(1R,5S,8r)-3-benzyl-3-azabicyclo[3.2.1]octan-8-amine | 108640-15-9

• 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: (1R,5S,8r)-3-benzyl-3-azabicyclo[3.2.1]octan-8-amine
• CAS: 108640-15-9
• 化学式: C₁₄H₂₀N₂
• 分子量: 216.326
• InChiKey: QHPWRLXAKMANSW-WDNDVIMCSA-N

物化性质

• 沸点：
  317.1±35.0 °C(Predicted)
• 密度：
  1.082±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.86
• 重原子数：
  16.0
• 可旋转键数：
  2.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  29.26
• 氢给体数：
  1.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  (1R,5S,8r)-3-benzyl-3-azabicyclo[3.2.1]octan-8-amine 在 sodium hydride 、 三乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 3.5h， 生成
  参考文献：
  名称：

  [EN] HETEROCYCLIC AMIDE AND UREA COMPOUNDS AS JAK2 INHIBITORS
  [FR] COMPOSÉS D'URÉE ET D'AMIDE HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE JAK2

  摘要：

  The present disclosure provides heterocyclic amide and urea compounds and compositions thereof useful for inhibiting JAK2.

  公开号：

  WO2024035627A1
• 作为产物：
  描述：

  (1R,5S)-3-benzyl-3-azabicyclo[3.2.1]octan-8-one 在 ammonium acetate 、 甲醇 、 sodium cyanoborohydride 作用下， 以 甲醇 为溶剂， 以60 %的产率得到(1R,5S,8r)-3-benzyl-3-azabicyclo[3.2.1]octan-8-amine
  参考文献：
  名称：

  [EN] HETEROCYCLIC AMIDE AND UREA COMPOUNDS AS JAK2 INHIBITORS
  [FR] COMPOSÉS D'URÉE ET D'AMIDE HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE JAK2

  摘要：

  The present disclosure provides heterocyclic amide and urea compounds and compositions thereof useful for inhibiting JAK2.

  公开号：

  WO2024035627A1

文献信息

• HETEROARYL-SUBSTITUTED SULFONAMIDE COMPOUNDS AND THEIR USE AS SODIUM CHANNEL INHIBITORS
  申请人：Xenon Pharmaceuticals Inc.

  公开号：US20200071313A1

  公开（公告）日：2020-03-05

  This invention is directed to heteroaryl-substituted sulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.

  这项发明涉及杂环取代磺酰胺化合物，包括其立体异构体、对映异构体、互变异构体或其混合物；或其药用可接受盐、溶剂合物或前药，用于治疗与电压门控钠通道相关的疾病或症状，如癫痫。
• [EN] BRIDGED PIPERIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE PIPÉRIDINE PONTÉS
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012116965A1

  公开（公告）日：2012-09-07

  The present invention relates to compounds of formula (l); hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N; hetaryl II is a six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, or N, wherein at least one ring is aromatic in nature; R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen or halogen; R2 is lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, cycloalkyl substituted by lower alkyl or lower alkyl substituted by halogen, or is lower alkyl substituted by hydroxy, or is furyl, or is O-benzyl, (CH2)p-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkyl or by cyano; R3 is hydrogen or lower alkyl; Y is (CH2)n-, -CH2OCH2-, -CH2O-, CH2S-, -CH2SCH2- and is bonded to two of the ring carbon atoms, bonding being to either the ring carbon atoms a and b or the ring carbon atoms c and d; p is 0 or 1; m is 0, 1 or 2; if m is 2 then R1 may be the same or different; -75- n is 2 or 3; o is 0, 1 or 2, if o is 2, then R2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimers disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

  本发明涉及以下式（l）的化合物；hetaryl I 是一个含有1至3个杂原子（S或N）的五元或六元杂芳基团；hetaryl II 是一个含有1至3个杂原子（S或N）的六元杂芳基团，或者是一个含有1至4个杂原子（S或N）的两元环系统，其中至少一个环具有芳香性质；R1 是低碳基、低烷氧基、被卤素取代的低烷基或卤素；R2 是低碳基、被卤素取代的低烷基、卤素、低烷氧基、被低烷基取代的环烷基、或被卤素取代的低烷基，或者是被羟基取代的低烷基，或是呋喃基，或是O-苄基，（CH2）p-苯基，可选择地被卤素、低烷氧基、被卤素取代的低烷基、低烷基或氰基取代；R3 是氢或低碳基；Y 是（ ）n-、- O -、- O-、 S-、- S -，与两个环碳原子结合，结合到环碳原子a和b或环碳原子c和d之一；p 为0或1；m 为0、1或2；若m为2，则R1 可相同或不同；n 为2或3；o 为0、1或2，若o为2，则R2 可相同或不同；或其药用酸盐。本发明的式I化合物是淀粉样蛋白β的调节剂，因此可能对与大脑中β-淀粉样蛋白沉积相关的疾病的治疗或预防有用，特别是阿尔茨海默病，以及其他疾病，如脑淀粉样血管病、家族性脑出血伴淀粉样蛋白沉积、荷兰型（HCHWA-D）、多梗塞性痴呆、拳击性痴呆和唐氏综合征。
• Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors
  申请人：Xenon Pharmaceuticals Inc.

  公开号：US10752623B2

  公开（公告）日：2020-08-25

  This invention is directed to heteroaryl-substituted sulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.

  本发明涉及杂芳基取代的磺酰胺化合物，作为其立体异构体、对映体、同系物或其混合物；或其药学上可接受的盐、溶液剂或原药，用于治疗与电压门控钠通道相关的疾病或病症，如癫痫。
• [EN] HETEROARYL-SUBSTITUTED SULFONAMIDE COMPOUNDS AND THEIR USE AS SODIUM CHANNEL INHIBITORS<br/>[FR] COMPOSÉS DE SULFONAMIDE SUBSTITUÉS PAR HÉTÉROARYLE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE CANAUX SODIQUES
  申请人：XENON PHARMACEUTICALS INC

  公开号：WO2020047312A1

  公开（公告）日：2020-03-05

  This invention is directed to heteroaryl-substituted sulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.