Meso-((1R,5S,6s)-3-benzyl-3-azabicyclo[3.1.0]hexan-6-yl)methanol | 1246025-66-0

• 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: Meso-((1R,5S,6s)-3-benzyl-3-azabicyclo[3.1.0]hexan-6-yl)methanol
• 英文别名: [(1R,5S,65)-3-benzyl-3-azabicyclo[3.1.0]hexan-6-yl]methanol；(1A,5A,6A)-3-BENZYL-6-HYDROXYMETHYL-3-AZABICYCLO[3.1.0]-hexane
• CAS: 1246025-66-0
• 化学式: C₁₃H₁₇NO
• 分子量: 203.284
• InChiKey: NMJRXNUMGKZPHG-CLLJXQQHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.36
• 重原子数：
  15.0
• 可旋转键数：
  3.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  23.47
• 氢给体数：
  1.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  Meso-((1R,5S,6s)-3-benzyl-3-azabicyclo[3.1.0]hexan-6-yl)methanol 在 5%-palladium/activated carbon 甲酸铵 作用下， 以 甲醇 为溶剂， 反应 8.0h， 生成 3-Azabicyclo[3.1.0]hexane-6-methanol, (1α,5α,6β)-
  参考文献：
  名称：

  [EN] OXAZOLIDINONE DERIVATIVES AS ANTIMICROBIALS
  [FR] DERIVES D'OXAZOLIDINONES EN TANT QU'AGENTS ANITMICROBIENS

  摘要：

  本发明涉及某些带有取代基的苯基噁唑烷酮，其化学式为h，其中T是一个环，并涉及其合成过程。这些化合物是有用的抗微生物剂，对许多人类和兽医病原体有效，包括革兰氏阳性厌氧细菌，如多重耐药葡萄球菌、链球菌和肠球菌，以及厌氧生物，如杆菌属和梭菌属物种，以及耐酸生物，如结核分枝杆菌、分枝杆菌和结核分枝杆菌、分枝杆菌和分枝杆菌属。

  公开号：

  WO2004069816A1
• 作为产物：
  描述：

  ethyl (1α,5α,6β)-3-benzyl-3-azabicyclo[3.1.0]hexane-2,4-dione-6-carboxylate 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 0.5h， 以83%的产率得到Meso-((1R,5S,6s)-3-benzyl-3-azabicyclo[3.1.0]hexan-6-yl)methanol
  参考文献：
  名称：

  Synthesis and structure–activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists

  摘要：

  A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modi. cation of a screening hit. Structure-activity relationships and efforts undertaken to achieve a favourable pharmacokinetic pro. le in rat are described. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.06.140

文献信息

• COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
  申请人：CHIESI FARMACEUTICI S.P.A.

  公开号：US20180016267A1

  公开（公告）日：2018-01-18

  Compounds of formula I defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.

  本处定义的I式化合物既作为肌肉收缩受体拮抗剂，又作为β2肾上腺素受体激动剂，可用于预防和/或治疗支气管阻塞或炎症性疾病。
• [EN] TRIAZINE-OXADIAZOLES<br/>[FR] TRIAZINE-OXADIAZOLES
  申请人：NOVARTIS AG

  公开号：WO2012035023A1

  公开（公告）日：2012-03-22

  The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.

  这项发明涉及公式（I）的新衍生物，其中取代基如规范中所定义；制备这种衍生物的方法；包括这种衍生物的药物组合物；将这种衍生物用作药物；将这种衍生物用于治疗慢性疼痛。
• Azabicyclic amine histamine-3 receptor antagonists
  申请人：Wlodecki Bishop

  公开号：US20060047114A1

  公开（公告）日：2006-03-02

  This invention is directed to compounds of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastrointestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.

  这项发明涉及本文中定义的I式化合物，或其药学上可接受的盐；含有I式化合物的药物组合物；一种治疗可能通过拮抗组胺H3受体而治疗的紊乱或疾病的方法，该方法包括向需要此类治疗的哺乳动物施用上述I式化合物；以及一种治疗抑郁症、情绪障碍、精神分裂症、焦虑障碍、阿尔茨海默病、注意力缺陷障碍（ADD）、注意力缺陷多动障碍（ADHD）、精神障碍、睡眠障碍、肥胖、眩晕、癫痫、晕动病、呼吸道疾病、过敏、过敏诱导的气道反应、过敏性鼻炎、鼻塞、过敏性充血、充血、低血压、心血管疾病、胃肠道疾病、胃肠道的高低蠕动性和酸分泌的疾病的方法，该方法包括向需要此类治疗的哺乳动物施用上述I式化合物。
• [EN] COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR TRAITER DES ÉTATS PATHOLOGIQUES ASSOCIÉS À UNE ACTIVITÉ DE STING
  申请人：IFM DUE INC

  公开号：WO2022015977A1

  公开（公告）日：2022-01-20

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

  本公开涉及化学实体（例如，化合物或药物可接受的盐，水合物，共晶体或化合物的药物组合），其抑制（例如，对抗）干扰素基因刺激剂（STING）。这些化学实体是有用的，例如，用于治疗在该主题（例如，人类）中增加（例如，过度）STING激活（例如，STING信号传导）对病理学和/或症状和/或病情进展有贡献的状况，疾病或障碍（例如，癌症）。本公开还涉及包含相同的组合物以及使用和制造相同的方法。
• Triazine-oxadiazoles
  申请人：BARKER Oliver

  公开号：US20140051676A1

  公开（公告）日：2014-02-20

  The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.

  该发明涉及公式(I)的新衍生物，其中取代基如规范中所定义；制备这种衍生物的方法；包含这种衍生物的药物组合物；这种衍生物作为药物；这种衍生物用于治疗慢性疼痛。