5-(4-difluoromethoxy-3,5-dimethyl-phenyl)-5-(2-pyrimidin-5-yl-pyridin-4-yl)-5H-pyrrolo[3,4-b]pyridin-7-ylamine | 1226799-56-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 5-(4-difluoromethoxy-3,5-dimethyl-phenyl)-5-(2-pyrimidin-5-yl-pyridin-4-yl)-5H-pyrrolo[3,4-b]pyridin-7-ylamine
• 英文别名: 5-[4-(difluoromethoxy)-3,5-dimethylphenyl]-5-(2-pyrimidin-5-ylpyridin-4-yl)pyrrolo[3,4-b]pyridin-7-amine
• CAS: 1226799-56-9
• 化学式: C₂₅H₂₀F₂N₆O
• 分子量: 458.47
• InChiKey: JHANWDLZOCIQAW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  99.2
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  5-(2-chloro-pyridin-4-yl)-5-(4-difluoromethoxy-3,5-dimethyl-phenyl)-5H-pyrrolo[3,4-b]pyridin-7-ylamine 、 5-嘧啶硼酸 在 四(三苯基膦)钯 potassium carbonate 作用下， 以 乙二醇二甲醚 、 水 为溶剂， 反应 17.0h， 以38%的产率得到5-(4-difluoromethoxy-3,5-dimethyl-phenyl)-5-(2-pyrimidin-5-yl-pyridin-4-yl)-5H-pyrrolo[3,4-b]pyridin-7-ylamine
  参考文献：
  名称：

  NEW COMPOUNDS 574

  摘要：

  本发明涉及具有式（I）的新化合物及其药物组合物。此外，本发明涉及治疗方法，用于治疗和/或预防与Aβ相关的病理学，如唐氏综合征、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化，包括混合性血管性和退行性起源的痴呆、老年前期痴呆、老年痴呆和与帕金森病、进行性上丘脑麻痹或皮质基底节变性相关的痴呆。

  公开号：

  US20100125081A1

文献信息

• [EN] 5H-PYRROLO [ 3, 4-B] PYRIDIN DERIVATIVES AND THEIR USE<br/>[FR] DÉRIVÉS DE 5H-PYRROLO [ 3, 4-B] PYRIDINE ET LEUR UTILISATION
  申请人：ASTRAZENECA AB

  公开号：WO2010056194A1

  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 574
  申请人：HOLENZ Jorg

  公开号：US20100125081A1

  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.

  本发明涉及具有式（I）的新化合物及其药物组合物。此外，本发明涉及治疗方法，用于治疗和/或预防与Aβ相关的病理学，如唐氏综合征、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化，包括混合性血管性和退行性起源的痴呆、老年前期痴呆、老年痴呆和与帕金森病、进行性上丘脑麻痹或皮质基底节变性相关的痴呆。