Tert-butyl 3-oxo-1,2-diphenyl-2,7-diazaspiro[3.5]nonane-7-carboxylate | 1013033-86-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: Tert-butyl 3-oxo-1,2-diphenyl-2,7-diazaspiro[3.5]nonane-7-carboxylate
• CAS: 1013033-86-7
• 化学式: C₂₄H₂₈N₂O₃
• 分子量: 392.498
• InChiKey: TUCPACIKMKOCKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  49.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Tert-butyl 3-oxo-1,2-diphenyl-2,7-diazaspiro[3.5]nonane-7-carboxylate 在 三氟乙酸 作用下， 生成 1,2-Diphenyl-2,7-diazaspiro[3.5]nonan-3-one
  参考文献：
  名称：

  Spiro-piperidine azetidinones as potent TRPV1 antagonists

  摘要：

  A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.12.024
• 作为产物：
  描述：

  N-苄叉苯胺 、 N-Boc-4-哌啶甲酸乙酯 在 lithium hexamethyldisilazane 作用下， 生成 Tert-butyl 3-oxo-1,2-diphenyl-2,7-diazaspiro[3.5]nonane-7-carboxylate
  参考文献：
  名称：

  Spiro-piperidine azetidinones as potent TRPV1 antagonists

  摘要：

  A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.12.024

文献信息

• TREATING PAIN, DIABETES, AND DISORDERS OF LIPID METABOLISM
  申请人：Harris M. Joel

  公开号：US20080070892A1

  公开（公告）日：2008-03-20

  Disclosed is a method of treating a disease or condition (e.g., pain, diabetes or disorders of lipid metabolism) comprising administering an azetidine derivative of the formula I selected from the group consisting of the compounds defined by Tables 1, 2, 3a, 3b, 3c, 3d and 4a.

  揭示了一种治疗疾病或病症（例如疼痛、糖尿病或脂质代谢紊乱）的方法，包括给予从表1、2、3a、3b、3c、3d和4a定义的化合物组中选择的式I的吖啶衍生物。
• Azetidinone Derivatives and Methods of Use Thereof
  申请人：Aslanian G. Robert

  公开号：US20080076750A1

  公开（公告）日：2008-03-27

  The present invention relates to methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering a compound having the formula or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof, wherein: R 1 and R 2 are defined in Tables 1-6 herein, and R 3 is -phenyl, -4-chlorophenyl, -2-pyridyl, or -3-pyridyl.

  本发明涉及治疗或预防脂质代谢紊乱、疼痛、糖尿病、血管疾病、脱髓鞘或非酒精性脂肪肝病的方法，包括给予具有以下结构式的化合物或其药学上可接受的盐、溶剂化合物、酯、前药或立体异构体： R 1 和 R 2 在本文的表1-6中定义，并且 R 3 为-苯基、-4-氯苯基、-2-吡啶基或-3-吡啶基。
• [EN] AZETIDINONE DERIVATIVES AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS D'AZÉTIDINONE ET PROCÉDÉS D'UTILISATION DE CEUX-CI
  申请人：SCHERING CORP

  公开号：WO2008033465A1

  公开（公告）日：2008-03-20

  [EN] The present invention relates to methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering a compound having the formula (I) or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof, wherein: R¹ and R² are defined in Tables 1-6 herein, and R₃ is -phenyl, -4-chlorophenyl, -2-pyridyl, or -3-pyridyl.
  [FR] La présente invention concerne des procédés pour traiter ou prévenir un trouble du métabolisme lipidique, la douleur, le diabète, un état vasculaire, une démyélination ou une stéatose hépatique non alcoolique, lesdits procédés comportant l'administration d'un composé ayant la formule (I) ou un sel pharmaceutique acceptable, un solvate, un ester, un promédicament ou un stéréoisomère de celui-ci, formule dans laquelle : R¹ et R² sont définis dans les Tableaux 1-6 par les présentest, et R₃ est -phényle, -4-chlorophényle, -2-pyridyle, ou -3-pyridyle.
• [EN] TREATING PAIN, DIABETES, AND DISORDERS OF LIPID METABOLISM<br/>[FR] PROCÉDÉ DE TRAITEMENT DE LA DOULEUR, DU DIABÈTE ET DES TROUBLES DU MÉTABOLISME LIPIDIQUE
  申请人：SCHERING CORP

  公开号：WO2008033460A2

  公开（公告）日：2008-03-20

  [EN] Disclosed is a method of treating a disease or condition (e.g., pain, diabetes or disorders of lipid metabolism) comprising administering an azetidine derivative of the formula (I) selected from the group consisting of the compounds defined by Tables 1, 2, 3a, 3b, 3c, 3d and 4a.
  [FR] La présente invention concerne un procédé de traitement d'une maladie ou d'un trouble (par exemple, la douleur, le diabète ou les troubles du métabolisme lipidique) comprenant l'étape consistant à administrer un dérivé de l'azétidine de la formule (I) choisi dans le groupe comprenant les composés définis par les Tableaux 1, 2, 3a, 3b, 3c, 3d et 4a.
• Spiro-piperidine azetidinones as potent TRPV1 antagonists
  作者：Dong Xiao、Anandan Palani、Robert Aslanian、Brian A. McKittrick、Andrew T. McPhail、Craig C. Correll、P. Tara Phelps、John C. Anthes、Diane Rindgen

  DOI：10.1016/j.bmcl.2008.12.024

  日期：2009.2

  A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat. (C) 2008 Elsevier Ltd. All rights reserved.