4-(3-甲基-1-氮杂啶)-哌啶 | 864494-21-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 4-(3-甲基-1-氮杂啶)-哌啶
• 中文别名: 4-(3-甲基-1-氮杂环丁烷基)哌啶
• 英文名称: 4-(3-Methylazetidin-1-YL)piperidine
• CAS: 864494-21-3
• 化学式: C₉H₁₈N₂
• 分子量: 154.25
• InChiKey: MUQXCHGLMDDJBI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  11
• 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：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

文献信息

• [EN] BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY<br/>[FR] MOLÉCULES BIFONCTIONNELLES CONTENANT UNE FRACTION DE LIAISON À L'UBIQUITINE LIGASE E3 LIÉE À UNE FRACTION CIBLANT BCL6
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2021077010A1

  公开（公告）日：2021-04-22

  Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本发明描述了双功能化合物，其作为B细胞淋巴瘤6蛋白（BCL6；靶蛋白）的调节剂。特别是，本发明中的双功能化合物一端含有与相应的E3泛素连接酶结合的Von Hippel-Lindau、cereblon、凋亡蛋白抑制剂或小鼠双分钟同源蛋白2的配体，另一端含有与靶蛋白结合的部分，使得靶蛋白被置于泛素连接酶附近，以促进靶蛋白的降解（和抑制）。本发明中的双功能化合物展示了与靶蛋白降解/抑制相关的广泛药理活性。可以通过本发明中的化合物和组合物治疗或预防由靶蛋白聚集或积累引起的疾病或失调。
• MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE
  申请人：Arvinas Operations, Inc.

  公开号：US20220395576A1

  公开（公告）日：2022-12-15

  Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a cereblon ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
• [EN] QUINOLINE COMPOUNDS AND THEIR PREPARATION AND USE AS ANTIMALARIAL AGENTS<br/>[FR] COMPOSÉS DE QUINOLÉINE, LEUR PRÉPARATION ET LEUR UTILISATION EN TANT QU'AGENTS ANTIPALUDIQUES
  申请人：US HEALTH

  公开号：WO2019217957A1

  公开（公告）日：2019-11-14

  Disclosed are compounds of formula (I) wherein R1, R2, R3, A, and B are as defined herein, and a method of preparing such compounds. Also disclosed are pharmaceutical compositions containing the compound of formula (I) and a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria by killing or arresting the growth of Plasmodium organisms in a mammal, wherein the Plasmodium organisms are in a liver stage, an asexual stage, or gametocytes, comprising administering to an animal an effective amount of a compound of formula (I).
• [EN] ALKYL-SUBSTITUTED COMPOUND<br/>[FR] COMPOSÉ SUBSTITUÉ PAR UN ALKYLE<br/>[JA] アルキル置換化合物
  申请人：SUMITOMO DAINIPPON PHARMA CO LTD

  公开号：WO2020138499A1

  公开（公告）日：2020-07-02

  優れたβ－ラクタマーゼ阻害作用を有する新規な化合物を提供すること。 本発明は、優れたβ－ラクタマーゼ阻害作用を有する式（１ａ）、（１ｂ）または（１１）で表される化合物、またはその製薬学的に許容される塩を提供する。この化合物は、β－ラクタム系薬剤との併用もしくは単剤にて細菌感染症の有用な予防または治療剤を提供する。本発明はまた、種々の疾患のβ－ラクタム系薬剤との併用による治療のために有用な予防または治療剤を提供する。