1-(环丙基甲基)-3-甲基-哌嗪 | 82919-92-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 1-(环丙基甲基)-3-甲基-哌嗪
• 中文别名: L-苏氨酸盐酸
• 英文名称: 1-Cyclopropylmethyl-3-methyl-piperazine
• 英文别名: 1-(Cyclopropylmethyl)-3-methylpiperazine
• CAS: 82919-92-4
• 化学式: C₉H₁₈N₂
• 分子量: 154.255
• InChiKey: IWRIBHLFZPQASA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(环丙基甲基)-3-甲基-哌嗪 、 以 四氢呋喃 为溶剂， 反应 12.0h， 生成
  参考文献：
  名称：

  Discovery of γ-secretase inhibitors efficacious in a transgenic animal model of Alzheimer’s disease

  摘要：

  Attachment of the cyclopropylcarbamate group to the piperidine core of gamma-secretase inhibitors leads to a dramatic increase of their in vitro potency. Strategies for subsequent improvement of the in vivo pharmacokinetic profile of the series are discussed. Resulting compounds significantly reduce A beta levels in TgCRND8 mice after a single PO dosing at 30 mpk. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.10.011

文献信息

• Tricyclic inhibitors of the BCL6 BTB domain protein-protein interaction and uses thereof
  申请人：Ontario Institute for Cancer Research (OICR)

  公开号：US11242351B2

  公开（公告）日：2022-02-08

  The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

  本申请涉及式（I）化合物或其药学上可接受的盐、溶液剂和/或原药，涉及包含这些化合物或其药学上可接受的盐、溶液剂和/或原药的组合物，以及在治疗可通过抑制与 BCL6 BTB 的相互作用来治疗的疾病、失调或病症（如癌症）中的各种用途。
• 2,6-Disubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors
  作者：Dmitri A. Pissarnitski、Theodros Asberom、Thomas A. Bara、Alex V. Buevich、John W. Clader、William J. Greenlee、Henry S. Guzik、Hubert B. Josien、Wei Li、Michael McEwan、Brian A. McKittrick、Terry L. Nechuta、Eric M. Parker、Lisa Sinning、Elizabeth M. Smith、Lixin Song、Henry A. Vaccaro、Johannes H. Voigt、Lili Zhang、Qi Zhang、Zhiqiang Zhao

  DOI：10.1016/j.bmcl.2006.09.094

  日期：2007.1

  A novel piperidine series of gamma-secretase inhibitors, potentially useful for the treatment of Alzheimer's disease, is disclosed. SAR investigation revealed the requirement for cis-stereochemistry of the substituents attached to the core, which resulted in the chair-like diaxial conformation of the piperidine ring. The series was optimized to provide inhibitors with IC(50)'s in the single-digit nanomolar range. Absolute stereochemistry of the active enantiomer was assigned. (c) 2006 Elsevier Ltd. All rights reserved.
• TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
  申请人：Ontario Institute for Cancer Research (OICR)

  公开号：EP3728267A1

  公开（公告）日：2020-10-28
• US4474783A
  申请人：——

  公开号：US4474783A

  公开（公告）日：1984-10-02
• Discovery of γ-secretase inhibitors efficacious in a transgenic animal model of Alzheimer’s disease
  作者：Theodros Asberom、Zhiqiang Zhao、Thomas A. Bara、John W. Clader、William J. Greenlee、Lynn A. Hyde、Hubert B. Josien、Wei Li、Andrew T. McPhail、Amin A. Nomeir、Eric M. Parker、Murali Rajagopalan、Lixin Song、Gwendolyn T. Wong、Lili Zhang、Qi Zhang、Dmitri A. Pissarnitski

  DOI：10.1016/j.bmcl.2006.10.011

  日期：2007.1

  Attachment of the cyclopropylcarbamate group to the piperidine core of gamma-secretase inhibitors leads to a dramatic increase of their in vitro potency. Strategies for subsequent improvement of the in vivo pharmacokinetic profile of the series are discussed. Resulting compounds significantly reduce A beta levels in TgCRND8 mice after a single PO dosing at 30 mpk. (c) 2006 Elsevier Ltd. All rights reserved.