[8-(3-piperidin-1-yl-propoxy)-3,4-dihydro-2H-quinolin-1-yl]-thiophen-2-ylmethanone | 676255-13-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: [8-(3-piperidin-1-yl-propoxy)-3,4-dihydro-2H-quinolin-1-yl]-thiophen-2-ylmethanone
• 英文别名: [8-(3-piperidin-1-ylpropoxy)-3,4-dihydro-2H-quinolin-1-yl]-thiophen-2-ylmethanone
• CAS: 676255-13-3
• 化学式: C₂₂H₂₈N₂O₂S
• 分子量: 384.543
• InChiKey: JFSRBIHRASHFFM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  61
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  [8-(3-piperidin-1-yl-propoxy)-3,4-dihydro-2H-quinolin-1-yl]-thiophen-2-ylmethanone 在 盐酸 作用下， 以 甲醇 、 乙醚 为溶剂， 反应 0.08h， 以60%的产率得到[8-(3-piperidin-1-yl-propoxy)-3,4-dihydro-2H-quinolin-1-yl]-thiophen-2-ylmethanone hydrochloride
  参考文献：
  名称：

  [EN] HISTAMINE H3 RECEPTOR ANTAGONISTS, PREPARATON AND THERAPEUTIC USES
  [FR] ANTAGONISTES DU RECEPTEUR H3 D'HISTAMINE, PREPARATION ET APPLICATIONS THERAPEUTIQUES

  摘要：

  公开号：

  WO2004026837A3
• 作为产物：
  描述：

  8-甲氧基-1,2,3,4-四氢喹啉 在 盐酸 、 sodium hydroxide 、 caesium carbonate 、 三乙胺 、 potassium iodide 作用下， 以 1,4-二氧六环 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 生成 [8-(3-piperidin-1-yl-propoxy)-3,4-dihydro-2H-quinolin-1-yl]-thiophen-2-ylmethanone
  参考文献：
  名称：

  Synthesis and SAR of novel histamine H3 receptor antagonists

  摘要：

  The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H-3 receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H-3 receptors are reported. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.04.004

文献信息

• Histamine h3 receptor antagonists, preparation and therapeutic uses
  申请人：Beavers Selsam Lisa

  公开号：US20060167046A1

  公开（公告）日：2006-07-27

  The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-II3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods or using them to treat obesity and other histamine II3 receptor-related diseases.

  本发明揭示了化合物(I)或其药学上可接受的盐的新型化合物，其具有组胺H3受体拮抗活性，以及制备这些化合物的方法。在另一实施例中，本发明揭示了包括化合物(I)的药物组合物，以及使用它们治疗肥胖症和其他组胺H3受体相关疾病的方法。
• Synthesis and SAR of novel histamine H3 receptor antagonists
  作者：Cynthia D. Jesudason、Lisa S. Beavers、Jeffrey W. Cramer、Joelle Dill、Don R. Finley、Craig W. Lindsley、F. Craig Stevens、Robert A. Gadski、Samuel W. Oldham、R. Todd Pickard、Christopher S. Siedem、Dana K. Sindelar、Ajay Singh、Brian M. Watson、Philip A. Hipskind

  DOI：10.1016/j.bmcl.2006.04.004

  日期：2006.7

  The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H-3 receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H-3 receptors are reported. (c) 2006 Elsevier Ltd. All rights reserved.
• [EN] HISTAMINE H3 RECEPTOR ANTAGONISTS, PREPARATON AND THERAPEUTIC USES<br/>[FR] ANTAGONISTES DU RECEPTEUR H3 D'HISTAMINE, PREPARATION ET APPLICATIONS THERAPEUTIQUES
  申请人：LILLY CO ELI

  公开号：WO2004026837A3

  公开（公告）日：2005-08-18