1-(3-(2-(1,4''-Bipiperidin-1''-yl)thiazolo[4,5-b]pyridin-6-yl)phenyl)ethanone | 1198759-34-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(3-(2-(1,4''-Bipiperidin-1''-yl)thiazolo[4,5-b]pyridin-6-yl)phenyl)ethanone
• 英文别名: 1-[3-[2-(4-piperidin-1-ylpiperidin-1-yl)-[1,3]thiazolo[4,5-b]pyridin-6-yl]phenyl]ethanone
• CAS: 1198759-34-0
• 化学式: C₂₄H₂₈N₄OS
• 分子量: 420.579
• InChiKey: MRAZONMUKFSBSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  77.6
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-(1,4'-bipiperidine-1'-yl)-6-bromothiazolo[4,5-b]pyridine 、 3-乙酰基苯硼酸 在 palladium catalyst 作用下， 生成 1-(3-(2-(1,4''-Bipiperidin-1''-yl)thiazolo[4,5-b]pyridin-6-yl)phenyl)ethanone
  参考文献：
  名称：

  2-（1,4'-bipiperidin-1'-yl）thiazolopyridine作为H 3受体拮抗剂的合成及其构效关系

  摘要：

  合成了一系列2-（1,4'-联哌啶-1'-基）噻唑并吡啶类化合物，并将其作为非咪唑组胺H 3受体拮抗剂的新药。设计在吡啶环的6位引入多样性以增强体外效能并降低hERG活性。这些新型的噻唑并吡啶拮抗剂的结构活性关系进行了讨论。

  DOI：

  10.1016/j.bmcl.2009.09.006

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 relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H3 receptor antagonists
  作者：Ashwin U. Rao、Anandan Palani、Xiao Chen、Ying Huang、Robert G. Aslanian、Robert E. West、Shirley M. Williams、Ren-Long Wu、Joyce Hwa、Christopher Sondey、Jean Lachowicz

  DOI：10.1016/j.bmcl.2009.09.006

  日期：2009.11

  A series of 2-(1,4′-bipiperidine-1′-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H3 receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure–activity relationships for these new thiazolopyridine antagonists are discussed.

  合成了一系列2-（1,4'-联哌啶-1'-基）噻唑并吡啶类化合物，并将其作为非咪唑组胺H 3受体拮抗剂的新药。设计在吡啶环的6位引入多样性以增强体外效能并降低hERG活性。这些新型的噻唑并吡啶拮抗剂的结构活性关系进行了讨论。