2-(4-Piperidin-1-ylpiperidin-1-yl)-[1,3]oxazolo[4,5-b]pyridine | 1231933-81-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶唑并吡啶类
• 英文名称: 2-(4-Piperidin-1-ylpiperidin-1-yl)-[1,3]oxazolo[4,5-b]pyridine
• CAS: 1231933-81-5
• 化学式: C₁₆H₂₂N₄O
• 分子量: 286.377
• InChiKey: KBTIIRRRLNQBTC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  45.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-(4-Piperidin-1-ylpiperidin-1-yl)-[1,3]oxazolo[4,5-b]pyridine 在 溴 、 sodium acetate 、 溶剂黄146 、 sodium hydroxide 作用下， 以 水 为溶剂， 以79%的产率得到6-Bromo-2-(4-piperidin-1-ylpiperidin-1-yl)-[1,3]oxazolo[4,5-b]pyridine
  参考文献：
  名称：

  [EN] BICYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF USE THEREOF
  [FR] DÉRIVÉS HÉTÉROCYCLIQUES BICYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  本发明涉及新颖的双环杂环衍生物，包括该双环杂环衍生物的药物组合物以及利用这些化合物治疗或预防过敏、过敏引起的气道反应、充血、心血管疾病、炎症性疾病、消化系统疾病、神经系统疾病、认知障碍、代谢性疾病、肥胖或与肥胖相关的疾病、糖尿病、糖尿病并发症、糖耐量受损或空腹血糖受损的用途。

  公开号：

  WO2010071819A1
• 作为产物：
  描述：

  2-氨基-3-羟基吡啶 在 potassium carbonate 、 potassium hydroxide 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 生成 2-(4-Piperidin-1-ylpiperidin-1-yl)-[1,3]oxazolo[4,5-b]pyridine
  参考文献：
  名称：

  Synthesis and structure–activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists

  摘要：

  The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H-3 antagonists is described. Introduction of substituted phenyl, pyridyl and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H-3 antagonist activity in both ex vivo and in vivo assays. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.01.020

文献信息

• [EN] BICYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES BICYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：SCHERING CORP

  公开号：WO2010071819A1

  公开（公告）日：2010-06-24

  The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

  本发明涉及新颖的双环杂环衍生物，包括该双环杂环衍生物的药物组合物以及利用这些化合物治疗或预防过敏、过敏引起的气道反应、充血、心血管疾病、炎症性疾病、消化系统疾病、神经系统疾病、认知障碍、代谢性疾病、肥胖或与肥胖相关的疾病、糖尿病、糖尿病并发症、糖耐量受损或空腹血糖受损的用途。
• Bicyclic Heterocyclic Derivatives and Methods of Use Thereof
  申请人：Palani Anandan

  公开号：US20110319434A1

  公开（公告）日：2011-12-29

  The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
• US8283360B2
  申请人：——

  公开号：US8283360B2

  公开（公告）日：2012-10-09
• Synthesis and structure–activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists
  作者：Ning Shao、Robert Aslanian、Robert E. West、Shirley M. Williams、Ren-Long Wu、Joyce Hwa、Christopher Sondey、Jean Lachowicz、Anandan Palani

  DOI：10.1016/j.bmcl.2012.01.020

  日期：2012.3

  The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H-3 antagonists is described. Introduction of substituted phenyl, pyridyl and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H-3 antagonist activity in both ex vivo and in vivo assays. (C) 2012 Elsevier Ltd. All rights reserved.