2',3'-dihydro-1'H-spiro[cyclopropane-1,4'-quinoline] | 1304598-29-5

• 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: 2',3'-dihydro-1'H-spiro[cyclopropane-1,4'-quinoline]
• 英文别名: spiro[2,3-dihydro-1H-quinoline-4,1'-cyclopropane]
• CAS: 1304598-29-5
• 化学式: C₁₁H₁₃N
• mdl: MFCD20688508
• 分子量: 159.231
• InChiKey: ZFHFVUIJOYMULN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.454
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2',3'-dihydro-1'H-spiro[cyclopropane-1,4'-quinoline] 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 [3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]-spiro[2,3-dihydroquinoline-4,1'-cyclopropane]-1-ylmethanone
  参考文献：
  名称：

  Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1

  摘要：

  A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11 beta-HSD1 inhibitors. Rational chemical optimization provided potent and selective inhibitors of both human and murine 11 beta-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.02.111
• 作为产物：
  描述：

  tert-butyl 4-methylene-3,4-dihydroquinoline-1(2H)-carboxylate 在 盐酸 、 diethylzinc 作用下， 以 1,4-二氧六环 、 乙醚 为溶剂， 生成 2',3'-dihydro-1'H-spiro[cyclopropane-1,4'-quinoline]
  参考文献：
  名称：

  Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1

  摘要：

  A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11 beta-HSD1 inhibitors. Rational chemical optimization provided potent and selective inhibitors of both human and murine 11 beta-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.02.111

文献信息

• N-LINKED HETEROCYCLIC ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS
  申请人：Qiao Jennifer

  公开号：US20100197716A1

  公开（公告）日：2010-08-05

  The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y 1 receptor which can be used as medicaments.

  本发明提供了一种新型尿素，包含式（I）中的N-芳基或N-杂环芳基取代的杂环，或其立体异构体、互变异构体、药学上可接受的盐或溶剂形式，其中变量A、B、D和W如本文所定义。这些化合物是人类P2Y1受体的选择性抑制剂，可用作药物。
• TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES
  申请人：AbbVie Inc.

  公开号：US20140080816A1

  公开（公告）日：2014-03-20

  The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT 2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT 2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C receptor.

  本发明涉及三环喹啉和喹噁啉衍生物，以及含有这些化合物的药物组合物，它们的用途为5-HT2C受体的调节剂，特别是激动剂或部分激动剂，用于制备用于预防或治疗对5-HT2C受体调节有反应的病症和疾病的药物，以及用于预防或治疗对5-HT2C受体调节有反应的病症和疾病的方法。
• Tricyclic quinoline and quinoxaline derivatives
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：US10118926B2

  公开（公告）日：2018-11-06

  The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.

  本发明涉及三环喹啉和喹喔啉衍生物，涉及含有此类化合物的药物组合物，涉及它们作为 5-HT2C 受体调节剂（尤其是激动剂或部分激动剂）的用途，涉及它们用于制备预防或治疗对 5-HT2C 受体调节有反应的病症和紊乱的药物，还涉及一种预防或治疗对 5-HT2C 受体调节有反应的病症和紊乱的方法。
• DÉRIVÉS D'URÉES DE PIPERIDINE OU PYRROLIDINE, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
  申请人：Sanofi-Aventis

  公开号：EP2044057A2

  公开（公告）日：2009-04-08
• US7550499B2
  申请人：——

  公开号：US7550499B2

  公开（公告）日：2009-06-23