2-(2-amino-4,5-dihydro-3H-pyrrol-3-yl)-isoindole-1,3-dione hydrochloride | 937174-38-4

• 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: 2-(2-amino-4,5-dihydro-3H-pyrrol-3-yl)-isoindole-1,3-dione hydrochloride
• 英文别名: 2-(5-amino-3,4-dihydro-2H-pyrrol-4-yl)isoindole-1,3-dione;hydrochloride
• CAS: 937174-38-4
• 化学式: C₁₂H₁₁N₃O₂*ClH
• 分子量: 265.699
• InChiKey: NZYZYSHFUQPJDC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.83
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  75.8
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Substituted bicyclic pyrimidone derivatives
  申请人：Sanofi-Aventis

  公开号：EP1790649A1

  公开（公告）日：2007-05-30

  A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C1-3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 represents a hydrogen atom, a C1-6 alkoxy carbonyl group or a C1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.

  一种以化学式（I）表示的嘧啶酮衍生物，或其盐，或其溶剂合物，或其水合物： 其中： Y代表两个氢原子，一个硫原子，一个氧原子或一个C1-2烷基团和一个氢原子； Z代表一个键，一个氧原子，一个被氢原子或C1-3烷基团取代的氮原子，一个硫原子，一个可选择性取代的亚甲基基团； R1代表一个2、3或4-吡啶环或一个2、4或5-嘧啶环，环可选择性取代； R2代表一个苯环或一个萘环；环可选择性取代； R3代表一个氢原子，一个C1-6烷基团或一个卤原子； R4代表一个氢原子或一个C1-6烷基团； R5代表一个氢原子，一个C1-6烷氧羰基团或一个可选择性取代的C1-6烷基团； R6代表一个氢原子，一个C1-6烷基团或一个卤原子； R7代表一个氢原子或一个C1-6烷基团； n表示0到3；m表示0到1；o表示0到2。 该发明还涉及一种药物，包括所述衍生物或其盐作为活性成分，用于预防和/或治疗由GSK3β异常活性引起的神经退行性疾病，如阿尔茨海默病。
• SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES
  申请人：CHEREZE Nathalie

  公开号：US20090036427A1

  公开（公告）日：2009-02-05

  A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.

  一种由式（I）表示的吡啶酮衍生物或其盐、溶剂或水合物：其中Y、Z、R1、R2、R3、R4、R5、R6、R7、n、m和o如所述。本发明还涉及一种药物，其包含所述衍生物或其盐作为活性成分，用于预防和/或治疗由GSK3β异常活性引起的神经退行性疾病，如阿尔茨海默病。
• SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES
  申请人：FAYOL Aude

  公开号：US20090306088A1

  公开（公告）日：2009-12-10

  A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.

  本发明揭示和声明了由式(I)表示的吡啶酮衍生物，或其盐、溶剂或水合物。其中m、n、o、Y、Z、R1、R2、R3、R4、R5、R6和R7如本文所述。本发明还揭示了式(I)化合物的盐。本发明涉及一种药物，其包括所述衍生物或其盐作为活性成分，用于预防和/或治疗由GSK3β异常活性引起的神经退行性疾病，如阿尔茨海默病。
• US8148364B2
  申请人：——

  公开号：US8148364B2

  公开（公告）日：2012-04-03
• US8198287B2
  申请人：——

  公开号：US8198287B2

  公开（公告）日：2012-06-12