N-ethyl-3,8-diazabicyclo[3.2.1]octane-8-carboxamide | 1258073-90-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: N-ethyl-3,8-diazabicyclo[3.2.1]octane-8-carboxamide
• CAS: 1258073-90-3
• 化学式: C₉H₁₇N₃O
• 分子量: 183.253
• InChiKey: JXUZFTUZQJAIBO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  44.4
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  [1-[(3R,5R)-4-(4-chlorophenyl)sulfonyl-5-(cyclopropylmethyl)morpholin-3-yl]cyclopropyl] carbonochloridate 、 N-ethyl-3,8-diazabicyclo[3.2.1]octane-8-carboxamide 以 二氯甲烷 为溶剂， 生成 1-((3R,5R)-4-(4-chlorophenylsulfonyl)-5-(cyclopropylmethyl)morpholin-3-yl)cyclopropyl 8-(ethylcarbamoyl)-3,8-diazabicyclo[3.2.1]octane-3-carboxylate
  参考文献：
  名称：

  Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors

  摘要：

  Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel gamma-secretase inhibitors for the potential treatment of Alzheimer's disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excellent in vitro potency. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.09.028

文献信息

• SUBSTITUTED DIAZAHETERO-BICYCLIC COMPOUNDS AND THEIR USE
  申请人：Bayer Aktiengesellschaft

  公开号：US20210024545A1

  公开（公告）日：2021-01-28

  The present application relates to novel (imidazo[1,2-a]pyridin-3-yl)methyl-substituted diazaheterobicyclic compounds, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of respiratory disorders including sleep-related respiratory disorders such as obstructive sleep apnoea and central sleep apnoea and snoring. The present application further relates to a method of discovering a compound having TASK-1-and/or TASK-3-blocking properties.

  本申请涉及新颖的（咪唑[1,2-a]吡啶-3-基）甲基取代的二氮杂杂双环化合物，其制备方法，单独或组合使用以治疗和/或预防疾病，以及用于生产用于治疗和/或预防疾病的药物的用途，特别是用于治疗和/或预防呼吸系统疾病，包括睡眠相关的呼吸系统疾病，如阻塞性睡眠呼吸暂停症、中枢性睡眠呼吸暂停症和打鼾。本申请还涉及一种发现具有TASK-1和/或TASK-3阻断特性的化合物的方法。
• US7763613B2
  申请人：——

  公开号：US7763613B2

  公开（公告）日：2010-07-27
• [EN] COMBINATION OF AN α2-ADRENOCEPTOR SUBTYPE C (ALPHA-2C) ANTAGONISTS WITH A TASK1/3 CHANNEL BLOCKER FOR THE TREATMENT OF SLEEP APNEA<br/>[FR] COMBINAISON D'ANTAGONISTES D'UN SOUS-TYPE C DE RÉCEPTEUR α2-ADRÉNERGIQUE (ALPHA-2C) AVEC UN BLOQUEUR DE CANAL TASK1/3 POUR LE TRAITEMENT DE L'APNÉE DU SOMMEIL
  申请人：BAYER AG

  公开号：WO2020225185A1

  公开（公告）日：2020-11-12

  The present invention relates to a combination of selective blockers of TASK-1 and TASK-3 channels, in particular diazabicyclically substituted imidazo[1,2-a]pyrimidine derivatives and α2-Adrenoceptor subtype C (alpha-2C) antagonists, in particular aryl piperazines of formula (I) for the treatment and/or prophylaxis of sleep-related breathing disorders, preferably obstructive and central sleep apneas and snoring.
• Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors
  作者：Hongmei Li、Ruo Xu、David Cole、John W. Clader、William J. Greenlee、Amin A. Nomeir、Lixin Song、Lili Zhang

  DOI：10.1016/j.bmcl.2010.09.028

  日期：2010.11

  Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel gamma-secretase inhibitors for the potential treatment of Alzheimer's disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excellent in vitro potency. (C) 2010 Elsevier Ltd. All rights reserved.