4-氧代-1,4,5,6-四氢环戊并[b]吡咯-2-羧酸 | 1041429-47-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 4-氧代-1,4,5,6-四氢环戊并[b]吡咯-2-羧酸
• 英文名称: 4-oxo-1,4,5,6-tetrahydrocyclopenta[b]pyrrole-2-carboxylic acid
• 英文别名: 4-oxo-5,6-dihydro-1H-cyclopenta[b]pyrrole-2-carboxylic acid
• CAS: 1041429-47-3
• 化学式: C₈H₇NO₃
• 分子量: 165.148
• InChiKey: DFPHXLOGIRIMHQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  70.2
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  N-甲基哌嗪 、 4-氧代-1,4,5,6-四氢环戊并[b]吡咯-2-羧酸 在 N-甲基吗啉 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 以69%的产率得到2-(4-methylpiperazine-1-carbonyl)-5,6-dihydro-1H-cyclopenta[b]pyrrol-4-one
  参考文献：
  名称：

  EP2460794

  摘要：

  公开号：
• 作为产物：
  描述：

  N-(1-环戊烯基)吗啉 在 水 、 2,3-二氯-5,6-二氰基-1,4-苯醌 、 lithium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 水 、 甲苯 为溶剂， 反应 14.5h， 生成 4-氧代-1,4,5,6-四氢环戊并[b]吡咯-2-羧酸
  参考文献：
  名称：

  EP2460794

  摘要：

  公开号：

文献信息

• INHIBITORS OF D-AMINO ACID OXIDASE
  申请人：Heffernan Michele L. R.

  公开号：US20100029737A1

  公开（公告）日：2010-02-04

  The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

  本发明提供了新型D-氨基酸氧化酶酶的抑制剂。本发明的化合物可用于治疗或预防疾病和/或症状，其中调节D-丝氨酸水平和/或其氧化产物对缓解症状有效。本发明还提供了增强学习，记忆和/或认知的方法。例如，本发明提供了用于治疗或预防神经退行性疾病（如阿尔茨海默病）相关的记忆和/或认知丧失的方法。本发明还提供了预防神经退行性疾病特征性神经元功能丧失的方法。此外，还提供了用于治疗或预防神经精神疾病（例如，精神分裂症）和用于治疗或预防疼痛和共济失调的方法。
• Inhibitors of D-amino acid oxidase
  申请人：Sepracor, Inc.

  公开号：US07902252B2

  公开（公告）日：2011-03-08

  The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

  本发明提供了新型D-氨基酸氧化酶的抑制剂。本发明的化合物可用于治疗或预防疾病和/或症状，其中调节D-丝氨酸水平及/或其氧化产物可有效缓解症状。此外，本发明还提供了增强学习、记忆和/或认知的方法。例如，本发明提供了用于治疗或预防神经退行性疾病（如阿尔茨海默病）相关的记忆和/或认知损失的方法。本发明还提供了预防神经退行性疾病特征性神经元功能丧失的方法。此外，还提供了治疗或预防神经精神疾病（如精神分裂症）以及治疗或预防疼痛和共济失调的方法。
• PHARMACEUTICAL COMPOSITION CONTAINING FUSED HETERO-RING DERIVATIVE
  申请人：Shionogi & Co., Ltd.

  公开号：EP2460794A1

  公开（公告）日：2012-06-06

  The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R7)- or -O-; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R8)= or -N=; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.

  本发明提供了一种具有组胺 H4 受体调节活性的化合物。 由式（I）代表的化合物： 其中 一个环是由下式表示的环： 其中 R1是取代或未取代的烷基等，W是-O-等，n是0至6的整数；X是N(R7)-或-O-；R7是氢、取代或未取代的烷基等；Y是-C(R8)=或-N=；R8是氢、取代或未取代的烷基等；Z是=O、=S等； B 环是由下式表示的环 其中 R10各自独立地为取代或未取代的烷基、卤素、羟基、取代或未取代的烷氧基、取代或未取代的氨基；R11、R12a和R12b各自独立地为氢或取代或未取代的烷基等；p为0至4的整数，或其药学上可接受的盐，或其溶液。
• US7902252B2
  申请人：——

  公开号：US7902252B2

  公开（公告）日：2011-03-08
• [EN] INHIBITORS OF D-AMINO ACID OXIDASE<br/>[FR] INHIBITEURS DE D-AMINO ACIDE OXYDASE
  申请人：SEPRACOR INC

  公开号：WO2011011330A2

  公开（公告）日：2011-01-27

  The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.