2-{4-[3-(2-methyl-pyrrolidin-1-yl)-cyclopentyl]-phenyl}-1-oxo-2-aza-spiro[4.5]decane-8-carboxylic acid methyl ester | 1350476-20-8

• 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: 2-{4-[3-(2-methyl-pyrrolidin-1-yl)-cyclopentyl]-phenyl}-1-oxo-2-aza-spiro[4.5]decane-8-carboxylic acid methyl ester
• 英文别名: methyl 2-[4-[(1S)-3-(2-methylpyrrolidin-1-yl)cyclopentyl]phenyl]-1-oxo-2-azaspiro[4.5]decane-8-carboxylate
• CAS: 1350476-20-8
• 化学式: C₂₇H₃₈N₂O₃
• 分子量: 438.61
• InChiKey: YTAMITIRNKQJQV-KDNCPYKKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  32
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  49.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF<br/>[FR] SPIROLACTAMES ET AMIDES DE PHÉNYLCYCLOALKYLPYRROLIDINE (PIPÉRIDINE) SUBSTITUÉS, LEUR PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：SANOFI SA

  公开号：WO2011143150A1

  公开（公告）日：2011-11-17

  The present invention discloses and claims respectively a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (I) (Ia) and formula (Ib) 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 phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.

  本发明分别公开和声明了一系列取代苯基环烷基吡咯烷（哌啶）螺内酰胺和酰胺的化合物，其化学式如下（I）（Ia）和（Ib）。更具体地，本发明的化合物是H3受体调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种疾病在内的由H3受体调节的疾病中特别有用。此外，本发明还公开了取代苯基环烷基吡咯烷（哌啶）螺内酰胺和酰胺的制备方法，以及其中间体。
• SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：SANOFI

  公开号：US20130065877A1

  公开（公告）日：2013-03-14

  The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R 1 , R 2 , R 3 , R 4 , X, m, l, n, p and s 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 disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.

  本公开涉及一系列以取代苯基环烷基吡咯烷（哌啶）螺内酰胺和酰胺的公式（Ia）和公式（Ib）。其中，R1、R2、R3、R4、X、m、l、n、p和s如此描述。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/或预防包括与中枢神经系统相关的多种疾病在内的H3受体调节的疾病中，特别是作为药物剂量非常有用。此外，本公开还涉及制备取代苯基环烷基吡咯烷（哌啶）螺内酰胺和酰胺的方法以及其中间体。
• Substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides, preparation and therapeutic use thereof
  申请人：SANOFI

  公开号：EP2569280B1

  公开（公告）日：2015-02-25
• US20140275005A1
  申请人：——

  公开号：US20140275005A1

  公开（公告）日：2014-09-18
• US8735385B2
  申请人：——

  公开号：US8735385B2

  公开（公告）日：2014-05-27