3-(4-fluorophenyl)-6-[2-(4-fluorophenyl)-2H-pyrazol-3-yl]imidazo[1,2-a]pyridine | 1612185-10-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(4-fluorophenyl)-6-[2-(4-fluorophenyl)-2H-pyrazol-3-yl]imidazo[1,2-a]pyridine
• 英文别名: 3-(4-Fluoro-phenyl)-6-[2-(4-fluoro-phenyl)-2H-pyrazol-3-yl]-imidazo[1,2-a]pyridine；3-(4-fluorophenyl)-6-[2-(4-fluorophenyl)pyrazol-3-yl]imidazo[1,2-a]pyridine
• CAS: 1612185-10-0
• 化学式: C₂₂H₁₄F₂N₄
• 分子量: 372.377
• InChiKey: CAGFOYNELFAUOL-UHFFFAOYSA-N

物化性质

• 密度：
  1.32±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  35.1
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-溴-3-碘咪唑并[1,2-A]吡啶 在 sodium carbonate 作用下， 以 乙二醇二甲醚 为溶剂， 反应 34.25h， 生成 3-(4-fluorophenyl)-6-[2-(4-fluorophenyl)-2H-pyrazol-3-yl]imidazo[1,2-a]pyridine
  参考文献：
  名称：

  [EN] IMIDAZOPYRIDINE DERIVATIVES
  [FR] DÉRIVÉS D'IMIDAZOPYRIDINE

  摘要：

  本发明涉及通式（I）的化合物，其中Ar是苯基或吡啶基；X1是N或CH，X2是N或CH，但只有X1或X2是N，而另一个是CH；R1是氢，卤素，低烷基，低烷氧基，低烷基被卤素，氰或S（O）2-低烷基取代的；R2是氢，卤素，低烷基，低烷氧基，低烷基被卤素或氰取代的；n为1或2；或其药学上可接受的酸加合物，外消旋混合物或其对应的对映体和/或光学异构体。这些化合物可用于治疗精神分裂症、强迫症人格障碍、重度抑郁症、躁郁症、焦虑症、正常衰老、癫痫、视网膜退化、创伤性脑损伤、脊髓损伤、创伤后应激障碍、惊恐障碍、帕金森病、痴呆、阿尔茨海默病、轻度认知障碍、化疗引起的认知功能障碍、唐氏综合症、自闭症谱系障碍、听力损失、耳鸣、脊髓小脑性共济失调、肌萎缩侧索硬化症、多发性硬化症、亨廷顿病、中风、放射治疗、慢性压力、神经活性药物滥用，如酒精、鸦片类、甲基苯丙胺、苯环利定和可卡因。

  公开号：

  WO2014082979A1

文献信息

• IMIDAZOPYRIDINE DERIVATIVES
  申请人：Hoffmann-La Roche Inc.

  公开号：US20150259341A1

  公开（公告）日：2015-09-17

  The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X 1 is N or CH, X 2 is N or CH, with the proviso that only one of X 1 or X 2 is N and the other is CH; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(0) 2 -lower alkyl; R 2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.

  本发明涉及通式化合物，其中Ar为苯基或吡啶基; X1为N或CH，X2为N或CH，但只有X1或X2是N，另一个是CH; R1为氢、卤素、低碳基、低烷氧基、低碳基取代的卤素、氰或S（0）2-低碳基; R2为氢、卤素、低碳基、低烷氧基、低碳基取代的卤素或氰; n为1或2; 或其药学上可接受的酸加盐、外消旋混合物或其相应的对映体和/或光学异构体。这些化合物可用于治疗精神分裂症、强迫症人格障碍、重度抑郁症、双相障碍、焦虑症、正常衰老、癫痫、视网膜退化、创伤性脑损伤、脊髓损伤、创伤后应激障碍、惊恐障碍、帕金森病、痴呆、阿尔茨海默病、轻度认知障碍、化疗引起的认知功能障碍、唐氏综合症、自闭症谱系障碍、听力损失、耳鸣、脊髓小脑性共济失调、肌萎缩侧索硬化症、多发性硬化症、亨廷顿病、中风、放射治疗、慢性压力、神经活性药物滥用，如酒精、阿片类、甲基苯丙胺、苯环利定和可卡因。
• Imidazopyridine derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US09315502B2

  公开（公告）日：2016-04-19

  The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(O)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.

  本发明涉及通式化合物，其中Ar为苯基或吡啶基；X1为N或CH，X2为N或CH，但仅有X1或X2为N，另一个为CH；R1为氢、卤素、较低烷基、较低烷氧基、被卤素、氰或S（O）2-较低烷基取代的较低烷基；R2为氢、卤素、较低烷基、较低烷氧基、被卤素或氰取代的较低烷基；n为1或2；或其药学上可接受的酸盐、外消旋体混合物或其对应的对映异构体。该化合物可用于治疗精神分裂症、强迫症人格障碍、重度抑郁症、双相障碍、焦虑症、正常衰老、癫痫、视网膜退化、创伤性脑损伤、脊髓损伤、创伤后应激障碍、惊恐障碍、帕金森病、痴呆、阿尔茨海默病、轻度认知障碍、化疗引起的认知功能障碍、唐氏综合症、自闭症谱系障碍、听力损失、耳鸣、脊髓小脑性共济失调、肌萎缩性脊髓侧索硬化症、多发性硬化症、亨廷顿病、中风、放射治疗、慢性压力、神经活性药物滥用，如酒精、阿片类、甲基苯丙胺、苯环已呋喃和可卡因。
• US9315502B2
  申请人：——

  公开号：US9315502B2

  公开（公告）日：2016-04-19
• [EN] IMIDAZOPYRIDINE DERIVATIVES<br/>[FR] DÉRIVÉS D'IMIDAZOPYRIDINE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2014082979A1

  公开（公告）日：2014-06-05

  The present invention relates to compounds of general formula (I) wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(O)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.

  本发明涉及通式（I）的化合物，其中Ar是苯基或吡啶基；X1是N或CH，X2是N或CH，但只有X1或X2是N，而另一个是CH；R1是氢，卤素，低烷基，低烷氧基，低烷基被卤素，氰或S（O）2-低烷基取代的；R2是氢，卤素，低烷基，低烷氧基，低烷基被卤素或氰取代的；n为1或2；或其药学上可接受的酸加合物，外消旋混合物或其对应的对映体和/或光学异构体。这些化合物可用于治疗精神分裂症、强迫症人格障碍、重度抑郁症、躁郁症、焦虑症、正常衰老、癫痫、视网膜退化、创伤性脑损伤、脊髓损伤、创伤后应激障碍、惊恐障碍、帕金森病、痴呆、阿尔茨海默病、轻度认知障碍、化疗引起的认知功能障碍、唐氏综合症、自闭症谱系障碍、听力损失、耳鸣、脊髓小脑性共济失调、肌萎缩侧索硬化症、多发性硬化症、亨廷顿病、中风、放射治疗、慢性压力、神经活性药物滥用，如酒精、鸦片类、甲基苯丙胺、苯环利定和可卡因。