8-cyclopentanecarbonyl-2-{4-[3-((2S,3'S)-2-methyl-piperidin-1-yl)-pyrrolidin-1-yl]-2-trifluoromethyl-phenyl}-2,8-diaza-spiro[4.5]decan-1-one | 1228603-28-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 8-cyclopentanecarbonyl-2-{4-[3-((2S,3'S)-2-methyl-piperidin-1-yl)-pyrrolidin-1-yl]-2-trifluoromethyl-phenyl}-2,8-diaza-spiro[4.5]decan-1-one
• 英文别名: 8-(cyclopentanecarbonyl)-2-[4-[(3S)-3-[(2S)-2-methylpiperidin-1-yl]pyrrolidin-1-yl]-2-(trifluoromethyl)phenyl]-2,8-diazaspiro[4.5]decan-1-one
• CAS: 1228603-28-8
• 化学式: C₃₁H₄₃F₃N₄O₂
• 分子量: 560.703
• InChiKey: WSNSLJODPHJFTE-DHLKQENFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  40
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.74
• 拓扑面积：
  47.1
• 氢给体数：
  0
• 氢受体数：
  7

文献信息

• [EN] SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONES USED AS H3 MODULATORS<br/>[FR] PIPÉRIDINE SPIRO PYRROLIDINONE ET PIPÉRIDINONES SUBSTITUÉS UTILISÉS COMME MODULATEURS DE H3
  申请人：SANOFI AVENTIS

  公开号：WO2010065803A1

  公开（公告）日：2010-06-10

  The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I), wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.

  本发明披露和声明了一系列以公式(I)表示的取代N-苯基-双吡咯啉羧酰胺，其中R1、R2、R3、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在治疗和/或预防由H3受体调节的各种疾病中特别有用，包括与中枢神经系统相关的疾病。此外，本发明还披露了取代N-苯基-双吡咯啉羧酰胺及其中间体的制备方法。
• SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：GAO Zhongli

  公开号：US20120258979A1

  公开（公告）日：2012-10-11

  The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R 1 , R 2 , R 3 , m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed.

  本公开涉及一系列式（I）的取代N-苯基双吡咯烷羧酰胺，其中R1、R2、R3、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此可用作药物，特别是在治疗和/或预防与中枢神经系统相关的多种H3受体调节的疾病方面。此外，本公开还揭示了取代N-苯基双吡咯烷羧酰胺及其中间体的制备方法。
• SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONES USED AS H3 MODULATORS
  申请人：SANOFI

  公开号：EP2373652B1

  公开（公告）日：2013-10-09
• US8227481B2
  申请人：——

  公开号：US8227481B2

  公开（公告）日：2012-07-24
• US8604046B2
  申请人：——

  公开号：US8604046B2

  公开（公告）日：2013-12-10