cis-6-Oxo-7-oxa-5-azaspiro[3.4]octane-2-carboxylic acid | 2135785-62-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: cis-6-Oxo-7-oxa-5-azaspiro[3.4]octane-2-carboxylic acid
• 英文别名: 6-oxo-7-oxa-5-azaspiro[3.4]octane-2-carboxylic acid
• CAS: 2135785-62-3
• 化学式: C₇H₉NO₄
• 分子量: 171.15
• InChiKey: IGXPOTLWCQJQJQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  75.6
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 危险性防范说明：
  P261,P280,P301+P312,P302+P352,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

文献信息

• [EN] AZASPIROCYCLES AS MONOACYLGLYCEROL LIPASE MODULATORS<br/>[FR] AZASPIROCYCLES SERVANT DE MODULATEURS DE LA MONOACYLGLYCÉROL LIPASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021191390A1

  公开（公告）日：2021-09-30

  Azaspirocycle compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein X, R1, R2a, R2b, R3, m, n, o, and p are defined herein.

  式(I)的Azaspirocycle化合物，以及其药学上可接受的盐、同位素、N-氧化物、溶剂合物和立体异构体，含有它们的药物组合物，制备它们的方法，以及使用它们的方法，包括用于治疗与MGL调节相关的疾病状态、紊乱和症状的方法，例如与疼痛、精神紊乱、神经紊乱（包括但不限于重度抑郁症、治疗抵抗性抑郁症、焦虑性抑郁症、自闭症谱系障碍、阿斯伯格综合症、双相情感障碍）、癌症和眼部疾病相关的方法：其中X、R1、R2a、R2b、R3、m、n、o和p在此处定义。
• [EN] MONOACYLGLYCEROL LIPASE MODULATORS<br/>[FR] MODULATEURS DE LA MONOACYLGLYCÉROL LIPASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021160602A1

  公开（公告）日：2021-08-19

  3.1.0 and 4.1.0 Azabicycle compounds of Formula (I), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. Wherein X, Y, R1, R2a, and R2b are defined herein.

  3.1.0和4.1.0 Azabicycle化合物的化学式（I），含有它们的药物组合物，制备它们的方法，以及使用它们的方法，包括用于治疗与MGL调节相关的疾病状态、疾病和症状的方法，例如与疼痛、精神障碍、神经系统疾病（包括但不限于重度抑郁症、治疗抵抗性抑郁症、焦虑性抑郁症、躁郁症）、癌症和眼部疾病相关的方法。其中X、Y、R1、R2a和R2b在此处定义。
• [EN] AMINOCYCLOBUTANES AS MONOACYLGLYCEROL LIPASE MODULATORS<br/>[FR] AMINOCYCLOBUTANES SERVANT DE MODULATEURS DE LA MONOACYLGLYCÉROL LIPASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021191391A1

  公开（公告）日：2021-09-30

  Aminocyclobutane compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein X, R1, R2a, R2b, R3 and R4 are defined herein.

  化合物的分子式（I）为氨基环丁烷化合物，以及其药用盐、同位素、N-氧化物、溶剂合物和立体异构体，包含它们的药物组合物，以及使用它们的方法，包括用于治疗与MGL调节相关的疾病状态、紊乱和条件的方法，如与疼痛、精神障碍、神经障碍（包括但不限于重度抑郁症、治疗抵抗性抑郁症、焦虑性抑郁症、自闭症谱系障碍、阿斯伯格综合征、躁郁症）、癌症和眼部疾病相关的方法：其中X、R1、R2a、R2b、R3和R4在此处有定义。
• [EN] ARYL PIPERIDINES AS MONOACYLGLYCEROL LIPASE MODULATORS<br/>[FR] ARYLPIPÉRIDINES EN TANT QUE MODULATEURS DE LA MONOACYLGLYCÉROL LIPASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021191384A1

  公开（公告）日：2021-09-30

  Aryl piperidine compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein X, R2a, R2b, R3, R4, R5a and R5b are as defined herein.

  化学式（I）的芳基哌啶化合物，以及其药用可接受的盐、同位素、N-氧化物、溶剂合物和立体异构体，含有它们的药物组合物，以及使用它们的方法，包括用于治疗与MGL调节相关的疾病状态、障碍和情况的方法，例如与疼痛、精神障碍、神经系统障碍（包括但不限于重性抑郁障碍、治疗抵抗性抑郁症、焦虑性抑郁症、自闭症谱系障碍、阿斯伯格综合征、躁郁症）、癌症和眼部疾病相关的情况：其中X、R2a、R2b、R3、R4、R5a和R5b的定义如本文所述。
• HETEROCYCLIC COMPOUND
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US20170283406A1

  公开（公告）日：2017-10-05

  The present invention provides a compound having an MAGL inhibitory action, and useful as an agent for the prophylaxis or treatment of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis etc.), anxiety disorder, pains (e.g., inflammatory pain, cancerous pain, neurogenic pain etc.), epilepsy, depression and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

  本发明提供了一种具有MAGL抑制作用的化合物，可用作预防或治疗神经退行性疾病（例如阿尔茨海默病、帕金森病、亨廷顿病、肌萎缩侧索硬化、创伤性脑损伤、青光眼、多发性硬化等）、焦虑障碍、疼痛（例如炎症性疼痛、癌症疼痛、神经源性疼痛等）、癫痫、抑郁症等。本发明涉及一种由下式（I）表示的化合物：其中每个符号如规范中定义，或其盐。