1-(4-哌啶基)丙酮 | 106140-41-4

• 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: 1-(4-哌啶基)丙酮
• 英文名称: 1-(piperidin-4-yl)propan-2-one
• 英文别名: 1-(piperidin-4-yl)acetone；4-acetonylpiperidine；[4]piperidyl-acetone；[4]Piperidyl-aceton；1-piperidin-4-ylpropan-2-one
• CAS: 106140-41-4
• 化学式: C₈H₁₅NO
• 分子量: 141.213
• InChiKey: LKLPWBVOFQVJKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(4-哌啶基)丙酮 在 盐酸 、 potassium tert-butylate 、 mercury(II) diacetate 、 sodium hydride 、 potassium carbonate 、 甲基磺酰氯 、 三乙胺 作用下， 以 水 、 苯 为溶剂， 反应 33.5h， 生成 4-azatricyclo<5.2.2.0^4,8>undecan-11-one
  参考文献：
  名称：

  Functionalized 2-azabicyclo[3.3.1]nonanes. 6. Studies directed to the synthesis of pentacyclic Strychnos indole alkaloids

  摘要：

  DOI：

  10.1021/jo00378a019
• 作为产物：
  描述：

  1-哌啶羧酸,4-(2-羰基丙基)-,乙基酯 在 硫酸 作用下， 以96%的产率得到1-(4-哌啶基)丙酮
  参考文献：
  名称：

  Functionalized 2-azabicyclo[3.3.1]nonanes. 6. Studies directed to the synthesis of pentacyclic Strychnos indole alkaloids

  摘要：

  DOI：

  10.1021/jo00378a019

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
  申请人：Arvinas, Inc.

  公开号：US20190151295A1

  公开（公告）日：2019-05-23

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the 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 present disclosure exhibits 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.

  本公开涉及双功能化合物，其作为白细胞介素-1受体相关激酶4（IRAK-4；目标蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端结合E3泛素连接酶的Von Hppel-Lindau、cereblon配体的双功能化合物，另一端结合目标蛋白的部分，使得目标蛋白靠近泛素连接酶以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性。本公开的化合物和组合物用于治疗或预防由目标蛋白聚集或积累导致的疾病或紊乱。
• [EN] METHODS OF TREATING ALZHEIMER'S DISEASE USING AROMATICALLY SUBSTITUTED omega-AMINO-ALKANOIC ACID AMIDES AND ALKANOIC ACID DIAMIDES<br/>[FR] METHODES DE TRAITEMENT DE LA MALADIE D'ALZHEIMER AU MOYEN D'AMIDES D'ACIDE O-AMINO-ALCANOIQUE A SUBSTITUTIONS AROMATIQUES ET DE DIAMIDES D'ACIDE ALCANOIQUE
  申请人：ELAN PHARM INC

  公开号：WO2003103652A1

  公开（公告）日：2003-12-18

  Disclosed.are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I) wherein the variables R1, R2, R3, R4, R5, X1, and X2 are defined herein.

  披露了治疗阿尔茨海默病和其他疾病，和/或抑制β-分泌酶酶，和/或通过使用式(I)化合物在哺乳动物体内抑制Aβ肽沉积的方法，其中变量R1、R2、R3、R4、R5、X1和X2在此处定义。
• TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
  申请人：Arvinas, Inc.

  公开号：US20180155322A1

  公开（公告）日：2018-06-07

  The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which 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 present disclosure exhibits 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.

  本公开涉及双功能化合物，这些化合物可用作雌激素受体（目标蛋白）的调节剂。特别是，本公开涉及包含在一段至少有一种Von Hippel-Lindau配体、一种cereblon配体、凋亡抑制蛋白配体、小鼠双分钟同源2配体或其组合的双功能化合物，这些配体与相应的E3泛素连接酶结合，在另一端有一个与目标蛋白结合的部分，使得目标蛋白被置于泛素连接酶附近，以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白降解/抑制相关的广泛药理活性。可以通过本公开的化合物和组合物治疗或预防由目标蛋白聚集或积累引起的疾病或障碍。
• [EN] HETEROCYCLIC SPIRO-COMPOUNDS AS AM2 RECEPTOR INHIBITORS<br/>[FR] COMPOSÉS SPIRO HÉTÉROCYCLIQUES CONSTITUANT DES INHIBITEURS DU RÉCEPTEUR DE L'AM2
  申请人：UNIV SHEFFIELD

  公开号：WO2020099885A1

  公开（公告）日：2020-05-22

  Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1, R2, R4, R5, R6, R7, R8, R9, R10,Z, X1, X2, X3, L2, HET, n and q are as defined herein. The compounds are inhibitors of adrenomedullin receptor subtype 2 (AM2). Also disclosed are the compounds for use in the treatment of diseases modulated AM2, including proliferative diseases such as cancer; pharmaceutical compositions comprising the compounds; methods for preparing the compounds; and intermediates useful in the preparation of the compounds.

  揭示了以下式（I）的化合物及其药学上可接受的盐：其中R1、R2、R4、R5、R6、R7、R8、R9、R10、Z、X1、X2、X3、L2、HET、n和q如本文所定义。这些化合物是肾上腺髓质素受体亚型2（AM2）的抑制剂。还揭示了这些化合物用于治疗调节AM2的疾病，包括增殖性疾病如癌症；包含这些化合物的药物组合物；制备这些化合物的方法；以及制备这些化合物的有用中间体。
• [EN] ANTIMALARIAL COMPOUNDS<br/>[FR] COMPOSÉS ANTIPALUDIQUES
  申请人：LIVERPOOL SCHOOL TROPICAL MEDICINE

  公开号：WO2012069856A1

  公开（公告）日：2012-05-31

  The present invention relates to antimalarial compounds. More specifically, the present invention relates to novel substituted quinolone derivatives of formula (I) and related quinoline derivatives of formula (II) as defined herein that possess potent antimalarial activity. The present invention also relates to processes for the preparation of these quinolone and quinoline derivatives, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of malaria.

  本发明涉及抗疟疾化合物。更具体地，本发明涉及具有强效抗疟活性的本发明中定义的新型取代喹诺酮衍生物（式（I））和相关喹啉衍生物（式（II））。本发明还涉及制备这些喹诺酮和喹啉衍生物的方法，包括含有它们的药物组合物以及它们作为治疗和/或预防疟疾的治疗剂的用途。