1-(3-Bromophenyl)-4-fluoro-1-(5-methoxy-4,6-dimethylpyridin-2-yl)-1H-isoindol-3-amine | 1227163-07-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 1-(3-Bromophenyl)-4-fluoro-1-(5-methoxy-4,6-dimethylpyridin-2-yl)-1H-isoindol-3-amine
• 英文别名: 3-(3-bromophenyl)-7-fluoro-3-(5-methoxy-4,6-dimethylpyridin-2-yl)isoindol-1-amine
• CAS: 1227163-07-6
• 化学式: C₂₂H₁₉BrFN₃O
• 分子量: 440.315
• InChiKey: CLCVDLPUGJSBNI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  60.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(3-Bromophenyl)-4-fluoro-1-(5-methoxy-4,6-dimethylpyridin-2-yl)-1H-isoindol-3-amine 、 5-嘧啶硼酸 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 caesium carbonate 作用下， 以 乙二醇二甲醚 、 乙醇 、 水 为溶剂， 反应 0.33h， 以17%的产率得到4-Fluoro-1-(5-methoxy-4,6-dimethylpyridin-2-yl)-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine
  参考文献：
  名称：

  NEW COMPOUNDS 578

  摘要：

  本发明涉及式(I)的新化合物及其药物组合物。此外，本发明涉及用于治疗和/或预防与Aβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合性血管性和退行性起源的痴呆，早老性痴呆，老年性痴呆和与帕金森病，进行性上核性麻痹或皮层基底变性相关的痴呆有关的治疗方法。

  公开号：

  US20100125082A1
• 作为产物：
  描述：

  2-bromo-5-methoxy-4,6-dimethylpyridine 、 N-((3-bromophenyl)(2-cyano-3-fluorophenyl)methylene)-2-methylpropane-2-sulfinamide 在 叔丁基锂 、 盐酸 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 1.0h， 以84%的产率得到1-(3-Bromophenyl)-4-fluoro-1-(5-methoxy-4,6-dimethylpyridin-2-yl)-1H-isoindol-3-amine
  参考文献：
  名称：

  NEW COMPOUNDS 578

  摘要：

  本发明涉及式(I)的新化合物及其药物组合物。此外，本发明涉及用于治疗和/或预防与Aβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合性血管性和退行性起源的痴呆，早老性痴呆，老年性痴呆和与帕金森病，进行性上核性麻痹或皮层基底变性相关的痴呆有关的治疗方法。

  公开号：

  US20100125082A1

文献信息

• Substituted Isoindoles
  申请人：HOLENZ Jörg

  公开号：US20110319426A1

  公开（公告）日：2011-12-29

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及式（I）的新型化合物及其制药组合物。此外，本发明涉及治疗和/或预防与Aβ相关的病理学，例如唐氏综合症、β-淀粉样蛋白血管病，例如脑淀粉样血管病或遗传性脑出血，与认知障碍有关的疾病，例如轻度认知障碍（MCI）、阿尔茨海默病、记忆丧失、与阿尔茨海默病相关的注意力缺陷症状、与阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合的血管性和退行性起源的痴呆症、老年前期痴呆症、老年痴呆症和与帕金森病、进行性核上性麻痹或皮质基底节变性有关的痴呆症的治疗方法。
• Substituted isoindoles for the treatment and/or prevention of Aβ- related pathologies
  申请人：AstraZeneca AB

  公开号：US08030500B2

  公开（公告）日：2011-10-04

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及式（I）的新化合物及其制药组合物。此外，本发明涉及治疗和/或预防与Aβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样血管病或遗传性脑出血，与认知障碍有关的疾病，如但不限于轻度认知障碍（MCI），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与阿尔茨海默病或痴呆症等神经退行性疾病相关的神经退化，包括混合血管性和退行性起源的痴呆、早老性痴呆、老年性痴呆和与帕金森病、进行性核上性麻痹或皮层基底节变性相关的痴呆的治疗方法。
• US8030500B2
  申请人：——

  公开号：US8030500B2

  公开（公告）日：2011-10-04
• [EN] NEW COMPOUNDS 578<br/>[FR] NOUVEAUX COMPOSÉS 578
  申请人：ASTRAZENECA AB

  公开号：WO2010056196A1

  公开（公告）日：2010-05-20

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
• NEW COMPOUNDS 578
  申请人：HOLENZ Jörg

  公开号：US20100125082A1

  公开（公告）日：2010-05-20

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及式(I)的新化合物及其药物组合物。此外，本发明涉及用于治疗和/或预防与Aβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合性血管性和退行性起源的痴呆，早老性痴呆，老年性痴呆和与帕金森病，进行性上核性麻痹或皮层基底变性相关的痴呆有关的治疗方法。