5-Trichloromethyl-3-(4'-methylbiphenyl-2-yl)-1,2,4-oxadiazole | 147403-94-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-Trichloromethyl-3-(4'-methylbiphenyl-2-yl)-1,2,4-oxadiazole
• 英文别名: 3-[2-(4-Methylphenyl)phenyl]-5-(trichloromethyl)-1,2,4-oxadiazole
• CAS: 147403-94-9
• 化学式: C₁₆H₁₁Cl₃N₂O
• 分子量: 353.635
• InChiKey: JXMHZUIDKRRNLF-UHFFFAOYSA-N

物化性质

• 沸点：
  448.5±55.0 °C(Predicted)
• 密度：
  1.376±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  38.9
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-Trichloromethyl-3-(4'-methylbiphenyl-2-yl)-1,2,4-oxadiazole 以76的产率得到[2'-(5-trichloromethyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl bromide
  参考文献：
  名称：

  Heterocyclic compounds and their use as angiotensin antagonists

  摘要：

  以上公式所示的化合物或其盐具有强烈的血管紧张素II拮抗活性、降压作用和中枢神经系统活性，并可用作循环系统疾病（如高血压病和心脏疾病（例如高心率、心力衰竭、心肌梗塞）、中风、脑出血、肾炎、动脉硬化、老年痴呆症等）的治疗剂。

  公开号：

  US05583141A1
• 作为产物：
  描述：

  4-Methylbiphenyl-2'-carboxamidoxime 以77的产率得到5-Trichloromethyl-3-(4'-methylbiphenyl-2-yl)-1,2,4-oxadiazole
  参考文献：
  名称：

  Heterocyclic compounds and their use as angiotensin antagonists

  摘要：

  以上公式所示的化合物或其盐具有强烈的血管紧张素II拮抗活性、降压作用和中枢神经系统活性，并可用作循环系统疾病（如高血压病和心脏疾病（例如高心率、心力衰竭、心肌梗塞）、中风、脑出血、肾炎、动脉硬化、老年痴呆症等）的治疗剂。

  公开号：

  US05583141A1

文献信息

• Cyclic compounds and their use
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US05500427A1

  公开（公告）日：1996-03-19

  The present invention relates to a compounds represented by the following formula or salts thereof. ##STR1## The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for the treatment of circulatory diseases such as hypertension, heart diseases, cerebral apoplexy, nephritis, atherosclerosis or Alzheimer's disease and senile dementia, and for agents of improving cerebral function.

  本发明涉及以下化合物或其盐所代表的化合物。上述化合物具有强大的抗肾素Ⅱ作用、降压作用和对中枢神经系统的作用，对于治疗高血压、心脏病、脑卒中、肾炎、动脉粥样硬化或阿尔茨海默病和老年性痴呆等循环系统疾病以及改善脑功能的药物非常有用。
• Compound which is angiotensin II antagonist
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US05243054A1

  公开（公告）日：1993-09-07

  ##STR1## compounds shown by the above formula or salt thereof show a strong angiotensin II antagonistic activity and hypotensive action and CNS activity, and are useful as therapeutic agents of circulatory diseases such as hypertensive diseases and heart diseases (e.g. hypercardia, heart failure, cardiac infarction), strokes, cerebral apoplexy, nephritis, atherosclerosis, Alzheimer's disease, senile dementia, etc.

  上述化学式所示的化合物或其盐具有强烈的血管紧张素II拮抗活性、降压作用和中枢神经系统活性，可用作循环系统疾病（如高血压病和心脏病，如高心率、心力衰竭、心肌梗死）、中风、脑卒中、肾炎、动脉硬化、阿尔茨海默病、老年性痴呆症等的治疗剂。
• 1,2,4-Oxadiazolyl- or 1,2,4-thiadiazolyl-biphenyl derivatives as angiotensin II antagonists
  申请人：TAKEDA CHEMICAL INDUSTRIES, LTD.

  公开号：EP0588299A2

  公开（公告）日：1994-03-23

  57 The present invention relates to a compounds represented by the following formula or salts thereof. The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for the treatment of circulatory diseases such as hypertension, heart diseases, cerebral apoplexy, nephritis, atherosclerosis or Alzheimer's disease and senile dementia, and for agents of improving cerebral function.

  57 本发明涉及下式所代表的化合物或其盐类。 上述化合物具有很强的血管紧张素 II 拮抗作用、降压作用和对中枢神经系统的作用，可用于治疗循环系统疾病，如高血压、心脏病、脑中风、肾炎、动脉粥样硬化或阿尔茨海默病和老年痴呆症，也可用于改善脑功能的制剂。
• Heterocyclic compounds having angiotensin II antagonistic activity and use thereof
  申请人：TAKEDA CHEMICAL INDUSTRIES, LTD.

  公开号：EP0603712A2

  公开（公告）日：1994-06-29

  This invention relates to a compound represented by the formula wherein the ring A stands for a 5-10 membered aromatic heterocyclic group optionally having, besides R1 and R2, further substituents; R1 stands for an optionally substituted hydrocarbon residue which is optionally bonded through a hetero-atom; R2 stands for a group capable of liberating proton in a living body or a group convertible thereinto; R3 stands for an 5-7 membered optionally substituted heterocyclic residue having, as a group capable of constituting the ring, carbonyl group, thiocarbonyl group, an optionally oxidized sulfur atom or a group convertible into them; X shows that the ring Y and the ring W are bonded to each other directly or through a spacer having an atomic length of two or less; the ring W and the ring Y are each an optionally substituted aromatic hydrocarbon or aromatic heterocyclic residue; and n denotes an integer of 1 to 3, or a salt thereof and to an angiotensin II antagonistic agent containing the compound (I) or a salt thereof.

  本发明涉及一种由式表示的化合物 其中，环 A 代表 5-10 位芳香杂环基团，除 R1 和 R2 外，还可选择具有其他取代基；R1 代表可选择取代的烃残基，该烃残基可选择通过杂原子键合；R2 代表可在活体内释放质子的基团或可与之转化的基团；R3 代表 5-7 位可选择取代的杂环残基，该杂环残基具有可构成环的基团、羰基、硫代羰基、可选择氧化的硫原子或可与之转化的基团；X表示环Y和环W直接或通过原子长度为2或更小的间隔物相互键合；环W和环Y各自为任选取代的芳香烃或芳香杂环残基；n表示1至3的整数，或其盐，以及表示含有化合物（I）或其盐的血管紧张素II拮抗剂。
• Heterocyclic compounds and their use as angiotensin II antagonists
  申请人：TAKEDA CHEMICAL INDUSTRIES, LTD.

  公开号：EP0829479A1

  公开（公告）日：1998-03-18

  The present invention relates to a compounds represented by the following formula or salts thereof. The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for the treatment of circulatory diseases such as hypertension, heart diseases, cerebral apoplexy, nephritis, atherosclerosis or Alzheimer's disease and senile dementia, and for agents of improving cerebral function.

  本发明涉及下式所代表的化合物或其盐类。 上述化合物具有很强的血管紧张素 II 拮抗作用、降压作用和对中枢神经系统的作用，可用于治疗循环系统疾病，如高血压、心脏病、脑中风、肾炎、动脉粥样硬化或阿尔茨海默病和老年痴呆症，也可用于改善脑功能的制剂。