3-fluoro-10-aza-tricyclo[6.3.1.0.2.7]dodeca-2(7),3,5-triene | 357425-69-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 3-fluoro-10-aza-tricyclo[6.3.1.0.2.7]dodeca-2(7),3,5-triene
• 英文别名: 3-Fluoro-10-azatricyclo[6.3.1.02,7]dodeca-2(7),3,5-triene
• CAS: 357425-69-5
• 化学式: C₁₁H₁₂FN
• 分子量: 177.221
• InChiKey: MQWQCNHPYKVXNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  在 palladium dihydroxide 盐酸 、 氢气 作用下， 以 甲醇 为溶剂， 生成 3-fluoro-10-aza-tricyclo[6.3.1.0.2.7]dodeca-2(7),3,5-triene
  参考文献：
  名称：

  3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation

  摘要：

  3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha 4 beta 2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha 4 beta 2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic doparnine system, a key measure of therapeutic potential for smoking cessation. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.08.035

文献信息

• Nicontinic acetylcholine receptor antagonists in the treatment of restless legs syndrome
  申请人：Pfizer Inc.

  公开号：US20030134844A1

  公开（公告）日：2003-07-17

  This invention relates to the use of nicotinic acetylcholine receptor agonists for the treatment of restless legs syndrome (RLS). The invention further relates to the use of a nicotinic acetylcholine receptor agonist in the manufacture of a medicament for the treatment of RLS. The present invention also relates to a pharmaceutical composition for the treatment of RLS containing a nicotinic acetylcholine receptor agonist.

  这项发明涉及尼古丁型乙酰胆碱受体激动剂用于治疗不安腿综合征（RLS）。该发明还涉及尼古丁型乙酰胆碱受体激动剂在制造治疗RLS药物中的应用。本发明还涉及一种含有尼古丁型乙酰胆碱受体激动剂的治疗RLS的药物组合物。
• [EN] PROCESS FOR THE PREPARATION OF ARYL FUSED POLYCYCLIC LACTAMS<br/>[FR] PROCEDE DE PREPARATION DE LACTAMES POLYCYCLIQUES A FUSION ARYLE
  申请人：PFIZER PROD INC

  公开号：WO2004063164A1

  公开（公告）日：2004-07-29

  A process for the preparation of aryl fused polycyclic lactams of formulaI which are useful intermediates in the synthesis of aryl fused azapolycyclic compounds as agents for the treatment of neurological and psychological disorders.

  一种制备公式I的芳基融合多环内酰胺的方法，这些化合物是合成芳基融合氮杂多环化合物的有用中间体，可作为治疗神经和心理障碍的药物。
• Aryl fused azapolycyclic compounds
  申请人：——

  公开号：US20030130260A1

  公开（公告）日：2003-07-10

  This invention is directed to compounds of the formula (I): 1 and their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

  本发明涉及式(I)的化合物及其药学上可接受的盐，其中R1、R2和R3如本文所定义；用于合成此类化合物的中间体，含有此类化合物的药物组合物；以及使用此类化合物治疗神经和心理疾病的方法。
• Process for the preparation of aryl fused polycyclic lactams
  申请人：Handfield Jr Eugene Robert

  公开号：US20070066827A1

  公开（公告）日：2007-03-22

  A process for the preparation of aryl fused polycyclic lactams which are useful intermediates in the synthesis of aryl fused azapolycyclic compounds as agents for the treatment of neurological and psychological disorders.

  一种制备芳基融合多环内酰胺的方法，这些化合物是合成芳基融合氮杂多环化合物的有用中间体，可以用作治疗神经和心理障碍的药物。
• Therapeutic combination for cognititon enhancement and psychotic disorders
  申请人：Romano Joseph Steve

  公开号：US20050215571A1

  公开（公告）日：2005-09-29

  This invention relates to combinations of an atypical antipsychotic, and a nicotinic receptor agonist or antagonist, kits containing such combinations, pharmaceutical compositions comprising such combinations, and methods of using such combinations to treat patients suffering from cognitive impairment disorders or psychotic disorders or conditions.

  本发明涉及一种非典型抗精神病药和一种烟碱受体激动剂或拮抗剂的组合物、含有这种组合物的试剂盒、包含这种组合物的药物组合物以及使用这种组合物治疗患有认知障碍疾病或精神病的患者的方法。