tert-butyl 4-(piperazine-1-carbonyl)piperazine-1-carboxylate | 203520-35-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: tert-butyl 4-(piperazine-1-carbonyl)piperazine-1-carboxylate
• CAS: 203520-35-8
• 化学式: C₁₄H₂₆N₄O₃
• 分子量: 298.385
• InChiKey: RERBITYCANEVPA-UHFFFAOYSA-N

物化性质

• 沸点：
  418.1±45.0 °C(Predicted)
• 密度：
  1.162±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  65.1
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-(piperazine-1-carbonyl)piperazine-1-carboxylate 在 bis-triphenylphosphine-palladium(II) chloride 、 copper(l) iodide 、 potassium carbonate 、 三乙胺 作用下， 以 1,4-二氧六环 、 乙腈 为溶剂， 反应 144.5h， 生成 1-(4-(4-(4-(piperazine-1-carbonyl)piperazin-1-yl)but-1-yn-1-yl)phenyl)dihydropyrimidine-2,4(1H,3H)-dione
  参考文献：
  名称：

  [EN] BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE
  [FR] AGENTS DE DÉGRADATION BIFONCTIONNELS ET LEURS MÉTHODES D'UTILISATION

  摘要：

  本发明描述了双功能降解剂化合物、它们的多种靶点、它们的制备方法、包含它们的药物组合物，以及它们在治疗由各种靶点蛋白质介导的条件、疾病和失调症中的用途。

  公开号：

  WO2021053495A1
• 作为产物：
  描述：

  哌嗪 、 1-(tert-butoxycarbonyl)-4-(4-nitrophenyloxycarbonyl)-piperazine 以 四氢呋喃 为溶剂， 以74.7 %的产率得到tert-butyl 4-(piperazine-1-carbonyl)piperazine-1-carboxylate
  参考文献：
  名称：

  [EN] CYTOTOXICITY TARGETING CHIMERAS
  [FR] CHIMÈRES CIBLANT LA CYTOTOXICITÉ

  摘要：

  The present disclosure relates to heterobifunctional molecules, referred to as cytotoxicity targeting chimeras (CyTaCs) or antibody recruiting molecules (ARMs) that are able to simultaneously bind a target cell-surface protein as well as an exogenous antibody protein. The present disclosure also relates to agents capable of binding to a receptor on a surface of a pathogenic cell and inducing the depletion of the pathogenic cell in a subject for use in the treatment of cancer, inflammatory diseases, autoimmune diseases, viral infection, or bacterial infection.

  公开号：

  WO2023017484A1

文献信息

• Heterocyclic compounds useful as oxido-squalene cyclase inhibitors
  申请人：Zeneca Limited

  公开号：US06440972B1

  公开（公告）日：2002-08-27

  This invention concerns heterocyclic derivatives of formula (I) which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence the lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.

  这项发明涉及式(I)的杂环衍生物，其在抑制氧化齿萜环化酶方面具有用途，以及其制备方法和含有它们的药物组合物。本发明还涉及能够抑制胆固醇生物合成并因此降低血浆胆固醇水平的杂环衍生物。本发明还涉及在高胆固醇血症和动脉粥样硬化等疾病和医疗状况中使用这种杂环衍生物的方法。
• Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor
  作者：M. Raymond V. Finlay、Mark Anderton、Susan Ashton、Peter Ballard、Paul A. Bethel、Matthew R. Box、Robert H. Bradbury、Simon J. Brown、Sam Butterworth、Andrew Campbell、Christopher Chorley、Nicola Colclough、Darren A. E. Cross、Gordon S. Currie、Matthew Grist、Lorraine Hassall、George B. Hill、Daniel James、Michael James、Paul Kemmitt、Teresa Klinowska、Gillian Lamont、Scott G. Lamont、Nathaniel Martin、Heather L. McFarland、Martine J. Mellor、Jonathon P. Orme、David Perkins、Paula Perkins、Graham Richmond、Peter Smith、Richard A. Ward、Michael J. Waring、David Whittaker、Stuart Wells、Gail L. Wrigley

  DOI：10.1021/jm500973a

  日期：2014.10.23

  receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring sensitizing (or activating) mutations for a number of years. Despite encouraging clinical efficacy with these agents, in many patients resistance develops leading to disease progression. In most cases, this resistance is in the form of the T790M mutation. In addition, EGFR wild

  表皮生长因子受体（EGFR）抑制剂已在临床上用于治疗具有致敏（或激活）突变的非小细胞肺癌（NSCLC）患者，已有多年历史。尽管这些药物具有令人鼓舞的临床疗效，但在许多患者中，耐药性仍在发展，导致疾病进展。在大多数情况下，这种抗性是T790M突变的形式。另外，这些试剂固有的EGFR野生型受体抑制作用可导致皮疹和腹泻的剂量限制性毒性。我们在本文中描述了早期突变选择性导致临床候选药物AZD9291的进化，它是EGFR致敏（EGFRm +）和T790M抗性突变的不可逆抑制剂，对受体的野生型具有选择性。
• [EN] N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES<br/>[FR] DÉRIVÉS DE N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHÉNYL)BENZAMIDE
  申请人：NOVARTIS AG

  公开号：WO2019186343A1

  公开（公告）日：2019-10-03

  The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

  该发明涉及公式（I）的化合物或其药用可接受的盐，其中取代基如规范中定义；涉及制备该化合物的中间体，包括该化合物的药物组合物以及该化合物在治疗疾病中的用途。
• Substituted pyrimidine derivatives and their pharmaceutical use
  申请人：Zeneca Limited

  公开号：US06093718A1

  公开（公告）日：2000-07-25

  This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.

  本发明涉及杂环衍生物，其在抑制氧化齐墨酰基环化酶方面具有用途，以及制备它们的过程和含有它们的制药组合物。本发明还涉及能够抑制胆固醇生物合成并因此降低血浆中胆固醇水平的杂环衍生物。本发明还涉及在疾病和医疗条件（如高胆固醇血症和动脉硬化）中使用这种杂环衍生物的方法。
• 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors
  作者：Italo Beria、Barbara Valsasina、Maria Gabriella Brasca、Walter Ceccarelli、Maristella Colombo、Sabrina Cribioli、Gabriele Fachin、Ronald D. Ferguson、Francesco Fiorentini、Laura M. Gianellini、Maria L. Giorgini、Jurgen K. Moll、Helena Posteri、Daniele Pezzetta、Fulvia Roletto、Francesco Sola、Dania Tesei、Michele Caruso

  DOI：10.1016/j.bmcl.2010.09.060

  日期：2010.11

  A series of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives was optimized as Polo-like kinase 1 inhibitors. Extensive SAR afforded a highly potent and selective PLK1 compound. The compound showed good antiproliferative activity when tested in a panel of tumor cell lines with PLK1 related mechanism of action and with good in vivo antitumor efficacy in two xenograft models after iv administration. (C) 2010 Elsevier Ltd. All rights reserved.