(1R,3r,5S)-3-methoxy-8-azabicyclo[3.2.1]octane

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: (1R,3r,5S)-3-methoxy-8-azabicyclo[3.2.1]octane
• 英文别名: (3-Endo)-3-Methoxy-8-azabicyclo[3.2.1]octane；(1S,5R)-3-methoxy-8-azabicyclo[3.2.1]octane
• 化学式: C₈H₁₅NO
• 分子量: 141.213
• InChiKey: GPCOICWXCKOIEM-DHBOJHSNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(2-((S)-2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinolin-3-yl)-2-hydroxyethyl)-4,4-dimethyl-1-oxo-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid 、 (1R,3r,5S)-3-methoxy-8-azabicyclo[3.2.1]octane 在 1-丙基磷酸酐 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 tert-butyl (S)-3-((R)-1-hydroxy-2-(6-((1R,3R,5S)-3-methoxy-8-azabicyclo[3.2.1]octane-8-carbonyl)-4,4-dimethyl-1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate 、 tert-butyl (S)-3-((S)-1-hydroxy-2-(6-((1R,3S,5S)-3-methoxy-8-azabicyclo[3.2.1]octane-8-carbonyl)-4,4-dimethyl-1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
  参考文献：
  名称：

  [EN] PRMT5 INHIBITORS
  [FR] INHIBITEURS DE PRMT5

  摘要：

  本发明提供了化合物的公式（I）或其药学上可接受的盐，这些化合物是PRMT5抑制剂。

  公开号：

  WO2019094312A1

文献信息

• [EN] NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES<br/>[FR] COMPOSÉS TRICYCLIQUES INNOVANTS TELS QUE DES INHIBITEURS D'ENZYMES IDH MUTANTES
  申请人：MERCK SHARP & DOHME

  公开号：WO2017074914A1

  公开（公告）日：2017-05-04

  The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

  本发明涉及式(I)、(Ia)或(Ib)的三环化合物，这些化合物是一种或多种突变的IDH酶的抑制剂。本发明还涉及这些三环化合物在潜在治疗或预防涉及一种或多种突变IDH酶的癌症中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在预防或治疗此类癌症中的用途。
• Tricyclic compounds as inhibitors of mutant IDH enzymes
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10399972B2

  公开（公告）日：2019-09-03

  The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

  本发明涉及式(I)、(Ia)或(Ib)的三环化合物，它们是一种或多种突变 IDH 酶的抑制剂。本发明还涉及这些三环化合物在涉及一种或多种突变 IDH 酶的癌症的潜在治疗或预防中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在预防或治疗此类癌症中的用途。
• NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP3371191A1

  公开（公告）日：2018-09-12
• PRMT5 INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20200354377A1

  公开（公告）日：2020-11-12

  The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.