, NRAS, KRAS HRAS, PTEN, PIK3CA, and P16 and administering a drug combination therapy comprising the B-Raf inhibitor and a second inhibitor which overcomes resistance to the B-Raf inhibitor, which second inhibitor is selected based on genetic alterations discovered in the tumor sample.

  逆转对治疗增殖性疾病的B-Raf抑制剂的耐药性，方法是获取患者的肿瘤样本并检测其在一组基因中的遗传改变，这些基因包括BRAF、CRAF、CCND1、CDK4、HER2、IGF-1R、cMET、FGFR1、FGFR2、FGFR3 EGFR、MAP2K1、MAP2K2、NRAS、KRAS HRAS、PTEN、PIK3CA和P16、NRAS、KRAS HRAS、PTEN、PIK3CA 和 P16，并施用一种药物组合疗法，其中包括 B-Raf 抑制剂和第二种抑制剂，第二种抑制剂可克服对 B-Raf 抑制剂的耐药性，第二种抑制剂是根据肿瘤样本中发现的基因改变来选择的。