1-[1-(4-Methoxyphenyl)sulfonylpiperidin-4-yl]-4-methylpiperidine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-[1-(4-Methoxyphenyl)sulfonylpiperidin-4-yl]-4-methylpiperidine
• 化学式: C₁₈H₂₈N₂O₃S
• 分子量: 352.5
• InChiKey: XCBHYDPDIJQQGM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  58.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-甲基[1,4’]二哌啶 、 对甲氧基苯磺酰氯 生成 1-[1-(4-Methoxyphenyl)sulfonylpiperidin-4-yl]-4-methylpiperidine
  参考文献：
  名称：

  THERAPEUTICS TARGETING TRUNCATED ADENOMATOUS POLYPOSIS COLI (APC) PROTEINS

  摘要：

  所描述的发明提供了小分子抗癌化合物，其选择性靶向并抑制截短的APC蛋白、一种免疫人结肠上皮细胞（HCEC）模型的可测生物活性，并包含至少一种小分子抗癌化合物和药用载体的制药组合物。

  公开号：

  US20150232444A1

文献信息

• [EN] THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER<br/>[FR] AGENTS THÉRAPEUTIQUES CIBLANT LA POLYPOSE ADÉNOMATEUSE COLIQUE (APC) MUTANTE POUR LE TRAITEMENT DU CANCER
  申请人：UNIV TEXAS

  公开号：WO2020117972A1

  公开（公告）日：2020-06-11

  The present disclosure reports an extensive medicinal chemistry evaluation of a large collection of Truncating APC-Selective Inhibitor (TASIN) compounds. The compounds were evaluated for activity against a series of colon cancer cell lines with and without truncating APC-mutations, as well as in an isogenic cell line pair reporting on the status of APC- dependent selectivity. A number of very potent and selective compounds were identified, including compounds with good metabolic stability and PK properties. The small molecules reported herein thus represent a first-in-class genotype-selective series that specifically target ape mutations present in the vast majority of CRC patients, and therefore serves as a translational platform towards a potential targeted therapy for colon cancer.

  本披露报告了对大量截断APC-选择性抑制剂（TASIN）化合物的广泛药物化学评估。这些化合物针对一系列结肠癌细胞系进行了活性评估，包括具有截断APC突变和不具有截断APC突变的细胞系，以及在报告APC依赖性选择性状况的同源细胞系对。鉴定了一些非常有效和选择性的化合物，包括具有良好代谢稳定性和药代动力学性质的化合物。因此，本文报道的小分子代表了一种首创的基因型选择性系列，专门针对存在于绝大多数结直肠癌患者中的猿类突变，因此可作为一个转化平台，朝着结肠癌的潜在靶向治疗迈进。
• COMPOUNDS AND METHODS OF PROMOTING MYELINATION
  申请人：Case Western Reserve University

  公开号：EP3838287A2

  公开（公告）日：2021-06-23

  A method of promoting the generation of oligodendrocytes from oligodendrocyte precursor cells by enhancing their survival and/or maturation includes administering to the cell an effective amount of an agent that enhances and/or induces accumulation of Δ8,9-unsaturated sterol intermediates of the cholesterol biosynthesis pathway in the oligodendrocyte precursor cells.

  一种通过提高少突胶质细胞前体细胞的存活率和/或成熟度来促进少突胶质细胞生成的方法，包括向细胞施用有效量的制剂，该制剂可提高和/或诱导胆固醇生物合成途径的Δ8,9-不饱和固醇中间体在少突胶质细胞前体细胞中的积累。
• Therapeutics targeting truncated adenomatous polyposis coli (APC) proteins
  申请人：Board of Regents of the University of Texas System

  公开号：US10577344B2

  公开（公告）日：2020-03-03

  The described invention provides small molecule anti-cancer compounds that selectively target and inhibit measurable biological activity of truncated APC proteins, an immortalized Human Colonic Epithelial Cell (HCEC) model, and pharmaceutical compositions comprising at least one of the small molecule anti-cancer compounds and a pharmaceutically acceptable carrier.

  本发明提供了选择性靶向和抑制截短 APC 蛋白可测量生物活性的小分子抗癌化合物、永生化人结肠上皮细胞（HCEC）模型，以及包含至少一种小分子抗癌化合物和药学上可接受的载体的药物组合物。
• Compounds and methods of promoting myelination
  申请人：Case Western Reserve University

  公开号：US11344511B2

  公开（公告）日：2022-05-31

  A method of promoting the generation of oligodendrocytes from oligodendrocyte precursor cells by enhancing their survival and/or maturation includes administering to the cell an effective amount of an agent that enhances and/or induces accumulation of Δ8,9-unsaturated sterol intermediates of the cholesterol biosynthesis pathway in the oligodendrocyte precursor cells.

  一种通过提高少突胶质细胞前体细胞的存活率和/或成熟度来促进少突胶质细胞生成的方法，包括向细胞施用有效量的制剂，该制剂可提高和/或诱导胆固醇生物合成途径的Δ8,9-不饱和固醇中间体在少突胶质细胞前体细胞中的积累。
• THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER
  申请人：The Board Of Regents Of The University Of Texas System

  公开号：EP3890715A1

  公开（公告）日：2021-10-13