6-[2-(4-Chlorophenyl)pyrazol-3-yl]-3-(4-methylsulfonylphenyl)imidazo[1,2-a]pyridine;6-[2-(4-fluorophenyl)pyrazol-3-yl]-3-(4-methylsulfonylphenyl)imidazo[1,2-a]pyridine;3-(4-fluorophenyl)-6-[2-[4-(trifluoromethyl)phenyl]pyrazol-3-yl]imidazo[1,2-a]pyridine

• 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: 6-[2-(4-Chlorophenyl)pyrazol-3-yl]-3-(4-methylsulfonylphenyl)imidazo[1,2-a]pyridine;6-[2-(4-fluorophenyl)pyrazol-3-yl]-3-(4-methylsulfonylphenyl)imidazo[1,2-a]pyridine;3-(4-fluorophenyl)-6-[2-[4-(trifluoromethyl)phenyl]pyrazol-3-yl]imidazo[1,2-a]pyridine
• 英文别名: 6-[2-(4-chlorophenyl)pyrazol-3-yl]-3-(4-methylsulfonylphenyl)imidazo[1,2-a]pyridine;6-[2-(4-fluorophenyl)pyrazol-3-yl]-3-(4-methylsulfonylphenyl)imidazo[1,2-a]pyridine;3-(4-fluorophenyl)-6-[2-[4-(trifluoromethyl)phenyl]pyrazol-3-yl]imidazo[1,2-a]pyridine
• 化学式: C69H48ClF5N12O4S2
• 分子量: 1303.8
• InChiKey: NFWKXGZDEVYFQZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  15.32
• 重原子数：
  93
• 可旋转键数：
  11
• 环数：
  15.0
• sp3杂化的碳原子比例：
  0.04
• 拓扑面积：
  190
• 氢给体数：
  0
• 氢受体数：
  15

文献信息

• [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。
• IMIDAZOPYRIDINE DERIVATIVES
  申请人：F.Hoffmann-La Roche AG

  公开号：EP2925756A1

  公开（公告）日：2015-10-07