2-(2-fluoroethyl)-8-methyl-2,8-diazaspiro[4,5]decane-1,3-dione | 1187036-89-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: 2-(2-fluoroethyl)-8-methyl-2,8-diazaspiro[4,5]decane-1,3-dione
• 英文别名: 2-(2-Fluoroethyl)-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione；2-(2-fluoroethyl)-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione
• CAS: 1187036-89-0
• 化学式: C₁₁H₁₇FN₂O₂
• 分子量: 228.267
• InChiKey: IPRAKAXWBDSOCW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  40.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  cyano-(1-methyl-piperidin-4-ylidene)-acetic acid ethyl ester 在 盐酸 、 ammonium hydroxide 、 水 、 sodium hydride 作用下， 以 乙醇 、 水 、 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 47.5h， 生成 2-(2-fluoroethyl)-8-methyl-2,8-diazaspiro[4,5]decane-1,3-dione
  参考文献：
  名称：

  [EN] COMPOUNDS AND COMPOSITIONS FOR THE DETECTION AND TREATMENT OF ALZHEIMER'S DISEASE AND RELATED DISORDERS
  [FR] COMPOSÉS ET COMPOSITIONS POUR LA DÉTECTION ET LE TRAITEMENT DE LA MALADIE D'ALZHEIMER ET DES TROUBLES ASSOCIÉS

  摘要：

  公开号：

  WO2009117728A3

文献信息

• Compounds and Compositions for the Detection and Treatment of Alzheimer's Disease and Related Disorders
  申请人：Elmaleh David R.

  公开号：US20110060138A1

  公开（公告）日：2011-03-10

  One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.

  本发明的一个方面涉及化合物、组合物和方法，用于诊断和/或治疗患有淀粉样变性相关病理状况的受试者。在某些实施例中，本发明的成像和/或治疗剂可以被注射给受试者，以便识别和/或治疗淀粉样沉积。一种特定的成像方法通过将成像剂注射给受试者并检测剂的空间分布来检测淀粉样沉积。剂的差异积累表明AD或淀粉样变性相关病理状况，并可以通过使用PET或SPECT相机进行监测。
• Cromolyn derivatives and related methods of imaging and treatment
  申请人：The General Hospital Corporation

  公开号：US10188757B2

  公开（公告）日：2019-01-29

  Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula; wherein X is OH, C1-C6 alkoxyl; Y and Z are independently selected from a C1-C6 alkyl, C1-C6 alkoxyl, halogen, mi-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

  本发明公开了可用作检测动脉粥样硬化斑块和治疗动脉粥样硬化及阿尔茨海默氏症的成像剂的新型色瑞林类似物，以及制造色瑞林类似物的方法。色甘宁类似物具有通式； 其中 X 是 OH、C1-C6 烷氧基；Y 和 Z 独立选自 C1-C6 烷基、C1-C6 烷氧基、卤素、mi-取代或 C1-C6 取代的胺、18F、19F 或 H；n 是 1、2 或 3；对于结构 (I)，如果 n 均为 1 且 Y 和 Z 均为 H，则 X 是 OH。
• Combination therapies for the treatment of Alzheimer's disease and related disorders
  申请人：The General Hospital Corporation

  公开号：US10398704B2

  公开（公告）日：2019-09-03

  The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.

  本发明涉及治疗阿尔茨海默氏症或淀粉样变性相关病理状况的组合疗法，包括联合施用治疗有效量的第一种化合物和治疗有效量的第二种化合物。在某些实施方案中，第一种化合物或第二种化合物抑制AB肽聚合；抗炎；改善认知功能、情绪或社会行为；与Tau或α-突触核蛋白相关；或调节淀粉样肽冲洗。
• Combination therapies for the treatment of Alzheimer'S disease and related disorders
  申请人：The General Hospital Corporation

  公开号：US10413551B2

  公开（公告）日：2019-09-17

  The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.

  本发明涉及治疗阿尔茨海默氏症或淀粉样变性相关病理状况的组合疗法，包括联合施用治疗有效量的第一种化合物和治疗有效量的第二种化合物。在某些实施方案中，第一种化合物或第二种化合物抑制AB肽聚合；抗炎；改善认知功能、情绪或社会行为；与Tau或α-突触核蛋白相关；或调节淀粉样肽冲洗。
• Compounds and compositions for the detection and treatment of Alzheimer's disease and related disorders
  申请人：The General Hospital Corporation

  公开号：US10857247B2

  公开（公告）日：2020-12-08

  One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.

  本发明的一个方面涉及用于诊断和/或治疗淀粉样变性相关病症的化合物、组合物和方法。在某些实施方案中，本发明的成像剂和/或治疗剂可用于受试者淀粉样蛋白沉积的鉴定和/或治疗。具体的成像方法是通过向受试者施用成像剂并检测成像剂的空间分布来检测淀粉样蛋白沉积。淀粉样蛋白沉积物的不同程度的积聚表明了多发性硬化症或与淀粉样蛋白沉积相关的病理状况，可使用 PET 或 SPECT 相机进行监测。