2-methyl-4,6-bis-trifluoromethyl-1(3)H-benzimidazole | 102153-70-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 2-methyl-4,6-bis-trifluoromethyl-1(3)H-benzimidazole
• 英文别名: 2-Methyl-4,6-bis-trifluormethyl-1(3)H-benzimidazol；2-methyl-4,6-bis(trifluoromethyl)-1H-benzimidazole
• CAS: 102153-70-8
• 化学式: C₁₀H₆F₆N₂
• 分子量: 268.161
• InChiKey: IJEAEWOQWFFWDQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  28.7
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-氯-1-硝基-3,5-双三氟甲苯 在 盐酸 、 乙醇 、 氨 、 tin(ll) chloride 作用下， 生成 2-methyl-4,6-bis-trifluoromethyl-1(3)H-benzimidazole
  参考文献：
  名称：

  Jagupol'skii; Troizkaja, Zhurnal Obshchei Khimii, 1959, vol. 29, p. 2730,2735, 2736; engl. Ausg. S. 2697, 2701

  摘要：

  DOI：

文献信息

• Benzimidazole carboxamides as raf kinase inhibitors
  申请人：Buchstaller Hans-Peter

  公开号：US20070093532A1

  公开（公告）日：2007-04-26

  The present invention relates to benzimidazole carboxamides of formula (I), the use of the compounds of formula (I) as inhibitors of as inhibitors of one or more kinases, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. Accordingly, the compound of Formula (I) or a pharmaceutically acceptable salt thereof is administered for the treatment of diseases mediated by one or more kinase phathways, preferably by the raf kinase pathway, especially cancers.

  本发明涉及式（I）的苯并咪唑羧酰胺，以化合物式（I）作为一个或多个激酶的抑制剂，以化合物式（I）制备制药组合物的用途以及治疗方法，包括向患者给予该制药组合物。因此，式（I）的化合物或其药学上可接受的盐被用于治疗由一个或多个激酶途径介导的疾病，优选是通过raf激酶途径，特别是癌症。
• Benzimidazole derivatives and their use as protein kinases inhibitors
  申请人：Berdini Valerio

  公开号：US20070135477A1

  公开（公告）日：2007-06-14

  The invention provides compounds of the formula (1): The compounds have activity against cyclin depdenent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.

  该发明提供了式（1）的化合物： 这些化合物具有对环素依赖性激酶、糖原合成酶激酶和Auroa激酶的活性，因此可用于治疗癌症和病毒性疾病。
• Benzimidazole derivatives as raf kinase inhibitors
  申请人：Buchstaller Hans-Peter

  公开号：US20070010560A1

  公开（公告）日：2007-01-11

  The present invention relates to benzimidazole derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. Accordingly, the compound of Formula I or a pharmaceutically acceptable salt thereof is administered for the treatment of diseases mediated by one or more kinase pathways, preferably by the raf kinase pathway, especially cancers, [FORMULA]

  本发明涉及公式I的苯并咪唑衍生物，公式I化合物作为一个或多个激酶的抑制剂的用途，公式I化合物的用途用于制备制药组合物和治疗方法，包括将该制药组合物给患者。因此，公式I化合物或其药学上可接受的盐被用于治疗由一个或多个激酶途径介导的疾病，优选是由raf激酶途径介导的疾病，特别是癌症。[公式]
• Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases
  申请人：Berdini Valerio

  公开号：US20080312223A1

  公开（公告）日：2008-12-18

  The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR 5 or N; each of Q 1 and Q 2 is a carbon atom; Q 3 is selected from S and CH; Q 4 is selected from CR 2 and S; provided that one of Q 3 and Q 4 is S and the other of Q 3 and Q 4 is not S; wherein when Q 3 is S, there is a double bond between Q 1 and Q 4 and a double bond between Q 2 and the adjacent ring nitrogen atom N; and when Q 4 is S, there is a double bond between Q 1 and Q 2 , and a double bond between Q 3 and the adjacent ring nitrogen atom N; A is a bond or —(CH 2 ) m —(B) n —; B is C═O, NR 8 (C═O) or O(C═O) wherein R 1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R o is hydrogen or, together with NR g when present, forms a group —(CH 2 ) p — wherein p is 2 to 4; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is as defined in the claims. The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.

  本发明提供一种化合物，其化学式为（I）或其盐，N-氧化物，互变异构体或溶剂化物，其中X为CR5或N; Q1和Q2中的每一个都是碳原子; Q3从S和CH中选择; Q4从CR2和S中选择; 假设Q3和Q4中的一个是S，而另一个不是S; 当Q3为S时，Q1和Q4之间有一个双键，Q2和相邻的环氮原子N之间有一个双键; 当Q4为S时，Q1和Q2之间有一个双键，并且Q3和相邻的环氮原子N之间有一个双键; A是键或-(CH2)m-(B)n-; B为C═O，NR8（C═O）或O（C═O），其中R1为氢或C1_4烃基，可选择地被羟基或C1-4烷氧基取代; m为0、1或2; n为0或1; Ro为氢或与NRg一起形成一个群体-(CH2)p-，其中p为2至4; R1为氢，具有3至12个环成员的碳环或杂环基，或可选择地被取代的C1-8烃基基团; R2为氢、卤素、甲氧基或可选择地被卤素、羟基或甲氧基取代的C1-4烃基基团; R3和R4与它们所连接的碳原子一起形成一个可选择地取代的融合碳环或杂环环，其具有5至7个环成员，其中最多可有3个异原子，选择自N、O和S; R5为氢、R2基团或R10基团，其中R10如权利要求所定义。该化合物具有作为细胞周期依赖性激酶、糖原合成酶激酶和极化子激酶的抑制剂的活性。
• BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS
  申请人：BERDINI Valerio

  公开号：US20110224203A1

  公开（公告）日：2011-09-15

  The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Aurora kinases and are therefore useful to treat cancer and viral diseases.

  该发明提供了式(I)的化合物：这些化合物对于细胞周期依赖性激酶、糖原合成酶激酶和极化激酶具有活性，因此可用于治疗癌症和病毒性疾病。