2-(4-fluoro-benzyl)-6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-1,2,3,4-tetrahydro-isoquinoline | 1350411-05-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-(4-fluoro-benzyl)-6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-1,2,3,4-tetrahydro-isoquinoline
• 英文别名: 2-[(4-fluorophenyl)methyl]-6-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]-3,4-dihydro-1H-isoquinoline
• CAS: 1350411-05-0
• 化学式: C₂₅H₃₂FN₃
• 分子量: 393.548
• InChiKey: UJEINTPIEDKKAB-DFBJGRDBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  9.7
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF<br/>[FR] DÉRIVÉS N-ALKYL ET N-ACYL TÉTRAHYDRO-ISOQUINOLINE SUBSTITUÉS, PROCÉDÉ DE PRÉPARATION ET APPLICATION THÉRAPEUTIQUES ASSOCIÉS
  申请人：SANOFI SA

  公开号：WO2011143145A1

  公开（公告）日：2011-11-17

  The present invention discloses and claims a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). Wherein R, R1, R2, X, 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-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本发明揭示并声明了一系列式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物。其中R、R1、R2、X、m、n和p如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此在制药剂中特别有用，尤其是在治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还揭示了制备式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。
• SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：SANOFI

  公开号：US20130065919A1

  公开（公告）日：2013-03-14

  The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R 1 , R 2 , X, 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 disclosure also relates to methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本公开涉及一系列式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物，其中R、R1、R2、X、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/或预防包括与中枢神经系统相关的多种受H3受体调节的疾病中，特别有用作为药物制剂。此外，本公开还涉及制备式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。
• US8871788B2
  申请人：——

  公开号：US8871788B2

  公开（公告）日：2014-10-28