<1-methyl-4-(ethoxycarbonyl)piperidin-4-yl>acetic acid hydrochloride | 117280-91-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: <1-methyl-4-(ethoxycarbonyl)piperidin-4-yl>acetic acid hydrochloride
• 英文别名: (1-methyl-4-carboxypiperidin-4-yl) acetic acid hydrochloride；1-methyl-4-carboxymethylpiperidine-4-carboxylic acid hydrochloride；(1-Methyl-4-carboxypiperidin-4-yl)acetic acid.hydrochloride；4-(carboxymethyl)-1-methylpiperidine-4-carboxylic acid;hydrochloride
• CAS: 117280-91-8
• 化学式: C₉H₁₅NO₄*ClH
• 分子量: 237.683
• InChiKey: DBZMLJWRFFDIHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.68
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  77.8
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  <1-methyl-4-(ethoxycarbonyl)piperidin-4-yl>acetic acid hydrochloride 在 ammonium hydroxide 、 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 7.5h， 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
• 作为产物：
  描述：

  cyano-(1-methyl-piperidin-4-ylidene)-acetic acid ethyl ester 在 盐酸 、 水 作用下， 以 乙醇 、 水 为溶剂， 反应 40.0h， 生成 <1-methyl-4-(ethoxycarbonyl)piperidin-4-yl>acetic acid hydrochloride
  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

• Azaspiro compounds and their use
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US04804665A1

  公开（公告）日：1989-02-14

  Azaspiro compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, a hydrocarbon residue which may have a substituent, or an acyl group which may have a substituent; R.sub.3 represents hydrogen or a hydrocarbon residue which may have a substituent; each of X.sub.1 and X.sub.2 is oxygen or sulfur; Y represents oxygen, sulfur or a group of the formula: --N(R.sub.4)--, wherein R.sub.4 represents hydrogen or a lower alkyl group; m represents 0 or 1; n represents 0 or 1, and its salt are novel compounds, possess excellent brain function-improving action, and are of use as drugs for the prevention and therapy of senile dementia of Alzheimer type, vascular-type dementia and dementia derived from Alzheimer's disease, Pick's disease, Huntington's disease, Creutzfeldt-Jakob's disease, Parkinson's disease and spinocerebellar degeneration.

  Azaspiro化合物的结构式为##STR1##其中R.sub.1和R.sub.2分别代表氢、可能具有取代基的碳氢残基，或者可能具有取代基的酰基；R.sub.3代表氢或者可能具有取代基的碳氢残基；X.sub.1和X.sub.2中的每一个代表氧或者硫；Y代表氧、硫或者具有以下结构的基团：--N(R.sub.4)--，其中R.sub.4代表氢或者较低的烷基基团；m代表0或1；n代表0或1，其盐是新颖的化合物，具有出色的改善脑功能的作用，并可用作预防和治疗老年性阿尔茨海默型痴呆、血管型痴呆以及源自阿尔茨海默病、皮克氏病、亨廷顿病、克雅茨菲尔德-雅各布病、帕金森病和脊髓小脑变性病的药物。
• Central Cholinergic Agents. III. Synthesis of 2-Alkoxy-2,8-diazaspiro(4.5)decane-1,3-diones as Muscarinic Agonists.
  作者：Yuji ISHIHARA、Hidehumi YUKIMASA、Masaomi MIYAMOTO、Giichi GOTO

  DOI：10.1248/cpb.40.1177

  日期：——

  and tested for muscarinic receptor binding affinity using [3H]pirenzepine and [3H]oxotremorine M as ligands. They were also evaluated for agonistic activities in the guinea pig ileum assay. 2-Methoxy- 2,8-diazaspiro[4.5]decane-1,3-dione (1i) was found to be a relatively M1 selective agonist. It reversed CO2-induced impairment of passive avoidance response with long duration of action, but also displayed

  合成了一系列的2-烷氧基-2,8-二氮杂螺[4.5]癸烷-1,3-二酮和相关化合物，并以[3H]哌仑西平和[3H]氧代苯甲酸M作为配体测试了毒蕈碱受体的结合亲和力。还通过豚鼠回肠试验评估了它们的激动活性。发现2-甲氧基-2,8-二氮杂螺[4.5]癸烷-1,3-二酮（1i）是相对M1选择性的激动剂。它以较长的作用时间逆转了CO2引起的被动回避反应的损害，但在低剂量时也表现出外周效应。为了最小化这些副作用，我们提出了将1i与毒蕈碱拮抗剂结合的想法。因此，检查了1i的氨基甲酸酯连接的共轭物（1u）与甲基阿托品。
• 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。
• Azaspiro compounds, their production and use
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0273659A1

  公开（公告）日：1988-07-06

  Azaspiro compounds of the formula: wherein R₁ and R₂ independently represent hydrgen, a hydrocarbon residue which may have a substituent, or an acyl group which may have a substituent; R₃ represents hydrogen or a hydrocarbon residue which may have a substituent; each of X₁ and X₂ is oxygen or sulfur; Y represents oxygen, sulfur or a group of the formula: -N(R₄)-, wherein R₄ represents hydrogen or a lower alkyl group; m represents 0 or 1; n represents 0 or 1, and its salt are novel compounds, possess excellent brain functionimproving action, and are of use as drugs for the prevention and therapy of senile dementia of Alzheimer type, vascular-type dementia and dementia derived from Alzheimer's disease, Pick's disease, Huntington's disease, Creutzfeldt-­Jakob's disease, Parkinson's disease and spinocerebellar degeneration.

  式中的氮杂环化合物： 其中 R₁ 和 R₂ 独立地代表氢、可具有取代基的烃残基或可具有取代基的酰基；R₃ 代表氢或可具有取代基的烃残基；X₁ 和 X₂ 各自为氧或硫；Y 代表氧、硫或式中的基团：-N(R₄)-，其中 R₄ 代表氢或低级烷基；m 代表 0 或 1；n 代表 0 或 1，其盐是新型化合物，具有优异的改善脑功能的作用，可用作预防和治疗阿尔茨海默型老年痴呆症、血管型痴呆症以及由阿尔茨海默病、皮克病、亨廷顿病、克雅氏病、帕金森病和脊髓小脑变性引起的痴呆症的药物。
• 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。